Medicinal Plants in Tropical West Africa (PDFDrive)

Medicinal plants in tropical West Africa
BEP OLIVER-BEVER
Medicinal plants in
tropical
West Africa
WITH ILLUSTRATIONS BY THE AUTHOR
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CONTENTS
Foreword ProfessorG.B.MariniBettolo vii

Preface D r T . A. Lambo ix
Acknowledgements xi
1 Introduction 1
Early traditional medicine 3
Practical therapeutic indications and mechanism of
action of the drugs 6
2 The cardiovascular system 9
I Plants in tropical West Africa with an action on
the cardiovascular system 9
(a) Cardiotonics 10
(b) Cardiac depressants: anti-arrhythmic agents 31
(c) Vascular agents 35
3 The nervous system 56
I CNS stimulants 64
II Plants with a depressant action mainly via the CNS 82
III Peripherally acting depressants of the CN S 92
IV Plants with cholinergic and adrenergic actions 103
4 Anti-infective activity of higher plants 123
I Plants with antibiotic activity 125
(a) Antibacterial plants 125
(b) Antifungal plants 143
(c) Antiviral plants 152
(d) Antiprotozoal plants 160
(e) Antimetozoal plants (anthelmintics) 169
II Plants with insecticidal or molluscicidal activity 176
(a) Insecticidal plants 176
(b) Molluscicidal plants 186
5 Hormones of the adrenal cortex 191
I Introduction: the action of plants on hormone secretion in Man 191
II Plants acting like hormones of the adrenal cortex 192
Anti-inflammatory plants 195
6 Sex hormones and thyroid hormones 215
I Sex hormones 215
(a) Female sex hormones 215
(b) Plants in birth control 218
(c) Male sex hormones (androgens) 241
II Thyroid hormones 241
7 Oral hypoglycaemic action 245
I Plants containing hypoglycaemic phytosterin glycosides 246
II Plants containing hypoglycaemic alkaloids 250
III Plants containing hypoglycaemic organic sulphur compounds 255
IV Hypoglycaemic plants containing anthocyanins, catechols or
flavonoids, or their glycosides and/or tannins 257
V Hypoglycaemic plants containing other active constituents 264
VI Mechanism of action of hypoglycaemic plants 264
VII Sweetening agents 265
Notes 268
References 269
General references 269
References for Chapter 1 270
Botanical and general index 355
FOREWORD
In 1975 I began to be interested in the study of the active principles of African

medicinal plants and searched for relevant literature. At the time I was particularly
interested in receiving more information on West African plants as we were
developing experimental work in collaboration with the Chemistry Department of
the Nigerian University of Nsukka and I became aware of the great difficulty in
finding fairly reliable documentation even on some of the best-known traditional
herbal remedies.
Factors which may account for this are that the local uses were very numerous and
often differed from one tribe, village or healer to another. Also, not only did
superstition play an important part (often both magical purposes and empirical
beliefs were attributed to the plants) but purgatives, diuretics and emetics were often
used to chase the evil influences the people did not understand.
The patient work of some distinguished scholars working in the field in Africa
provided an important contribution to our acquisition of knowledge on the tra-
ditional uses but only a few publications gave a more selective view on the subject.
Among these one of the most relevant to me was the book of Dr Bep Oliver
(Oliver-Bever), Medicinal Plants in Nigeria. She selected uses which were confirmed
by the use of the same plants as cures by primitive populations in other parts of the
world with similar climate, and also those which were likely to have real therapeutic
value from a consideration of the then known chemical and pharmacological
information.
Dr Oliver's book, which was published in Nigeria in 1960, was the best I could
expect for what I needed, but it was out of print and completely unavailable. By
courtesy of the author, who showed me her copy, I managed to obtain photocopies
of some parts and I considered myself very lucky. At the same time I thought that
this important material had to be republished so that this information on the
Nigerian plants could be available to scientists and therefore suggested to Dr Oliver
that she prepare a second edition of her publication.
It was a real pleasure when I learned that Dr Oliver was preparing not just a second
edition of the first book but a new book on medicinal plants in West Africa including
Vlll
much of the information present in the earlier book but covering a larger area and
with up-to-date bibliographical information on botanical, pharmacological and
chemical aspects and properties of the plants.
The book covers a large number of plants. Confronted by the difficulty of finding
a proper classification of the very abundant material, the Author has chosen a
simplified pharmacological approach, presenting in different chapters the plants
with constituents which act on the cardiovascular system, on the nervous system, on
infectious diseases and on hormone secretions in man.
The great interest of this publication is that it contributes to the knowledge of the
basic principles of the plants used in traditional therapy in tropical West Africa. It
provides the exact botanical identity and synonyms of the plants mentioned: many
people involved in the study of African plants found most of their difficulties in
obtaining the exact identification. The book also gives the known chemical aspects
of the active constituents of the plants, based on recent published data.
Parallel to the traditional uses of the mentioned plants a modern pharmacological
appreciation or interpretation is given, and where traditional medicinal uses may
lead to quoting a number of claimed and non-documented results of the treatments
with the plants, the data reported in the above-mentioned sections are presented
scientifically and based on abundant literature.
The interest of the book exists not only in its multidisciplinary aspect but also
because it suggests areas for further research.
In my position as a chemist devoted for many years to research into the biologically
active principles of plants, I found in Dr Oliver's book a great deal of very important
information for research and a basis for an important aspect of traditional medicine
in Africa. This work, to my opinion, fits perfectly in the WHO program on
Traditional Medicine, for a better knowledge of plants used in a vast area of Africa,
and will surely contribute to better health care of these populations.
Professor G. B. Marini Bettolo

Professor of Chemistry, University of Rome
'La Sapienza', Roma
Chairman, Scientific Committee, WHO Coordinating Centre

for Traditional Medicine, Instituto halo Africano, Roma
PREFACE
Plants and herbs have been used by man to cure disease and heal injuries since time
immemorial. In recent years, renewed interest has been shown in the use of
medicinal plants, and scientific studies are beginning to explain some of the curative
phenomena associated with traditional herbal remedies. There has also been
growing awareness by governments, and the scientific and medical communities, of
the importance of medicinal plants in health care systems in many developing
countries. This has led the World Health Organization to develop an international
programme which will, inter alia, review available scientific data relating to the
efficacy of medicinal plants in the treatment of specific conditions and diseases. A
major task therefore will be to identify those plants suitable for use in primary health
care, and to identify simple and/or intermediate technology that will produce
enough drugs and therapeutic agents at low cost.
This work presents clear and concise scientific data on the pharmacology of West
African plants and extends our knowledge of medicinal plants in West Africa. It will
be of particular value to those interested in specific drug applications and will further
encourage research into local herbs which in its turn will generate technology locally;
this is more reliable and more relevant than introduced technology.
The flora of tropical West Africa has for centuries provided a wealth of material
for healing purposes, and its further investigation presents a challenge to scientists
who seek to contribute to the search to find new means of alleviating suffering and
disease.
The author has put many years of labour and meticulous research into this work,
thefindingsof which are presented clearly and succinctly in this book.
DrT. A. Lambo
Deputy Director-General
World Health Organization
Geneva
9 January 1984
ACKNOWLEDGEMENTS
I want to thank Dr Lambo, Deputy Director of the World Health Organization in

Geneva for the interest and encouragement he showed all these years for my work
and also want to thank him and his coworkers for helping me with some practical
problems and arranging for some photographs to be made of a few of my water-
colours.
I also am grateful to Dr Laurent Rivier and Mr Ian Holmes, editors of the Journal
of Ethnopharmacology in Lausanne, in which the first chapters of this book were
published in order to raise an interest, for encouragement, useful criticism and
minor corrections.
In addition I want to acknowledge the kind assistance of Professor Norman
Farnsworth, Professor of the Department of Pharmacognosy and Pharmacology at
Illinois University, USA, and Dr David Griffin, Manager of Research in Human
Reproduction at the WHO, in providing recent documentation allowing me to select
the more important information in the very extensive field of antifertility plants.
My thanks also go to Dr Norman Langford, Freelance interpreter at the United
Nations for reading through part of the text to check my English, which is not my
mother tongue.
I would also like to acknowledge the great kindness of Dr Dinah James, OBE,
former Professor of Pharmacology in Nigeria, in reading through a great part of my
text and for her extremely helpful suggestions, queries and corrections.
My thanks also go to Mrs Louise Sanders, subeditor of Cambridge University
Press, for her help in preparing the text for publication.
Throughout the text, the descriptions of the plants include some of the local
medicinal uses (L), the chemical constituents (where known) (C) and the phar-
macological and clinical actions of the plant concerned (P), when this knowledge is
available. As a short and therefore incomplete botanical description could be
misleading, no botanical details have been given. These can be found in the revised
edition of Hutchinson and Dalziel's Flora of West Tropical Africa (1954-72), which
provided the information for the occurrence of the plants described and their names
and synonyms. Non-indigenous plants currently cultivated or grown in the area
have also been included in the book, this being mentioned in the text or indicated in
the tables by c. before or after the botanical name.
Thus:
L indicates local uses
C indicates chemistry
P indicates pharmacology
c. indicates non-indigenous plants
Within each therapeutic group, plants are, as far as possible, assembled by
chemical constituents. A chemical relationship often exists in the same botanical
family, hence the plants are assembled by families within these groups. The des-
criptions, when dealing with well-known plants appearing in most Pharmacopoeias,
have been restricted to a few essentials; details are available in most standard
textbooks. On the other hand, West African plants which, while less well known,
seem of potential medicinal interest have been treated in greater detail, in the belief
that such details might prove useful in further scientific investigations. Some plants
with weaker pharmacological action or with higher toxicity have also been included
as further research and chemical separation might enable their use.
Many plants contain a number of different constituents and if these are employed
for different purposes the plant may appear under several pharmacodynamic
groups. To avoid repetition for plants already described, their action(s) will be
mentioned only briefly and for further details reference will be made to earlier
information.
Introduction
This book is a sequel to the monograph Medicinal Plants in Nigeria, written in 1960
(Oliver, 1960), which was a critical survey of the scattered information available
about drug plants found in Nigeria; it suggested a first choice of the plant material
which seemed potentially most important, and made suggestions concerning points
requiring further scientific investigation (constituents, pharmacology, etc.).
As medical science develops and becomes more organized in the West African
countries, the time would seem to have come to reassemble and update our
knowledge of the subject and extend it to the whole of tropical West Africa.
Furthermore, greater importance is now being attached to the use of locally available
medicines as a means of reducing reliance on expensive imported drugs.
Since the first book appeared, a number of papers dealing with the chemical
analysis, pharmacology and clinical action of West African plants have been
published. Supplementary information now available about individual plants will be
included here, and the range of plants considered can thus be more selective. This
time an attempt is made to classify the drugs according to their established or
possible medical uses, this being the best way of rapidly assessing the medical
interest of any particular drug.
The value of a drug will depend on several factors:
(1) whether it is the only drug, or one of the few drugs, used in the treatment of
a disease;
(2) whether the disease in the treatment of which it is used is a common one;
(3) whether it is less toxic than other existing drugs for a particular purpose;
(4) whether it can be produced more cheaply than alternative drugs used in
treating the same disease.
This last criterion may hold good for plants grown for other commercial uses (fibres,
timber, fixed oils (liquid fats or fatty oils), essential oils, gums, resins, etc.), for in
such cases the drug may be available as a by-product, with a substantial cut in
production costs.
The following points, which were mentioned in my earlier publications, still hold
good:
(a) Recognized drug plants which also grow in West Africa and are officially
listed in various Pharmacopoeias or are already in use elsewhere have to be
checked by well-established methods to ascertain whether the yield in
active constituents of the plant when grown in West Africa reaches a suit-
able standard. If it does, the plant can, if not indigenous, be grown on a
greater scale and the relevant drugs produced by standard procedures.
(b) The therapeutic action of a plant depends on its chemical constituents and
can often be forecast and easily investigated pharmacologically if these
constituents are known.
(c) The botanical relationship of a particular plant to well-known drug plants,
or to plants containing therapeutically active constituents, may be an indi-
cation of a potential therapeutic interest. Indeed, chemical relationship,
based on secondary substances specifically found in certain genera and
families, has been observed and is made use of in botanical taxonomy.
Several genera of one botanical family may thus have a similar action. Many
Solanaceae contain alkaloids with a parasympatholytic action, and many
Labiatae contain essential oils, while cardiac heterosides are often found
among the Asclepiadaceae and Apocynaceae.
(d) As many plants found in tropical West Africa also grow in other areas of
similar climate, such as parts of India, Sri Lanka and Indonesia, their use in
such countries will require investigation too. However, an attempt ought
to be made to ascertain whether the African plants have the same constitu-
ents in equivalent quantities, and the same properties, for in these other
countries the content of active principles may not be the same. Such
differences may be attributed to differences in climate, soil or other eco-
logical conditions, but are more likely to be due to varying degrees of enzy-
matic destruction of the chemical principles (Debray, 1966, p. 51, quoted
inOliver-Bever, 1968).
(e) Local medicinal usage may provide useful information about lesser-known
plants. Unfortunately, local uses can be very numerous and often differ
completely from one tribe to another for one and the same plant. It should
not be forgotten that superstition plays a considerable part in folk medi-
cine. Vesicants, purgatives, diuretics and emetics are often used because
they 'oppose strong action' or 'expel evil influences'. However, the herbal-
ist is sometimes right and then his medicine has to be investigated further.
In some cases certain local plants are used in the same way by many different
tribes, or for similar ailments in other parts of the world where such plants are also
found. This would seem to make this use more likely to be accurate. It could,
however, be empirical and might be based, for instance on the 'Law of Signatures',
which has adepts among several under-developed peoples existing without contacts.
Hence in 1960 the local uses indicated for tropical West Africa (Dalziel, 1937) were
compared with the uses to which the same species are put in India (Chopra et al.,
1956), Sri Lanka (Jayaweera, 1945,1952,1954), Indonesia (van Steenis-Kruseman,
1953), the Ivory Coast (Kerharo and Bouquet, 1950), Ghana (Irvine, 1930), Senegal
(Sebire, 1899; Chevalier, 1905-13), Guinea (Pobeguin, 1912), the Congo (Staner
and Boutique, 1937), Nigeria (Holland, 1908-29), Africa in general (Githens, 1949),
etc. This resulted in a fairly rigorous selection of local medicinal uses and this
information was partly made use of in the preparation of the present text. Some
interesting indications may thus well have been overlooked, but a rapid survey of the
existing knowledge seemed to be the first requirement. More detailed and more
up-to-date information on local medicinal uses can be found in the 'Memoires'
published by the Office de la Recherche Scientifique et Technique Outre Mer
(ORSTOM) (see e.g. Bouquet, 1969) in Kerharo and Adam (1974) and in Ayensu
(1978). These latter books (and some of the others) also give the vernacular names of
the plants they deal with.
Throughout the text, the phrase 'plants acting on . . . ' i s used as convenient
terminology for 'plants whose leaves (or roots, extracts, active principles, etc.) act on
. . .' . The chapters themselves are named on the basis of the physiological system
affected.
Early traditional medicine

Treatment has been provided in West Africa by the native 'doctors' (ifas,
juju men and herbalists). The juju man is believed to be able to get the support of the
gods (through magic and tribal rituals) for the numerous problems affecting his
applicants. He not only treats diseases, which the people consider to be an adversity
imposed upon them by outside forces they do not comprehend, but is also required
to be a rainmaker or to perform rites to ensure good crops, prosperity, etc., or to help
in calamities caused by offended dead relatives or evil spirits (Oliver-Bever, 1983).
Therefore his aims, being so closely related to mystic practices, are often more
concerned with the spirit than with the body. It seems that early civilizations felt the
importance of a psychosomatic approach to illness long before this received attention
in modern medicine!
A great quantity and variety of 'medicines' based on plants, or parts thereof
(Oliver, 1960), are given by the different herbalists throughout West Africa. Often
they are sold in the markets to people in search of cures and a great number are
'assured' to heal almost every disease under the sun: others have a definite use. Of
course, this materia medica is by no means limited to plants, and frequently in 'strong
medicines' components like the heart of chicken, animal remains, human saliva and
even flesh and blood are part of the preparation. Generally, the drugs are made up in
the shape of small rissoles or balls of mastic, but liquid potions, ointments or powder
can also be found and even enemas or fumigations are used in a local fashion.
The knowledge of the properties of the drug plants shown by some local juju men
may either have been passed on to them by their elders or be based on experience.
Frequently, neither the 'doctor' nor the patient attributes the action to the plant
itself, a situation reminiscent of a similar attitude in Europe in the Middle Ages.
Indeed, disease in old Anglo-Saxon times was attributed to 'possession by devils' or
to 'flying venom' or to 'the loathed things that rove through the land' (Rohde, 1922).
To counteract these evils, religious rites, together with herbs and charms of
traditional value, were employed not only for man but also for his cattle (Rohde,
1922) (religion was the outward sign of man's appeasement of forces that he did not
understand). Also, it was superstitiously believed that when a plant was pulled out
of the ground it uttered shrieks and caused death or at least insanity to the gatherer
if he heard them (Lloyd, 1921). Shakespeare refers to this belief in Romeo and Juliet
when he writes (Act 4, Scene 2): 'shrieks like mandrakes torn out of earth, that living
mortals, hearing them, run mad . . .'. The problem of gathering the root, therefore,
was overcome by tying a dog to the plant while the gatherer stopped his ears lest he
should hear anything.
The if a may say that he has discovered a plant possessing a spirit stronger than the
disease spirit, and he and his patients believe that the power of this spirit, or the soul
of the medicine, is not manifested before the healer has spoken some magic words or
has chanted an incantation over the plant. Before doing so the if a himself may appeal
for advice to gods or worship idols which in Yoruba country (Western Nigeria) are
often small carved figures of a man or woman and sometimes also of animals. The
patients in turn should not only take or apply the medicine but also appeal to and
make offerings to communal and household gods, which may also be carved statues
or other objects blessed by the local priests in ceremonies that generally last for days.
In a school in Badagry (Nigeria, near the frontier with Dahomey) there were in a dark
corner places of sacrifice consisting of cones of clay with an irregular shiny surface.
They were streaked in white, turquoise, yellow and brown by the numerous
offerings that had been made, and had the odd piece of eggshell and feather glued to
them. Trees can also be idols, for example the iroko tree, Chlorophora excelsa, which
is regarded as a sacred tree by the Ibos (Eastern Nigeria) and is credited for
'furnishing souls for the newborn'. Sacrifices are made to this tree and offerings are
often found at its base. The household gods (Jkenja) are always carved from
iroko-wood and pieces of its bark are added to many medicines to increase their
action.
Another rare but interesting tree used by the juju men is Okoubaka aubrevillei. The
bark is used by the Binis (Eastern Nigeria) to drive away evil from a house or to inflict
a curse upon an enemy. The bark, according to Hardie (1963), may be removed but
never at sunset or sunrise when it 'spits poison' (the foliage then exudes a dark
poisonous liquid). Before removal of the bark, however, the spirit of the tree must
be propitiated by the offering of gifts. These usually consist of portions of kola nut,
white yam, coco yam and plantain, two cowrie shells, a piece of white drill cloth and
a quantity of chalk. With these it is possible to approach an Okuobisi (its local name)
after having stripped off all clothes at a safe distance. The gifts are laid at the foot of
the tree and at the same time the spirit is begged for whatever help may be required.
A small piece of bark can now be removed with the aid of a wooden batten (under no
circumstances may a machete or metal implement be used) after which it is advisable
to run away quickly 'out of sight' and to re-dress. The reason for this is that the spirit
of the tree may not have been sufficiently appeased by the gifts and if it pursues the
applicant it will fail to recognize him fully clothed.
An Ibibio in trouble may say to the iroko: 'Oh tree! you who are a strong man and
to whom heavy things are light, I am only a small weak creature, and my worry is so
big that I cannot carry it, will you, who are strong, take it from me? It would be a
straw to you.' And he will sacrifice to the tree and leave in peace, convinced that his
burden will be taken from him.
Formerly, plants were used not only for healing but also for killing. Arrow poisons
were prepared by rubbing certain seeds between two stones until they formed a paste
to which was added saliva and the juice of different toxic plants. A vesicant latex, for
example from Euphorbia spp., was often used as this damaged the skin, thus
facilitating penetration and absorption. Often the remains of animals were also
added for magic purposes. Another method consisted of extracting the active
constituent, generally with water or palm wine, and concentrating the extract until
it formed a paste. If the poison was part of the latex of a plant then the latex might be
dried out until it had the right consistency.
In trials by ordeal, a man suspected of evil influence or action was forced with
much ceremony to swallow a dose of poison. If he survived, this was the wish of the
tribal gods and he was considered innocent; if he died this was evidence of guilt. A
classical example is the trial of Lander in Badagry in 1827. Fortunately, Lander, who
had been given a decoction of a portion of bark from Erythrophleum guineense (Sassy
bark), which contains erythrophleine, a strong heart poison, was wise enough to take
a violent emetic immediately afterwards and so survived.
Apart from the local juju men, who treat the more complicated and resistant cases,
the more common ailments are treated by villagers, generally elderly women, with
knowledge of the local plants. The reasons for the local selection of drug plants is
varied. In a number of cases prescriptions are based on the observation of what
happened to animals and men who had eaten certain plants accidentally. In other
cases it was noticed that the plants produced, for example, a local irritation of the
skin but at the same time relieved a pain or cleared up a sore on persons who touched
them, and so local inhabitants used such plants in this way.
Other uses are just empirical, for example those based on the 'Law of Signatures'.
This is an old belief which says that nature has provided a plant for every disease and
has indicated by an obvious sign for which disease or which part of the body each
drug plant is to be used. Thus the shape of a plant or of one of its components may
suggest a cure. This belief existed in many parts of the world, including Europe in
the Middle Ages. The classical example was a walnut, which having the shape of a
brain, should thus be used for diseases affecting the brain. Grier (1937) cites other
examples: 'Plants with red flowers were to be used in blood disorders and those with
yellow flowers, also turmeric, in jaundice. Saxifrages, which grow on rocks and
break them up, would be useful for stones in the bladder, a belief in the Middle Ages
in England (Grier, 1937). Euphrasia was to be given in eye diseases, because a black
spot in the flower resembles the pupil of the eye.' Similar beliefs are prevalent in
primitive West African medicine and have been documented by many authors.
. . . plants with white latex are used to increase milk production; those with big
swollen fruits to favour fertility (Githens, 1949): Commelina, with its bright blue
flowers like eyes, for ophthalmic treatment (Dalziel, 1937, p. 465): Eryngium
foetidum, a plant with a powerful odour, is supposed to bring a person to his senses;
the stems of Palisota hirsuta, with joints which are swollen and bend like a knee, are
used for sprained knees; and the bark of Pentaclethra macrophylla, a tree which never
grows straight but always has a hump in the trunk, is part of a preparation applied to
the hump of a hunchback. The leaves of Ficus exasperata (sandpaper leaves) are
cooked with salt fish and eaten with the idea that these scratchy leaves will scrape out
whatever is causing the trouble (Harley, 1941).
On similar lines it is believed that 'the administration of owl's feathers makes the
disease fly silently away' (Githens, 1949, p. 2). In the Carneroons, for the treatment
of migraine, a spider's web spun on the grass is found, and grass, web and all are
mixed with white clay and rubbed on the patient's head. As the spider runs away on
its web, so will the headache run away (Talbot, 1926). Also, abuse exists like
everywhere else, and Gerarde's comment on the use of henbane seeds to cure
toothache (Woodward, 1931) is reminiscent of practices used in West Africa by some
unconscientious healers. He writes: 'The seed is used by Mountibank toothdrawers
which run about the country, to cause worms come forth of the teeth, by burning in
a chafing dish or coles, the party holding his mouth over the fume thereof; but some
crafty companions to gain money convey small lute-strings into the water, persuad-
ing the patients that those small creepers came out of his mouth and other parts
which he intended to ease.'
Even in those parts of the world where different populations communicated, often
through Greek or Latin texts, and where drugs were received by overland or sea
routes from China, India and the Far East (Gunther, 1934), it took from ancient
times until the eighteenth century before the causes and treatment of illness began
to be understood. The folklore of young isolated communities, still based on a
scheme similar to that of Anglo-Saxon medicine in the Middle Ages, is therefore not
surprising but it is rapidly disappearing with the development of communications
and education.
Practical therapeutic indications and mechanisms of action of the drugs

A distinction should be made between the practical use of a drug and the
way in which it acts. The therapeutic effects of a number of plants are the result of
their action on the nervous system.
First brief mention should be made of the mode of action of the drugs on the
nervous system. Their activity may be the result of:
(a) stimulant or depressant effects on the central nervous system, activity
being exerted at various levels from the higher centres to peripheral nerve
terminals;
(b) modulating effects on autonomic nervous system activity.
The therapeutically useful effects are those that are selectively induced at
important sites mainly by substances which simulate (mimic) neurotransmitters or
interact with them or their receptors.
Plants acting on the cardiovascular system (Chapter 2) mainly produce their
effects through the autonomic nervous system (ANS). Autonomically innervated
structures are regulated at a subconscious level by nerve fibres from the sympathetic
and parasympathetic divisions. The influence of each division varies with each
tissue, i.e. sympathetic activity augments the heartbeat but inhibits the tone of
intestinal and bronchiolar muscles. Constituents which stimulate the release of the
neurotransmitter (noradrenaline) will increase the adrenergic effects but drugs
which antagonize its activity give prominence to the cholinergic division and an
exaggeration of the cholinergic effects (Fig. 1.1).
The cardiovascular plants have been grouped into:
(a) cardiotonics, which are mainly used for their positive inotropic effects,
produce reinforcement of the contractibility of the heart;
(b) cardiac depressants, which are mainly used for their positive or negative
chronotropic effects, regulate the rhythm in tachycardia and fibrillation;
(c) vascular agents, the action on the blood pressure being treated here as well
as their action on vascular solidity, the permeability of capillaries and blood
coagulation and formation.
The ANS intervenes in many different functions of the organism. I have given the
descriptions of the plants under their principal effect, which is likely to control the
practical demand, rather than by their mode of action. Drugs affecting bronchial,
intestinal or uterine motility are described under their stimulating or antispasmodic
effect on the smooth muscles.
In Chapter 3 (The nervous system) I discuss mainly those plants used in mental
treatment, including sedatives, hypnotics, tranquillizers, anticonvulsants and hal-
lucinogens having a stimulating or depressant action on the central nervous system
(CNS) or the ANS. Analgesics, antipyretics, anaesthetics and antispasmodics are
also included in this chapter.
The mechanism of action of the drugs acting via the nervous system is believed to
be based on their interference with the action of chemical substances such as
acetylcholine and the catecholamines, the chemical mediators of nervous trans-
mission. This interference may occur through affinity of the plant constituents for
specific receptors, which can be cholinesterase, adenylcyclase or other enzymes or
Fig. 1.1. Action and sites of action on the ANS.

ADRENERGIC (Sympathomimetic)
SYMPATHETIC DIVISION
acts on peripheral adrenergic
nerve endings
A SUBSTANCES (mydriasis (ocular))
ADRENERGIC (Receptor and neurone
a and /? receptor sites) ANTAGONISTS
PARASYMPATHETIC CHOLINERGIC (Parasympathomimetic)
ANS
ACTIVITY
DIVISION
acts on peripheral cholinergic A SUBSTANCES (myosis (ocular))
nerve endings (muscarinic
receptor sites) "1: CHOLINERGIC (Antimuscarinic)
ANTAGONISTS
GANGLION
PARASYMPATHETIC
and SYMPATHETIC A STIMULANTS
DIVISIONS
lact on autonomic ganglia
H GANGLION
BLOCKERS
8
other macromolecules. Blocking at different peripheral levels leads to more or less

specific physiological effects. For more information on pharmacodynamic proper-
ties, specialized literature should be consulted.
Higher plants used in anti-infection therapy (Chapter 4) need to have different
properties as they must be toxic towards organisms that are infectious to or parasites
of Man but without notable action on the human beings. As could be expected, the
mechanism of action of the plant components varies not only from group to group
but also within several groups: there are different mechanisms of action often at a
cellular level, through enzymatic cell-receptors. Their supposed mode of action,
where known, is indicated under the corresponding groups of plant components.
Where plants acting on hormone secretion in Man are concerned (Chapters 5, 6
and 7), it has been noted that some plant constituents can directly replace certain
hormones in their biological functions because they have an almost identical or
very similar chemical structure to that of the hormones concerned. Other plant
constituents exert their action indirectly by stimulating or inhibiting the secretion of
the hypothalamus or the pituitary or of enzymes which intervene with the secretion
of certain hormones.
However, as future research will no doubt reveal, there are many more ways in
which the secretion of hormones can be stimulated or inhibited. This is illustrated
by details found under sections dealing with hormone secretion such as plants with
anti-inflammatory, oestrogenic, antifertility controlling, hypoglycaemic and other
activities on human hormone secretions.
The cardiovascular system
I Plants in tropical West Africa with an action on the

cardiovascular system
In the particular field of cardiovascular drugs, plants still provide the basis
of treatment, even in orthodox pharmacy. However, some of the plants accepted by
most Pharmacopoeias, such as Digitalis, Convallaria, Adonis, Helleborus and
Crataegus, which act mainly on the heart, and Hydrastis, Veratrum, Amni visnagi,
Viscum album and Aesculus hippocastanum, which act more specifically on the blood
vessels, do not grow in West Africa. On the other hand, the possibilities of many
plants that are locally available have not yet been fully investigated. Also, some of
the currently used cardiotonics have a high toxicity; less toxic but yet active
constituents might be found amongst the West African plants. As mentioned in the
general introduction only a limited number of local uses have been indicated.
Most herbalists will know that many plants in this group (several formerly used as
arrow poisons1 or even in ordeals) are very toxic and will avoid using them. A few
healers, however, may, in view of the fact that they are also emetics, purgatives or
diuretics, be tempted to make use of them. But these plants should be employed only
after complete extraction and with very exact dosages of the active constituents, and
then only by physicians in possession of a full clinical diagnosis. In this, these plants
differ from many others, which may be given as a decoction, an infusion or in dried
or powder form.
Cardiovascular activities are mainly controlled by the ANS. The ANS can be
divided into two main divisions. One, which through the influence of noradrenaline
on the corresponding nerve endings has a stimulating effect on the heart and
produces vasoconstriction, is called the adrenergic or sympathetic division. The
other, which through the influence of acetylcholine slows down the heartbeat and
produces a fall in blood pressure and vasodilatation, is called the cholinergic or
parasympathetic division. Both these divisions can stimulate or antagonize (block)
the autonomic ganglia (Fig. 1.1, p.7).
The actions of acetylcholine at the peripheral cholinergic nerve endings are known
as its muscarinic actions, because they are mimicked by muscarine (a mushroom
alkaloid).
10
Stimulation of the preganglionic nerve fibres to the ganglia results in liberation of

acetylcholine (physiological neurotransmitter in autonomic ganglia). This action is
almost immediately counterbalanced by cholinesterase, which destroys acetyl-
choline through hydrolysis. The cholinergic actions on the ganglia are referred to as
the nicotinic actions of acetylcholine because the effects of acetylcholine on the
ganglia are similar to those produced by nicotine. There is initial stimulation and
then blockade of the ganglion cells (Turner and Richens, 1978).
Changes in the force of contraction of the myocardium are called inotropic effects
while changes in the heart rate are called chronotropic effects. The myocardium,
which contains the p receptors for noradrenaline, responds to this by increasing the
frequency and amplitude of the heartbeat (Lechat et al.91978).
The plants which act on the cardiovascular system can be divided into three
groups:
(a) Cardiotonics. Cardiotonic drugs act on the force, the rate and the rhythm
of the heartbeat. They have a stimulating effect on the cardiac muscle and
thus increase the contractile force (inotropic effect), decrease the heart rate
and regularize the heartbeat (chronotropic effect). By increasing the renal
bloodflow, cardiotonics can have a diuretic action. They often produce
nausea and vomiting as they irritate the gastric mucosa, and are sometimes
used in small doses for their expectorant action, which precedes the
vomiting. By increasing the pulse rate, cardiotonics can also increase the
blood pressure.
(b) Cardiac depressants. These drugs have a depressant effect on the heart
muscle and some are particularly suited to the treatment of arrhythmias
(anti-arrhythmic drugs). By slowing the cardiac rhythm they often have an
antihypertensive action, either through vasodilatation of the coronary
arteries or through direct control by the nervous system.
(c) Vascular agents. These are plant constituents which act primarily on the
blood vessels.
(a) Cardiotonics
Today the plant cardiotonics are generally used in orthodox pharmacy as
isolated active principles. Many of the plants formerly used in Africa as arrow
poisons have been shown to contain cardenolides and to be valuable in minute doses
in treating heart conditions. Cardenolides are steroid heterosides. Their aglycones
(or genins) are responsible for the specific action but do not act by themselves as they
are insoluble and have a low power of fixation on the heart muscle (Mcllroy, 1950,
p. 79). The fixation on the tissues of the isolated frog heart could be attributed for
certain components like flavotannins from Paullinia pinnata (see below) to the
formation of a complex with calcium on the surface of the heart tissues (Bowden,
1962; Broadbent, 1962).
Table 2.1. Apocynaceae in tropical West Africa
In the leaves of the members of the Apocynaceae free ursolic acid is frequently found (Alstonia boonei, Rauvolfia vomitoria, Pleioceras barteri,
Thevetia neriifolia, etc.)? whereas in the coagulum of the latex the triterpenic alcohols /3-amyrin are often present. As most of the plants contain a
very great number of alkaloids or heterosides, only the main constituents and their most important uses have been indicated.
It appears from the table that only the Plumeroideae contain indole alkaloids and steroid alkaloids, whilst the Echitoideae and Cerberoideae
contain cardiac glycosides. However, from studies of the way in which the constituents are built up it appears that the Apocynaceae are able,
starting from a steroid nucleus, to produce either cardiac heterosides or steroid alkaloids, thus bringing the members of this family nearer than
they might appear atfirstsight (Goutarel, 1964; Paris and Delaveau, 1966). On the other hand, Paris and Delaveau (1966) mention the fact that
the same 'specific' chemical constituents are sometimes found in families which are far apart in their morphological classification. Thus in West
Africa cardiac glycosides are found not only in plants of the Apocynaceae and Asclepiadaceae but also in members of the Liliaceae (Urginea indica),
Moraceae (Antiaris africana), Tileaceae {Corchorus olitorius), Sterculiaceae {Mansonia altissima) and even Compositae (Vernonia colorata).
Similarly, indole alkaloids are also found in Rubiaceae (Mitragyna inermis,M. macrophylla, Corynanthepachyceras, Pausinystaliajohimbe, etc.), and
steroid alkaloids also occur in some Solanum species (Solanum nigrum, S. lycopersicum (Oliver-Bever, 1968).
Recognized or possible
Plant Part used Active constituent(s) Chemical group medicinal action"
Subfamily Plumeroideae
Carisseae
Carissa edulis Vahl Roots Carissin Cardenolide Oncolytic (sarcoma
180)(Abbotâ/.,1966)
Hunteria eburnea Pichon Seeds Burnamine Indole alkaloids Hypotensive
Picralima nitida Stapf Seeds Akuammine, akuammiline, Indole alkaloids Hypotensive, local
akuammidine, akuammigine, anaesthetic, sym-
etc. patholytic
Tabernaemontaneae6
Tabernaemontana crassa Roots, Isovoacangine, conopharyngine, Indole alkaloids Sympathomimetic
Benth. syn. {Conopharyngia bark conodurine, conoduramine
durissima Stapf) Seeds Voacamidine, tabersonine,
coronaridine
(Table continued)
Table 2.1. (Continued)
Plant Part used Active constituent(s) Chemical group medicinal action*
Tabernaemontana pachysiphon Roots Pachysiphine Aminosteroid Hypotensive (Heg-
Stapf syn. (Conopharyngia pachy- glycoside nauer, 1962-8,
siphon Stapf) Voacangine Indole alkaloid vol. 3, p. 129)
Hedranthera barteri (Hook.) Roots, Callichine, vobtusine Indole alkaloids Cardiotonic (Patel and
Pichon. syn. (Callichilia barteri Stapf, stems Rowson, 1964)
C. monopodiales (S chum.) Roots, Callichine Indole alkaloids Cardiotoxic (Patel and
Stapf) stems Rowson, 1964)
Leaves ? Ursolic acid Triterpene Cardiotonic
Voacanga africana Stapf Stembark Voacamine, voacangine, Indole alkaloids Cardiotonic, sympa-
and rootbark voacristine, voacorine, tholytic, hypotensive
voacamidine, vobasine, vobtusine,
etc.
Voacanga bracteata Stapf Stembark Indole alkaloids Same as V. africana
Voacamine, voacangine,
and rootbark voacorine, epivoacorine
Alstonieae
Alstonia boonei de Wild. syn. Bark Echitamine, echitamidine, Indole alkaloids Hypotensive?
(A. congensisChev. & Aubrev.) c. alstonine, reserpine (Raymond-Hamet,
Leaves Amyrin, lupeol, ursolic acid Triterpenes 1934,1941)
Catharanthus roseus (L.) Don. syn. Roots, Catharanthine, lochnerine, Indole alkaloids Hypoglycaemic
(Lochnera rosea Reichb.) c. twigs vindoline
Vincristine, vinblastine Indole alkaloids Oncolytic (Hodgkin's
disease, leukaemia)
Reserpine, ajmalicine Indole alkaloids Hypotensive, tranquil-
lizer
Holarrhenafloribunda (Don.) Stembark Conessine, conkurchine Steroid alkaloids Antibiotic (Entamoe-
Dur. & Schinz. syn. (H. africana, and rootbark biahistolytica, Tricho-
H. wulfsbergii) monas)
Bark Holarrhenine Steroid alkaloids Hypotensive, local
Leaves Holarrhimine, holaphyllamine, anaesthetic, spasmo-
holaphylline lytic
Allamanda cathartica L. c* Seeds, stems, Plumeriede = plumeroside, Glycoside of Cardio tonic,
roots allamandin iridoid lactone antitumour agent,
cardiotoxic
Leaves Ursolic acid
Plumeriarubrac. Latex, leaves Plumiericacid, Glycoside of Local anaesthetic,
and bark plumieride cinnamic acid cardiotonic
Bark Fulvoplumierin lactone Bacteriostatic
Rauvolfieae
Rauvolfia vomitoria Afzel. Rootbark and Reserpine, rescinnamine, Indole alkaloids Tranquillizer
stembark raumitorine Sedative
Hypotensive
Reserpiline, rauvanine Indole alkaloids Hypotensive
Ajmaline, rauvanine Anti-arrhythmic
Ajmalicine Raynaud's disease
vasodilating
Funtumia africana (Benth.) Stapf Bark, leaves Funtumine Steroid alkaloid Hemisynthesis of
corticosteroids
Pleioceras barteriBaill. syn. Rootbark, Alkaloids ? Steroid alkaloid Local use, emmena-
(Wrightia parviflora Stapf.) seeds gogue, abortifacient
Leaves Ursolic acid Triterpene Produces sodium re-
tention like desoxy-
corticosterone (Ker-
haro and Adam, 1974,
p.157)
(Table continued) ^
Plant Part used Active constituent(s) Chemical group medicinal action0
Malouetia heudelotii DC. Bark Malouetine Steroid alkaloid Curare action (Heg-
nauer,vol. 3, p. 129)
Subfamily Echitoideae
Adenium obesum (Forsk.) Latex Honghelosides A-G Cardenolides Cardiotonic (toxic)
Roem. & Schult. syn. (Adenium
honghelDC.)c.
Baissea leonensis Benth. Leaves Baisseoside = esculetol-6- Coumarin Vitamin P action
rutinoside glycoside
Nerium oleander L. c. Leaves Oleandrin, digitalin, adynerin, Cardenolides Cardiotonic
neriantin
Strophanthus gratus Franch. Seeds Strophanthins K, g, etc. Cardenolides Cardiotonic
Strophanthus hispidus DC. Seeds
Strophanthus gracilis Schum. Seeds
Strophanthus sarmentosus DC. Seeds Heterosides Steroid Hemisynthesis of
heterosides corticosteroids and
oral contraceptives
Strophanthus spp. Leaves Quercetol- and kaempferol-
heterosides
Subfamily Cerberoideae
Thevetia neriifolia Juss. ex Steud. syn. Roots, bark Thevetins A and B, peruvoside Cardenolides Cardiotonic
(T. peruviana) c. Leaves, seeds Aucubine Iridoid Insecticide
heteroside
References are indicated only when they are not mentioned in the text.
b
A number of Conopharyngia and Tabemaemontana species also contain voacangine and vobtusine. However, the principal use of those species is
based on their content of alkaloids of the ibogaine group, which act on the nervous system, and the plants will therefore be described with those
acting on the nervous system. Likewise Allamanda will be described with antitumour agents.
15
The plants containing the cardiotonics can be divided into two groups:
(A) Plants containing cardio tonic steroid heterosides. This group includes
plants belonging to the Apocynaceae, those belonging to the Asclepia-
daceae and Periplocaceae, and those belonging to other botanical families.
(B) Plants containing cardiotonic alkaloids.
Group A: Plants containing cardiotonic steroid heterosides
APOCYNACEAE. AS we see from Table 2.1, which lists the main medicinal
Apocynaceae in tropical West Africa, the family includes a number of plants
containing cardenolides. We also find amongst the West African Apocynaceae a few
of the more important cardiotonics, which appear next to the non-African Digitalis
in most Pharmacopoeias. I start by mentioning the better-known ones.
Strophanthus gratus (Hook.) Franch. APOCYNACEAE

The seeds and wood, like those of all Strophanthus species, were used in arrow1 and
fish poisons (Dalziel, 1937).
The seeds yield 3-7% of g-strophanthin or ouabain, first isolated in crystallized form
in 1877 (Paris and Moyse, 1971, vol. 3). On hydrolysis, rhamnose and ouabagenin
are obtained (Euw and Reichstein, 1950a, b). The seeds also contain several minor
alkaloids such as acolongo floroside K and strogoside (0.4%) (Geiger et aL, 1967).
Ouabain is used in preference to digitalis when a more rapid action is required. The
effect is more potent but is of shorter duration and non-cumulative (Martindale,
1958, p. 580). As it is badly absorbed when given orally, it is mostly administered
intravenously or intramuscularly. It does not cause peripheral vasoconstriction as
does digitalis. In toxic doses ouabain produces hypertension, tachycardia, auricular
and ventricular dissociation and, finally, cardiac arrest, in the dog.
Strophanthus hispidus DC. APOCYNACEAE

The seeds of this species yield 4—8% of amorphous strophanthoside H which,
although less important than g- or K-strophanthin, is also used for cardiac
insufficiencies. The seeds were also found to contain 1.47% of K-strophanthoside-a,
found originally in S. kombe (which contains 5-10% of active cardenolides). In
addition, sarmentocymaroside, saponosides and flavonosides have been reported to
be present in the seeds (Euw and Reichstein, 1950a; Keller and Tamm, 1959).
The use of the seeds of S. hispidus, official in the 1949 French Codex, is limited to
strophanthus tincture (1/10), whilst S. gratus is used for the extraction of ouabain for
intravenous injections (doses 0.12-0.25 mg).
Strophanthus gracilis Schum. & Pax APOCYNACEAE

The seeds of this species, which is also indigenous, contain the largest quantities of
total glycosides, including strophanthidin, strophanthidol, emicymarin, odoriside
H and G and graciloside. However, S. gracilis is not used in pharmacy, having less
active constituents than S. gratus and 5 . kombe.
16
Strophanthus sarmentosus DC. (Fig. 2.1) APOCYNACEAE

The heterosides of this species are of two different types according to the geographi-
cal origin of the plants. In those found in southern Nigeria, Congo and Togo the
genin is sarvogenin, whilst in those of the savannah areas of northern Nigeria and
Mali, it is sarmentogenin. The sugars are in both cases sarmentose and digitalose
(Fechtig etal., 1960; Fuhrer etal, 1969).
The heterosides, which are of no therapeutic interest, were examined with those of
other related species as a source of steroids to be used in the hemisynthesis of
corticosteroids and sex hormones, but the results were disappointing (Wall et al.,
1961; Reichstein, 1963).
Fig. 2.1. Strophanthus sarmentosus D C .

17
Thevetia neriifolia Juss. syn. (7\ peruviana Pers., C ethera thevetia L., C. peruviana
Pers. APOCYNACEAE
Yellow oleander
Largely cultivated as an ornamental plant. The bark is bitter and said in Ghana and
southern Nigeria to be a powerful antipyretic for intermittent fevers, but it is also an
emetic and poisonous in excess (Oliver, 1960).
The roots, stems and kernels (the latter also yield up to 57% of a yellow oil) contain
1-5% of a bitter heteroside, thevetin or thevetoside (a mixture of thevetin A and B),
and peruvoside. On hydrolysis, thevetin A yields cannogenin, gentiobiose and
thevetose; thevetin B, also called cerberoside, yields gentiobiose and neriifolin,
which on further hydrolysis yields one molecule of thevetose and the aglycone
digitoxigenin. Acetylneriifolin has also been isolated from the seeds (Frerejacque,
1947; Bloch etal., 1960; Bisset, 1961; Bisset etal., 1962; Frerejacque and Durgeat,
1971).
Thevetin has a short digitalis-like action on the heart and has the advantage of rapid
elimination. Peruvoside and neriifolin are more active (action about equal to that of
ouabain) and are more rapidly eliminated, but there is little difference between
effective and toxic doses. The LD 5 0 in the cat is 147 /xg/kg for peruvoside as against
1106 fig/kg for thevetin B (Kohli and Vohra, 1960; Chen and Henderson, 1962;
Datta and Datta, 1977).
Thevetin is used to a limited extent clinically in cases of intolerance to digitalis and
where oedema persists after digitalis therapy. It is recommended by Russian authors
for cardiac insufficiency with dyspnoea and for ventricular insufficiency due to
hypertension and atherosclerosis (dose 0.5-2 mg daily, orally or intravenously); it is
effective 4-6 h after oral administration (Ambrosia and Mangieri, 1955; Aleshkina
and Berezhinskaja, 1962; Arora etal., 1967).
An extract of the leaves and fruits of the plant yielded aucubine, an iridoid
heteroside. The extract has been found to give excellent results in killing larvae and
insects (Heal and Rogers, 1950; Paris and Etchepare, 1966).
Nerium oleander L. APOCYNACEAE

Ornamental shrub often grown all over West Africa.
The leaves of this species contain several heterosides; the most important of them,
representing up to 90% of the total heterosides, is oleandrin or oleandroside. On
hydrolysis oleandrin produces a sugar, oleandrose, and oleandrogenin, which is
identical with 16-acetyl-gitoxigenin (Abisch and Reichstein 1960, 1962a).
The plant is used for the extraction of oleandrin, which is an orally active cardiotonic
and diuretic and is listed as such in the Russian Pharmacopoeia. It can be given to
elderly patients with cardiac deficiencies who cannot tolerate digitalis or ouabain.
The dosage is similar to that of digitoxin with a maximum dose of 0.2 mg/day (tablets
of 0.1 mg = 3-4 frog doses). It also regularizes cardiac flutter and fibrillation.
Oleandrin is rapidly eliminated, producing a stronger diuresis than digitalin, and
is only weakly cumulative. The leaves also contain flavonoids (rutoside and
3-rhamnoglucoside of kaempferol), which contribute to the diuretic action. A
18 19
Table 2.2. Asclepiadaceae and Periplocaceae (formerly part of the Asclepiadaceae) in tropical West Africa
Plant Part used Active constituent(s) Chemical group medicinal action
PERIPLOCACEAE
Cryptolepis sanguinolenta Root Cryptolepin Indole alkaloid Hypotensive, anti-
(Lindl.)Schltr. In related C. apiculata, Cardenolide microbial
cryptoleposide
Cryptostegia grandiflora (Roxb.) Leaves Cryptograndosides A, B, etc. Cardiotoxic Cardiotoxic, oncolytic
R.Br. c. heterosides
Parquetina nigrescens (Afzel.) Bark, roots Periplocoside, periplocymarin = Cardiac glyco- Cardio tonic,
Bullock syn. (Periploca nigrescens leaves nigrescigenin, etc. sides of digitalis diuretic
Afzel., Omphalogonus nigritans group
N.E.Br.) Cymarin, strophanthidin Cytotoxic
ASCLEPIADACEAE
Subfamily Secamonoideae"
Asclepiadeae
Asclepias curassavica L. c. Roots Curassavicin, calotroposide Cardenolides Cardiotonic?
Leaves Polyphenols* Cytotoxic
Pachycarpus lineolatus (Decne.) Roots Asclepiadin, calotroposide, Cardenolides Ipeca substitute
Bullock syn. (Asclepias lineolata uzarigenin, corotoxigenin (India) cytotoxic
(Decne.) Schltr.)
Calotropis procera (Ait.) Ait. Latex, Calotroposide, uscharin, Cardenolides Cardiotonic,
bark calotropin, calotoxin, etc. cytotoxic
Calotropain Proteolytic Anthelmintic
enzyme
Pergularia daemia (Forsk.) Chiov. syn. Plant Pergularin (related to tomento- Steroid glycosides Spasmolytic,
(Asclepias daemia Forsk., genin); saponification to two pituitrin-like action
Pergularia external. E. Br.) stigmasterols on uterus
Stems, Uzarigenin, calactin, calotropin, Cardenolides Cardiotonic
seeds coroglaucigenin, etc.
(in Indian plants)
Xysmalobium heudelotianum Roots Uzarosides, genin = Steroid glycosides Dysmenorrhoea,
Decne. transdigitoxigenin, xysmalogenin, (pregnane deriva- antispasmodic
coroglaucigenin, etc. tives)
Sarcostemma viminale R.Br. Stems, Friedelin, derivatives of Pregnane glyco- Increase lactation
plant viminolon, metaplexin, sarcostin sides (Watt and Breyer-
(Schaub et al., 1968; Stockel etal., Brandwijk, 1962)
1969)
Marsdenieae
Gymnema sylvestre R.Br. Leaves Gymnemic acid = 9 glycosides of Glycosides* Reduces glycosuria
related constitution diabetes (US Disp.
1926)
GongronemalatifoliumBenth. syn. Stems In related spp. condurangoside Glycosides* Vermifuge
(Marsdenia latifolia (Benth.) Schum.) (cyramose + thevetose + glucose
+ aglycones derived from fluorene)
Leptadenia hastata (Pers.) Decne. syn. Leaves Glycosides related to condurangine Glycosides* Diuretic, expectorant,
(Cynanchum hastatum Pers.) In related Cyn. vincetoxicum, Alkaloid emetic (in French
tylophorine Codex, 1908)
"The subfamily Secamonoideae has been divided into four tribes: the Secamoeae, the Asclepiadeae and Marsdenieae (represented here) and the
Ceropegieae.
*A number of Asclepiadaceae contain condurangin and vincetoxin glycosides (Asclepias curassavica, Sarcostemma viminale, Gymnema sylvestre,
Marsdenia conduranga, Cynanchum vincetoxicum (Vincetoxicum officinale) etc.). In A. curassavica both cardenolides and the above-mentioned
glycoside esters are present: this is probably also the case in Sarcostemma australe R.Br.
20
cytostatic effect of the leafy stems on adenocarcinoma 755 has been reported
(Fauconnet and Pouly, 1962; Dykman et al., 1966; Paris and Moyse, 1971, pp. 54
and 55).
Adenium obesum (Forsk.) Roem. & Schult. syn. (A. honghel D C , Nerium obesum
Forsk.) (Fig. 2.2) APOCYNACEAE
The leaves and stem exude a latex which is used in Adamawa in northern Nigeria as
a fish poison and which was formerly used to poison arrows. In local medicine the
latex is applied to chronic wounds and ulcers or to carious teeth.
Seven heterosides, honghelosides A-G, were isolated from the stems and roots by
Hunger and Reichstein (1950) and by Hess and Hunger (1953). Hongheloside B is
identical with digitalinum verum from Digitalis purpurea. Hydrolysis of hon-
gheloside A yields cymarose and oleandrogenin. Hongheloside G is identical with
somalin (found in A. somalense in East Africa) (Hess and Hunger, 1953).
The plant acts as a cardiac poison in the same way as digitalin, but it also has an effect
on the central nervous system (CNS), on the nerve mechanism of the heart and even
Fig. 2.2. Adenium obesum (Forsk.) Roem. & Schult.

21
on the heart muscle (Perrot and Leprince, 1909). It does not appear to have been
used pharmaceutically.
ASCLEPIADACEAE AND PERIPLOCACEAE. Cardenolides and allocardenolides (in the

latter the A-B ring fusion is trans instead of cis, which considerably decreases the
cardiotonic efficacy) are also found in a number of Asclepiadaceae and Periplocaceae
(Table 2.2). They were formerly used as arrow poisons (Oliver-Bever, 1968).
Parquetina nigrescens (Afzel.) Bullock syn. (Periploca nigrescens Afzel.,

P. calophylla (Baill.) Roberty, Omphalogonus nigritanus N.E.Br.)
PERIPLOCACEAE
The whole plant is used to stupefy fish, and the leaves and latex are used in Ghana
and Liberia for the treatment of rickets, diarrhoea and skin lesions (Githens, 1949;
Oliver, 1960).
Reichstein and co-workers isolated in 1954 a series of digitalis heterosides from the
fresh wood of this species and identified several aglycones including strophanthidin,
strophanthidol and nigrescigenin. Later they also isolated, inter alia, 6-dehydroxy-
strophanthidin, strophanthigenin and convallotoxin (Mauli and Tamm, 1957; Patel
and Rowson, 1964; Berthold etal., 1965).
Calocin, a pregnane glycoside has been reported in this species by Sravasta et al.
(1982).
The barks of the related Periploca graeca and of P. aphylla (not found in West
Africa) yield the glycosides periplocin and periplocymarin of the digitalin group
(Paris and Moyse, 1971, p. 97).
In the USSR periplocin and periplocymarin are used as cardiotonics and diuretics
and are said to be better suited for slow intravenous injection than strophanthin (in
the Russian Pharmacopoeia the active dose is stated as 0.02-0.05 mg) (see also
Martindale, 1969).
Cryptostegia grandiflora (Roxb.) R.Br. ex. Lindley (Fig. 2.3) PERIPLOCACEAE

The latex of this widely cultivated ornamental shrub has been used as a source of
rubber, and has been considered to be oncolytic (Chopra et al., 1956; Paris and
Moyse, 1971).
In earlier investigations leaves and stems were found to contain two cardenolides,
cryptograndoside A and B, which are glycosides of oleandrogenin with sarmentose
and glucose, respectively, and thus are similar to hongheloside A (Aebi and
Reichstein, 1950; Mcllroy, 1950; Abisch and Reichstein, 1962b). In 1972 five
cardenolides were isolated and identified as oleandrogenin, gitoxigenin, rhodexin B,
16-propionylgitoxigenin and a new natural product, 16-anhydrotoxigenin (Dos-
kotch etal., 1972).
An alcoholic extract of the above-ground portion of the plant had been found to have
an inhibitory action against the cell culture (KB) of human carcinoma of the
nasopharynx (Abbot et al., 1966). In a further study at the Cancer Chemotherapy
National Service Centre (CCNSC), systematic fractionation showed that mainly
oleandrogenin, gitoxigenin and rhodexin B were significantly active (Abbot et al.,
22
Fig. 2.3. Cryptostegia grandiflora (Roxb.) R. Br. ex. Lindley.
(a) Flower
(ft) Fruit
23
1967). A parallel appears to exist between cytotoxicity towards KB cells, a heart

action and inhibition of the ATPase-mediated active transport of K + and Na +
(Kupchan etal., 1967; Doskotch et al., 1972).
Asclepias curassavica L. ASCLEPIADACEAE

Swallow wort, wild ipecacuanha
The roots of this West Indian species, widely cultivated in West Africa as an
ornamental shrub, are used in the West Indies and in India, in decoction or
pulverised, as an expectorant and emetic. They have similar effects to Ipecacuanha
roots but are more strongly purgative. The roots of an indigenous related species,
Pachycarpus lineolatus (Decne.) Bullock syn. (A. lineolata (Decne.) Schltr.), are
Fig. 2.4. Calotropisprocera (Ait.) Ait.

24
given in northern Nigeria in decoction with native soda for intestinal troubles. In
East Africa the roots are used to stimulate digestion (Dalziel, 1937).
The roots of both Asclepias spp. contain cardenolides of which the most important
aglycones are uzarigenin, corotoxigenin, and coroglaucigenin, but asclepogenin,
curassavogenin and ascurogenin have also been reported as well as the cardenolides
asclepin (in the Indian plants) and calotroposide which are both also found in
Calotropis (Tschesche et al., 1958; Patel and Rowson, 1964; Singh and Rastogi,
1969; Patnaik and Dhawan, 1971; Hocking, 1976). The leaves contain polyphenols
(quercetin and kaempferol) (Bate-Smith, 1962).
The alcoholic extract of the plant and asclepin have a digitoxin-like cardiotonic
action and the total extract is used as a diuretic, expectorant and emetic (Paris and
Moyse, 1971, p. 98).
Calotroposide shows an inhibiting action on malignant tumors (Kupchan et al.,
1964; Bezanger-Beauquesne and Pinkas, 1971).
Calotropis procera (Ait.) Ait. (Fig. 2.4) ASCLEPIADACEAE

Mudar, apple of Sodom, swallow wort
Local healers use the acid latex of this plant as a rubefacient and to extract guinea
worms (Dracunculns medinensis). Others use the dried rbotbark in soup to treat colic
and as a stomachic, and the burnt root is made up as an ointment for skin eruptions,
foul ulcers, etc. (Dalziel, 1937).
The very toxic latex contains a cardiac heteroside, calotroposide, with an aglycone
identical to ouabain, and seven other heteroside alkaloids; calotropin, calactin,
calotoxin, uscharin, uscharidin, voruscharin and proceroside. Apart from calactin
and proceroside these all have the same genin (calotropa H genin) (Hesse and
Ludwig, 1960;Croutefa/., 1963,1964). Besides the heterosides the latex is reported
to contain amyrin, traces of glutathione and a proteolytic enzyme, 'calotropain'.
The aqueous and alcoholic extracts of the roots initially produce a slight depression,
followed by a stimulation, of the rate and force of myocardial contractions in isolated
frog and rabbit hearts (0.2 ml/kg). They also produce marked vasoconstriction in
frog and rat and a persistent rise in blood pressure in the dog, which cannot be altered
by any sympathetic drug (Derasari and Shah, 1965; Indian Council of Medical
Research, 1976). In the cat the cardiotonic actions of calotroposide, calotoxoside and
uscharin are 83%, 76% and 58%, respectively, of the action of ouabain (Chen et al.,
1942). The cardioactive effect was confirmed by Patel and Rowson (1964).
The enzyme calotropain is said to be more active than papain, bromelin or ficin
(Atal and Sethi, 1962); it also has an anthelmintic action (Garg et aL, 1963).
Pergularia daemia (Forsk.) Chiov. syn. (P. extensa N.E.Br., Daemia extensa R.Br.,
Asclepias daemia Forsk.) ASCLEPIADACEAE
Locally, anthelmintic properties are attributed to the leaves of the plant. The latex
or a poultice of the leaves is also applied to boils and abscesses, and the plant is said
to have emmenagogic action. In Ghana a soup made with the leaves is given to
women immediately after childbirth (Dalziel, 1937).
The stems of the plant contain uzarigenin, coroglaucigenin and calactin (India),
25
whilst in the seeds calactin, calotropin and eight further cardenolides are found. The
plant also contains a bitter resin called pergularin, which is structurally near to
tomentogenin from Marsdenia tomentosa (Mittal et al., 1962). Patel and Rowson
(1964) established that in the Nigerian species only the seeds have cardiotonic action;
the leaves, roots and stems do not (Rowson, 1965; Paris and Moyse, 1971).
The plant has a physiological action on the uterus similar to that of pituitrin but
mainly limited to the upper part of the uterus and its use as a pituitrin substitute in
delivery has been suggested (Dutta and Gosh, 1947). This action is not inhibited by
progesterone. A general stimulating effect on involuntary muscles and an increase of
the arterial blood pressure has also been observed (Gupta etal., 1950; Unesco, 1960).
Xysmalobium heudelotianum Decne. ASCLEPIADACEAE

The tuber of this plant is used as a bitter tonic and is eaten by the Hausas (Northern
Nigeria) as a remedy for stomach troubles (Dalziel, 1937).
The tubers contain, like those of the East African X. undulatum R.Br., uzarosides
(uzarin is a monoglycoside of uzarigenin, an isomer of digitoxigenin) and glycosides
of xysmalogenin and of 17a-uzarigenin (Kuritzkes et al., 1963; Paris and Moyse,
1971, p. 97).
Glucosides of pregnane derivatives were reported in the roots of X. undulatum (L.)
Ait. by Tschesche and Snatzke in 1960 (Paris and Moyse, 1971, p. 96).
The uzarosides of X. heudelotianum have a weak cardiotonic action. They are mainly
used as antispasmodics and antidiarrhoeal agents and in dysmenorrhoea (Paris and
Moyse, 1971, p. 97).
PLANTS BELONGING TO OTHER BOTANICAL FAMILIES. Cardenolides related to those

found in the above-mentioned Apocynaceae and Asclepiadaceae are also occasionally
found in members of other botanic families.
Corchorus olitorius L. TILIACEAE

The bark provides a fibre (jute) and the mucilagenous leaves are used in food and as
a vegetable. In indigenous medicine in India the seeds are used as a purgative and the
leaves as a tonic and diuretic (Chopra et al., 1956; Oliver, 1960).
From the seeds, 11-15% of a fixed oil and several steroid heterosides could be
isolated (Chakrabasti and Senn, 1954). The corresponding aglycones, at first named
corchorin, corchorogenin, corchsularin and olitorigenin, were later identified as
strophanthidin (Senn et al., 1957). The main heterosides are corchoroside,
olitoroside and helveticoside. The latter can be hydrolysed to give one molecule of
strophanthidin and one molecule of D-digitoxose. Olitoroside is strophanthidin-/3-
D-boivinopyranoside-3/3-D-glucopyranoside (Chakrabasti and Senn, 1954; Senn et
al., 1957; Schmersal, 1969).
Strophanthidin has an action comparable to that of ouabain. The corresponding
corchorosides A and B were found to contain lethal doses of 0.0768 and 0.1413 mg/
kg, respectively, which thus makes corchoroside A one of the most potent heart
poisons (Frerejacque and Durgeat, 1954). Pharmacological and clinical trials have
been carried out by Russian research workers. In pharmacological tests on rabbits
26
with experimental myocarditis and myocardiosclerosis, and in dogs with acute

coronary insufficiency a therapeutic effect was obtained with doses of 0.05 units/kg
(one cat unit = 14 /xg/kg) (Kiteava, 1966).
In clinical trials favourable results have been obtained in cases of chronic cardiac
insufficiency both with the corchorosides and with olitoroside by several Soviet
authors. The clinical condition and electrocardiogram of the patients were improved
(increase in amplitude of T-wave) (Turova, 1962; Umarova et al., 1968).
Urginea indica (Roxb.) Kunth. syn. (Scilla indica Roxb.) LILIACEAE

In South Africa U. altissima is known to be fatal to stock (Watt and Breyer-
Brandwijk, 1962) and this probably also applies to U. indica. In northern Nigeria the
scorched and dried bulbs are included in a liniment for rheumatic knees and
sometimes the crushed bulbs are applied to bruises and aches (Dalziel, 1937).
From the bulbs of these species and from the Mediterranean U. maritima Bak. a
crystalline glycoside, scillaren A, and a mixture of amorphous glycosides, scillaren
B, have been extracted (Chopra et al., 1938, p. 251). The genin of scillaren A is
scillaridin. The glycosides are chemically related to the digitalis and strophanthus
glycosides. They are steroid heterosides of the bufanolid type (with a hexagonal
lactonic cycle) (Seshadri and Subramanian, 1950).
The bulbs are official in the British Pharmaceutical Codex (1949) and US National
Formulary. Scillaren, unlike digitalis, does not accumulate, but is bound more to the
myocardium than is strophanthin. Scillaren A acts quickly but is rapidly hydrolyzed
in the blood. Squill is mainly a diuretic which acts by increasing the renal circulation,
but excessive doses may cause irritation and obstruction of the kidneys. Average
doses in heart insufficiency are 6 mg/24 h with maintenance doses of 2 mg/24 h (Paris
and Moyse, 1967, p. 50). The glycosides have the advantage of being useful in the
treatment of conditions refractory to, or no longer responsive to, digitalis and
strophanthus therapy (Darwish, 1980).
Urginea extracts have also been found to have antiprotozoal, hypoglycaemic
(Bapat et al.91970) and oncolytic actions (Dhar et aL, 1968).
Mansonia altissima (Chev.) Chev. var. altissima STERCULIACEAE

The bark of this tree has been used in the Ivory Coast as an arrow poison and in West
African local medicine for the treatment of leprosy and as an aphrodisiac (Oliver,
1960).
It contains mansonin which is a 2,3-di-(O-methyl)-6-deoxy-/3-D-glucopyranoside of
strophanthidin. Strophothevoside is the corresponding 3-O-methyl-6-deoxy-/3-
glucopyranoside. Besides mansonin, minute quantities of as many as 30 other
cardenolides have been traced in the seeds by paper chromatography. They are all
derived from three genins: strophanthidin, nigrescigenin and an undetermined
genin (Algeier et aL, 1967).
An amorphous fraction of mansonin was found to have a cardiotonic activity
comparable to that of strophanthin G. Unfortunately, the yield of active substance
is small and variable (Terrioux, 1952).
27
Antiaris africana Engl. syn. (A. kerstingii Engl., A. toxicaria (Rumph. ex Pers.)
Lesch. var. africana) MORACEAE
Bark cloth tree
The tree is called 'bark cloth tree' as in Ashanti (Ghana) a strong white cloth is made
from the bark. In the Ivory Coast the bark has been used as a purgative and in the
treatment of leprosy (Dalziel, 1937).
Seven heterosides of the digitalis type are reported in the latex including a- and
)3-antiarin. On hydrolysis they produce antiarigenin and antiarose, and antiarigenin
and L-rhamnose respectively. The seeds contain everiomoside, antioside and several
other glycosides and aglycones (Bisset, 1962; Wehrli et al., 1962; Miihlrad et al.,
1965).
The West African Antiaris appears to be less toxic than the Asiatic A toxicaria (Pers.)
Lesch. The dried latex of the Asian species (water-soluble extract) is a violent heart
poison, causing fibrillation and a drastic fall in the blood pressure. In smaller doses
it appears to be a stimulant for the heart and circulation (Chopra et al., 1938; Patel
and Rowson, 1964).
Schwenkia americana L. syn. (S. hirta Wright, 5 . guineensis Schum. & Thonn.)
SOLANACEAE
The root of this solanaceous shrub is a common remedy for rheumatic pains and
swellings in northern Nigeria; in Ghana it is used as a cough medicine and in Angola
for chest complaints (Dalziel, 1937).
According to Rabate (1940), the leaves, roots and stems of the plant contain a
glycoside, schwenkioside, which has a phenolic aglycone, schwenkiol, and also
traces of alkaloids. However, Patel and Rowson (1964) could not identify schwen-
kioside but found a steroid sapogenin to be the main constituent of this herb in
Nigeria.
This sapogenin seems to behave physiologically as a cardiac glycoside. On a toad's
heart it has been found to cause, after initial inhibition, a prolonged stimulation. All
parts of the plant produce haemolysis of the red blood cells, probably due to the
saponin (Patel and Rowson, 1964).
Paullinia pinnata L. SAPINDACEAE

In West Africa, the juice of the leaves and seedpods is known for its haemostatic
action and is used as an infusion in dysentery and fever, as a tonic and in acute
infectious disease. The root and seeds are said to be highly toxic (Dalziel, 1937).
P. pinnata collected in West Africa is found to contain no alkaloids but a saponin
with a triterpenic aglycone (Kerharo and Adam, 1974). It contains quebrachitol in
both the leaves and bark in Madagascar (Plouvier, 1948) and Bowden (1962)
extracted a flavotannin from the leaves of the West African plant.
The flavotannin has a cardiotonic effect on the isolated frog's heart (Bowden, 1962)
and on the heart of mammals (Broadbent, 1962). When calcium is absent from the
perfusion liquid the tannin has no cardiotonic action. The tannin is shown to be
antagonistic to ouabain, probably by preventing the fixation of ouabain on the heart
28
surface and is said to act in forming a calcium-tannin complex on the surface of the
heart tissues. The action of the flavotannin on the mammalian heart is to increase the
strength of the diastole and the coronary flux (Broadbent, 1962). The saponin was
shown to be toxic to Paramecia, which were killed in 1 h by a concentration of 1:500
(Kerharo et al., 1960-2) (see Chapter 4).
Vernonia colorata (Willd.) Drake syn. (Eupatorium coloratumWiWd., V. senegalensis

Less.) COMPOSITAE
Bitter leaf
A decoction of the leaves is used in local medicine as an antipyretic, expectorant and
laxative. The bark of roots and stems is astringent, and is used against fever and
diarrhoea. The root without the bark is taken as a tonic (Oliver, 1960).
A bitter glycoside, vernonin, was first isolated from the roots by Heckel and
Schlagdenhaufen (1888) and was also detected in the roots of V. nigritiana Oliv. &
Hiern. V. amygdalina Del. and V. cinerea (L.) Less., and a 'bitter principle' was
reported in V. conferta Benth. and V. guineensis Benth. All these species have
similar local uses. Later Patel and Rowson (1964) found a cardiac glycoside in the
leaves, stems and roots of V. colorata and V. nigritiana collected in Nigeria. In
addition, Toubiana (1969) has isolated two sesquiterpenic lactones (with cytotoxic
action in vitro) from V. colorata, and from V. guineensis vernodalin and vernolepin,
which have activity against Wilme's myeloma and KB tumours, respectively
(Toubiana, 1975).
When injected intravenously in dogs vernonin produces hypotension and has an
action on the heart comparable to that of digitalin, but is much less toxic. The cardiac
glycosides isolated by Patel and Rowson (1964) similarly have a distinct cardiotonic
action but no cardiotoxic action. Jawalekar reports (in Caiment-Leblond, 1957) that
a leaf extract of V. amygdalina reduces the rate and force of contraction of the isolated
frog heart. In cats it causes a marked fall in the blood pressure, reduces the heart rate
and blocks the transmission of heart contractions. Further, it strongly stimulates
contractions of the isolated rabbit intestine. These effects can be blocked by atropine
(Kerharo and Bouquet, 1950; Caiment-Leblond, 1957). The LD 50 in mice for V.
colorata is 10 g/kg. The leaves of V. cinerea have a slight antibiotic action (Kerharo,
1968).
Group B: Plants containing cardiotonic alkaloids
Erythrophleum guineense G. Don CAESALPINIACEAE

Ordeal tree, sasswood, red water tree, sassy bark
The bark has been used in arrow poisons; its toxic aqueous decoction or cold infusion
is called 'red water' and was used in fetish trials and ordeals.2 Rigal (1941) observed
that in guinea pigs death occurred 3 h after a dose of 0.5 g/kg was administered and
55 min after a dose of 1 g/kg. The seeds were found to be more toxic than the bark in
spite of a lower alkaloid content. Probably this is due to the simultaneous presence
of a strongly haemolytic saponin (Rigal, 1941). In local medicine the bark is
sometimes used as a diuretic, emetic and sternutatory.
29
Bark and seeds contain 0.1-0.5% of total alkaloids, mainly erythrophleine (Paris and
Rigal, 1940, 1941), also cassaine, cassaidine, norcassaidine, coumingine and
erythrophleguine (Dalma, 1939; Lindwall et al., 1965). Apart from the alkaloids, a
catechuic tannin, a saponin and a flavonoside (luteolin glycoside) have been isolated
from the bark, as well as a wax with a high proportion of hexacosanol. Erythro-
phleum ivorense Chev. syn. (E. micranthum Harms.) is less toxic than E. guineense
probably because of a higher tannin and a lower alkaloid content (up to 0.3%).
The cardioactive properties of the alkaloids can be destroyed by saponification
and can be changed by chemical modifications. Thus, modification on C-3 of
cassenic acid produces a stronger and longer-lasting action (Hauth, 1971).
Erythrophleine has a digitalis-like action, whilst the action of coumingine, which is
the most active of the alkaloids, is similar to that of scillaren A in the cat. Cassaine
and cassaidine are less potent than erythrophleine, which raises the blood pressure,
slows the pulse whilst increasing the force of the heartbeat and decreases respiration
(Cotten et al., 1952). Overdoses of erythrophleine produce symptoms of circulatory
depression, breathing difficulties, vomiting and, through direct action on the
medulla, convulsions. Erythrophleine is said to be of use in spasmodic asthma
(Rigal, 1941). It also has a local anaesthetic action similar to that of cocaine but more
powerful and longer lasting. However, no use has been made so far of this action,
probably because of the general toxic effect of these alkaloids (Trabucchi, 1937).
Cassaine has convulsant action (Santi and Zweifel, 1936). Derivatives of these
alkaloids are being prepared in an attempt to decrease their toxicity (Hauth, 1971).
In low concentrations cassaine and coumingine increase the translocation of K + from
the plasma to the cells (Kerharo, 1968).
A bark extract of Erythrophleum sauveolens (Guill. & Perr.) Brenam has been
shown to have a strong spasmogenic effect on smooth muscles. It also has a
chronotropic and isotropic effect on the heart and shows a potent hypotensive action
which is probably mediated through release of catecholamines (Bamgbose, 1974).
Voacanga africana Stapf syn. (V. glabra Schum., V. Schweinfurtii var. parviflora
Schum., V. magnifolia Wernham, V. talbotti Wernham, V. eketensis Wernham, V.
glaberrima Wernham, V. africana var. glabra (Schum.) Pichon) (Fig. 2.5)
APOCYNACEAE
Locally the latex is used as a rubber adulterant and is applied to carious teeth (Oliver,
1960).
Since 1955 this plant has aroused considerable interest and has been the subject of
numerous publications. From the bark of the stem and the root many alkaloids have
been isolated (4—5% total alkaloids from the stembark and 5-10% from the
rootbark). These include voacamine (the main alkaloid), voacangine, voacristine (=
voacangarine), voacorine, vobasine, voacamidine (an isomer of voacamine) and
many others. Most of these alkaloids have also been found in Voacanga thouarsi
Roem. & Schult. and some in other species of Voacanga, Tabernaemontana and even
Alstonia. In the leaves of V. africana voaphylline and vobtusine are found, and
tabersonine is found in the seeds (Blanpin et al., 1961; Puisieux et al., 1965;
Oliver-Bever, 1967).
30
Voacamine and voacangine act on the heart in a similar way to the cardiac glycosides
but their toxicity is very low in comparison with that of other alkaloids with a
cardiostimulant action such as the Erythrophleum alkaloids. A dose of 100 /uug of
voacamine sulphate has a cardiotonic action equivalent to that of a dose of 0.25 units
of digitalis standard (in isolated rabbit auricles) (Oliver-Bever, 1967). Voacamine
does not bind to the cardiac proteins and has no cumulative action, but it has a direct
myotonic effect on the cardiac fibre (Quevauviller and Blanpin, 1957a). Lethal doses
for guinea pigs (by instillation in the jugular vein) are 313 mg/kg for voacamine
sulphate and 348 mg/kg for voacangine sulphate, compared to 2.5 mg/kg for digitalin
and 0.9 mg/kg for strophanthin. In mice the LD 50 of voacangine, given intra-
venously, is 41-42 mg/kg (La Barre and Gillo, 1955; Vogel and Uebel, 1961).
Therapeutic doses (1-3 mg daily) are well tolerated, act rapidly and are quickly
Fig. 2.5. Voacanga africana Stapf.

31
eliminated without any cumulative effect. Voacamine, voacangine and voacorine

also have a hypotensive action and are simultaneously mildly parasympatholytic and
sympatholytic. Voacangine, which is also said to have analgesic and local anaesthetic
action, and vobtusine increase the hypnotic effect of barbiturates. Voacorine is also
cardiotonic through direct action on the heart muscle and on the coronary perfusion
and seems to contribute considerably to the action of the total alkaloids of Voacanga
(Quevauviller and Blanpin, 1957b). Its minimum LD 5 0 in guinea pigs (by slow
intravenous injection) is 228 mg/kg (Blanpin et al., 1961).
For the leaf alkaloid vobtusine, given intravenously, the LD 50 is 33.75 mg/kg.
Vobtusine has a depressive action on the heart and has hypotensive and sedative
properties (Quevauviller et al., 1965). Tabersonine from the seeds has a hypotensive
action which is equivalent to 25% of that of reserpine (Zetler, 1964).
(b) Cardiac depressants: anti-arrhythmic agents
Argemone mexicana L. (naturalized) (Fig. 2.6) PAPAVERACEAE

Mexican poppy, prickly pepper, prickly poppy
The plant is used in Nigeria and Senegal mainly for its diuretic, sedative, cholagogic
and cicatrizing properties (Oliver, 1960; Kerharo and Adam, 1974). The seeds have
a cannabis-like effect and in many countries the herb, juice and flowers are reputed
to be narcotic (Watt, 1967).
Fig. 2.6. Argemone mexicana L.

32
Numerous alkaloids have been reported to be present in all parts of the plant. Thus,
leaves, stems and seeds contain berberine and protopine and the roots contain
coptisine, a-allocryptopine, chelerythrine and dihydrochelerythrine. In the oil of
the seeds sanguinarine and dihydrosanguinarine are found (Chakravarti et al., 1954;
Bose et al., 1963). Argemonine was isolated from the leaves and capsules and
identified as (—)A/-methylpavine (Martell et al., 1963).
a-Allocryptopine, (which represents 0.099%) of the roots of the plant in Czecho-
slovakia, is identical to a-fagarine. It slows down the heart rate and prolongs systole
in rats and frogs. In doses of 10-20 mg/kg it also slows down the heartbeat of cats and
rabbits. The action is a direct one on the myocardium and is also antifibrillatory, and
a-allocryptopine has found clinical applications in this field. Thus it is considered
more active than quinidine in cases of arrhythmias with fibrillation and auricular
flutter (Alles, 1952; Dhar et al., 1968; Manske and Holmes, 1950-71, vol. 5,
pp. 90-91).
Protopine was isolated from the total alkaloid fraction by Bose. He reported that
it stimulated the heart, blood pressure and respiration, as well as the striated and
smooth muscles on which it appears to act specifically (Manske and Holmes,
1950-71, vol. 5, pp. 92 and 138).
The seed oil is highly toxic due to sanguinarine (when given subcutaneously, the
LD 50 for mice is 1.8 mg/100 g). Sanguinarine can produce experimental glaucomas
(Hakim, 1954).
Berberine is relatively non-toxic (when given intravenously, the LD 5 0 in cats and
dogs is 0.025 mg/100 g). In doses of 2 mg/kg, berberine has a depressant and
vasodilating action on the heart. It also depresses breathing but stimulates the
smooth muscles of different organs (intestine, uterus, bronchi). Moreover, ber-
berine has marked antibiotic properties on Mycobacterium tuberculosis, Staphylo-
coccus aureus, Escherichia coli, Eberth typhosa and Shigella dysenteriae, and it also acts
at concentrations of 1:80000, on Leishmania tropica (Lambin and Bernard, 1953).
An alcohol-water extract of the fruits deprived of the seeds proved to be an excellent
hypnotic and sedative for convulsions and spasmodic conditions (Martinez, 1959, p.
110). Antifibrillatory action has also been reported for oleandrin from Nerium
oleander, described earlier under cardiotonics (Fauconnet and Pouly, 1962).
Zanthoxylum zanthoxyloides (Lam.) Watson syn. (Fagara zanthoxyloides Lam.,

F. senegalense (DC) Chev., Z. polyganum Schum.) RUTACEAE
Prickly ash, candle wood, toothache bark
The aromatic rootbark is used in Ghana and Nigeria as a decoction, or in application,
for its alleged antiseptic and analgesic properties, for example in the treatment of
painful conditions, in childbirth, for toothache, etc., sometimes mixed with other
ingredients. The decoction is also used as a vermifuge and in Guinea the bark is used
to stupefy fish. The fixed oil contained in the rootbark causes salivation, a numbing
action on the tongue and paralysis (Pobeguin, 1912; Irvine, 1930; Dalziel, 1937;
Oliver, 1960).
An amorphous alkaloid was isolated from the roots as early as 1887 and called
33
artarine. (Later this was found to be identical with ethoxychelerythrine (Torto et al.,
1969.) In 1911 a pungent principle which produced salivation was extracted from the
rootbark (Thorns and Thumen, 1911). It was called fagaramide, and proved to be an
Af-isobutylamide of piperonylacrylic acid.
Since 1947 a number of tertiary and quaternary alkaloids have been identified in
the bark and rootbark of Z. zanthoxyhides. These are, in addition to artarine,
/3-fagarine (= skimmianine, a dimethoxydictamnine), fagaridine (= erythro-
fagarine), angoline, angolinine, chelerythrine, dihydrochelerythrine, tembetarine,
magnoflorine, Af-methylcorydine. No a-fagarine (also called aegeline (from Aegle
marmelos) = allocryptopine) was reported in West African species (Paris and
Moyse-Mignon, 1947; Calderwood and Fish, 1966; Torto et al., 1969). The rootbark
also contains fagarol (a lignan) and pseudofagarol, and in the fruits two coumarins,
xanthotoxin and bergapten, were reported by Paris and Moyse-Mignon (1947). The
leaves contain traces of alkaloids and a flavone heteroside.
a-Fagarine is mainly extracted for pharmaceutical use from the leaves of the
Argentinian Z. coco as it has proved to be a useful substitute for quinidine in
auricular fibrillation. In some cases it has been found to normalize the sinus rhythm
within 30 min and is so far the only Fagara base to be exploited in medical science.
(Aegeline was considered to be a weak vasoconstrictor and in large doses a cardiac
depressant (Paris and Moyse, 1967, p. 304).)
Xanthotoxin is ichthyotoxic in concentrations of only 0.1 p.p.m. and the pungent
fagaramide has weak local anaesthetic action (Paris and Moyse-Mignon, 1947;
Bowden and Ross, 1963).
An aqueous extract of the rootbark has further been reported to bring about a
reversal of sickling and crenation in erythrocytes (Sofowora and Isaac-Sodeye, 1971;
Murayama and Makyo, 1972). Later the antisickling compound was isolated and
identified as 2-hydroxymethylbenzoic acid. On further investigation it was found
that the greatest amounts of this acid were contained in the leaves, then in the
stembark and lastly in the roots. Also the antisickling fractions varied among six
different Nigerian Zanthoxylum spp. and also varied amongst parts of the same
species (Isaac-Sodeye et al., 1975;Rumen, 1975; Sofowora et al., 1975).
From the roots of the Ghanaian species a new crystalline alkaloid was isolated in
1972 by Messmer et al. and called fagaronine. This benzophenanthridine alkaloid
has a cytotoxic action, and is believed to be an inhibitor of RNA-directed activity in
avian nucleoblastosis and in cases of infection by Rauscher leukaemia virus and
Simian sarcoma virus, probably by preventing the elongation reaction (Messmer et
al., 1972).
Fagara leprieuri (Guill. & Perr.) Engl., Zanthoxylum gillettii (de Wild.) Watson
syn. (F. macrophylla Engl.) and Zanthoxylum rubescens (Planch, ex Hook, f.)
Watson syn. (F. rubescens (Planch, ex Hook, f.) Engl.) are used in similar ways to Z.
zanthoxyloides in local medicine. They also contain /3-fagarine (skimmianine),
fagaridine, xanthofagarine, angoline, angolidine and a few other bases but so far no
a-fagarine has been reported (Fish and Waterman, 1971, 1972).
34
Cinchona spp. (cultivated in the Cameroons and Guinea) RUBIACEAE

One of the alkaloids of the Cinchona bark is used in cardiology. It is a dextrorotary
stereoisomer of quinine, quinidine, which is used preferably as the sulphate, in the
treatment of auricular arrhythmias as it has a specific depressant effect on the
auricular muscle. It should, however, be reserved for the treatment of early
persistent fibrillation as it is cumulative in action. Overdoses may cause extrasy stole,
paroxysmal ventricular tachycardia, ventricular fibrillation, intraventricular block
and cardiac arrest (Martindale, 1969).
Rauvolfia vomitoria Afzel. syn. (R. senegambiae D C , Hylacium owariense P.

Beauv.) (Fig. 2.7) APOCYNACEAE
Ajmaline, one of the sympatholytic alkaloids of this plant (the others are discussed
below under hypotensives), is chemically and pharmacologically closely related to
quinidine. It is used in the treatment of arrhythmias as it slows down the rhythm and
decreases myocardial excitability in doses of mg/kg without influencing the blood
pressure. In clinical trials it produced a return to normal sinus rhythm in a high
percentage of patients with multiple extrasystole and sinus tachycardia, but results
Fig. 2.7. Rauvolfia vomitoria Afzel.

35
have been more uncertain for atrial fibrillation (Knipel et al., 1971; Lampertico,
1971). The maximum single dose should not exceed 50 mg and constant cardio-
graphic control is required. The action of 10 mg of ajmaline (given intravenously) is
approximately equivalent to that of 100 mg of prominamide (Puech et al., 1964).
Rauvanine (also in R. vomitoria) has an effect on the cardiovascular system similar
to that of ajmaline (antifibrillatory, coronary dilating and slowing down the
heartbeat), but it is non-sympatholytic and also has hypotensive action. It is only half
as toxic as reserpine and is not ulcer producing (Quevauviller et al.9 1963, 1971,
1972).
(c) Vascular agents

These can be divided into three groups:
(A) Hypotensive and some hypertensive plants. Some of the plants discussed in the
sections on cardiotonics and cardiac depressants (above) were shown to act on the
blood pressure. Haemodynamically the blood pressure depends on (i) the cardiac
output and (ii) the peripheral resistance in the capillaries. The sympathetic system
controls hypertension through the action of noradrenaline: stimulation of the
a-receptors of the small arteries produces vasoconstriction while stimulation of the
/3-receptors causes vasodilatation. In normal conditions the action on the a-receptors
predominates over the action on the /3-receptors and a state of semi-contraction is
maintained.
Hypotensive treatment can include a depletion of catecholamines in the post-
ganglionic fibres of the sympathetic system as well as in the CNS. This is the case e.g.
of reserpine. As an increase in blood pressure entails adaptation of glomerular
filtration and maximum reabsorption of sodium, requiring an increase in sodium
excretion, hypotensive treatment often includes administration of diuretics to
produce sodium depletion.
(B) Plants containing compounds that are capable of increasing resistance and
decreasing the permeability of capillaries and veins. These compounds are widely
distributed in fruit and green leaves and are used on a large scale in capillary and
venous insufficiencies. Their action, discovered by Szent Gyorgyi in 1936, was at
first attributed to a compound called vitamin P, or sometimes vitamin C2. This
consists of several constituents, also called biofiavonoids, which mainly belong to
three groups:
(i) the coumarin or a-benzopyrone group, which includes aesculetol and its
glycoside aesculoside;
(ii) the chromane group, including polyhydroxylated derivatives of phenyl-
chromane or flavane (catechins, anthocyanins, leucoanthocyanins;
(iii) the chromone or y-benzopyrone group, comprisingflavanone,flavanol,
flavonol and their (polyhydroxylated) derivatives like the flavone deriva-
tives quercitin (3, 3', 4', 5, 7-pentahydroxyflavone), kaempferol (3,4', 5,
7-tetrahydroxyflavone), or the flavanones eryodictyol, naringetol and
hesperetol.
These flavonoids increase the capillary resistance, have an antihistamine and
antihyaluronidase action and can protect against radiation, the leucopenic effect of
36
cytostatics and disorders due to an atherogenic diet. They have also been called
citroflavonoids as they are found in the pericarp of citrus fruits and are extracted in
large quantities from different plants (Sophora, Vaccinium leaves, Eucalyptus macror-
rhyncha) for use in pharmacy. They appear to be well tolerated, no serious
side-effects having been reported (Paris, 1971; 1977). A few of the plants reported to
heal oedemas and piles in indigenous medicine may be found to contain
bioflavonoids.
(C) Plants containing constituents which act more specifically on blood coagulation
and formation. Some plants promote coagulation and are reputed to have a
haemostatic action (group Q ) . Amongst the constituents responsible for this action
there are some naphthoquinones closely related to vitamin K. In West Africa these
are found in, for example, Lawsonia inermis and Diospyros mespiliformis. Vitamins K
and Kx (phytylnaphthoquinone) improve prothrombin formation and as a result
hasten blood coagulation. Vitamin K is very easily prepared synthetically. Other
plants are anticoagulants (group C 2 ), inhibiting prothrombin formation, an action
which could be attributed to dicoumarin in the case of dried Melilotus sativa in
Europe, which produces a haemorrhagic syndrome in cattle. Yet other plants have
an anti-anaemic action (group C 3 ).
Most of the West African plants having a haemolytic action contain saponosides.
Coumarin derivatives (calophyllide and inophyllide) are found in a plant introduced
into West Africa, Calophyllum inophyllum Guttiferae, which increases capillary
permeability and has anticoagulant properties (see Chapter 5).
Group Aj: hypotensives
Plants containing hypotensive alkaloids. Amongst these many indole and

indoline alkaloids are found. Many of them act through the ANS or through the CNS
and, as we will see, most of them are not only hypotensive but are also sympatholytic
(yohimbine, akuammidine and corynanthine), sympathomimetic (eserine and Mit-
ragyna and Hunteria alkaloids), local anaesthetic (Mitragyna alkaloids) or sedative
(reserpine).
Rauvolfia vomitoria Afzel. (for synonyms see above) APOCYNACEAE

Ghanaian and Nigerian healers use the rootbark, which in high doses is a powerful
purgative and emetic, in cases of infantile convulsions, jaundice and gastrointestinal
troubles. The latex or a decoction of the leaves is used in the treatment of parasitic
skin diseases, head lice, etc. (Dalziel, 1937).
Although a decoction of the root was used in 1936 by Shapara as a sedative in cases
of maniacal symptoms, inducing several hours of sleep (see Dalziel, 1937), it was
only in 1952 that the Rauvolfia species raised any considerable interest. This was
after the isolation of reserpine, with its sedative and hypotensive action, from the
Indian R. serpentina Benth. (Miiller et al., 1952). Since then numerous alkaloids
have been isolated from different Rauvolfia spp. and their pharmacological proper-
ties tested. From R. vomitoria rootbark, 4-8% of total alkaloids have been isolated,
37
containing up to 1.7% of reserpine (which has to be separated from accompanying

resins). The plant thus contains more reserpine than the Indian R. serpentina and is
indicated in the 1968 British Pharmaceutical Codex and the 1968 British Phar-
macopoeia as a source of reserpine. Harvesting is done by periodically cutting small
pieces of root without uprooting the tree. Many other Rauvolfia alkaloids have now
been isolated; they appear to belong to four main groups. In thefirst,the yohimbane
group, in addition to reserpine, rescinnamine, seredine and yohimbine have been
reported. In the second, the heteroyohimbane group, have been found reserpiline,
raumitorine, alstonine (also in Alstonia), rauvanine and ajmalicine. In the third, the
ajmaline group, ajmaline is the main alkaloid, and in the fourth, the oxindole group,
rauvoxine. All these alkaloids are accompanied by a number of secondary alkaloids
(Woodsonera/., 1957; Patella/., 1964; Delaveau, 1966). A complete and clear table
of the numerous Rauvolfia alkaloids can be found in Kerharo and Adam (1974,
p. 182). Mainly reserpine, rescinnamine, ajmaline, ajmalicine and reserpiline are
extracted from the rootbark for therapeutic use by pharmaceutical firms.
From the seeds 2,6-dimethoxybenzoquinone, and from the leaves two flavone
heterosides, 3-rhamnoglucoside and the 3-glucoside of kaempferol, have been
isolated (Patel et aL, 1964; Paris and Etchepare, 1967; Paris and Moyse, 1971).
Reserpine has a hypotensive action in cases of hypertension and slows down the
heartbeat. The alkaloid also has sedative and tranquillizing effects but is not
hypnotic. It acts through the CNS and is active only in the presence of the
hypothalamus and diencephalon and seems to act as an antimetabolite of serotonin
and catecholamines, decreasing considerably the serotonin content of the nerve
centres. This explains why, next to its use as a hypotensive agent in arterial
hypertension, reserpine (given orally in 0.1-0.25 mg tablets) is currently used as a
tranquillizer in anxiety states and in psychoses with hallucinations and delirium.
Although it is not very toxic, the action of reserpine is cumulative and after
prolonged administration side-effects like nasal congestion, bradycardia, oedema,
stimulation of intestinal peristalsis and even ulceration are noticed (Woodson etal.,
1957; Smith, 1963; Delaveau, 1966; Fattorusso and Ritter, 1967).
Rescinnamine and, in particular, reserpiline also have a hypotensive action.
Reserpiline, representing up to 75% of the remaining alkaloids, produces, in
contrast to reserpine, no digestive troubles or ulcers in rats, even in doses of 2 mg/kg.
It has, however, no tranquillizing or hypnotic effects (La Barre and Gillo, 1958).
Ajmalicine, which also acts through the central nervous system, is a coronary and
peripheral vasodilator and is used in angina pectoris and Raynaud's disease (Fat-
torusso and Ritter, 1967).
Raumitorine has a hypotensive action similar to that of reserpiline (La Barre and
Hans, 1958) and does not act on the digestive tract. It has, however, to a certain
extent, the tranquillizing effect of reserpine (La Barre and Demarez, 1958; La Barre
and Gillo, 1958; La Barre et al., 1958). Rauvolfia macrophylla Stapf, R. caffra
Sond. and R. mannili Stapf also contain alkaloids but are less common than
R. vomitoria in tropical West Africa. Reserpine and ajmalicine (= vincaine =
5-yohimbine) are also found in Catharanthus roseus, now mainly used for the
extraction of antileukaemia principles (Oliver-Bever, 1971).
38
Picralima nitida (Stapf) Th. & H. Dur. syn. (P. macrocarpa Chev., Tabernae
montana nitida Stapf, P. klaineana Pierre) APOCYNACEAE
L The seeds are eaten locally as a tonic and excitant and are used in the treatment of
malaria and jaundice (Irvine, 1930; Dalziel, 1937).
C They contain 3-5% of total alkaloids many of which have been identified. The main
alkaloids are akuammine, akuammidine, and akuammigine, anisomer of ajmalicine.
Some further alkaloids reported are pseudoakuammidine and akuammiline (in-
doline derivatives), akuammicine (indole derivative), etc. (Olivier et al., 1965;
Pousset et al., 1965). From the leaves picraphylline and from the roots picracine and
melinosime have been isolated (Le Double et al.9 1964).
P Akuammine, the main alkaloid, has been found to be inactive in malaria both in
pharmacological and clinical trials, but it is a powerful sympathomimetic and has a
local anaesthetic action almost equal to that of cocaine (Raymond-Hamet, 1951;
Paris and Moyse, 1971, p. 94).
Akuammidine has a sympatholytic action and a hypotensive effect which is
weaker but longer lasting than that of yohimbine. Akuammidine also has a strong
local anaesthetic action (three times that of cocaine hydrochloride) (Raymond-
Hamet, 1944).
Holarrhena floribunda (Don) Dur. & Schinz v^v. floribunda syn. (H. africana D C ,
H. Wulfsbergii Stapf, Rondeletia floribunda Don) APOCYNACEAE
L Used in Ghana and Nigeria as an antipyretic and antidysenteric (Dalziel, 1937).
C The stembark and rootbark of this small tree have been found to contain 1.2-2.44%
and 2.5-3.8% of total alkaloids, respectively. Of these alkaloids at least 50% is
Fig. 2.8(a). Holarrhenine.
(CH 3 ) 2 N
Fig. 2.8(b). 5/3-pregnane.
CH2 CH3
39
conessine, used mainly for its antibiotic action, which is not relevant here. Most of
the main alkaloids of the bark are steroid alkaloids derived from conamine, whilst in
the leaves alkaloids derived from pregnane (Janot et al., 1959) plus 0.6% of a
non-steroid alkaloid, triacanthine (an adenine derivative), are found (Janot et al.,
1959, 1960). Further acid phenols (p-hydroxybenzoic, protocatechuic and
p-coumaric acids) are found in the leaves of Holarrhena and quercetol and kaempferol
flavonols are found in the leaves and seeds (Paris and Duret, 1973).
Many of the steroid alkaloids derived from conamine, holarrhenine (Fig. 2.8a) or
pregnane (Fig. 2.Sb), like holarrimine, holaphyllamine and holaphylline, have a
hypotensive action and are simultaneously local anaesthetic and spasmolytic.
Triacanthine also has a hypotensive action, but while conessine, holarrhenine, etc.,
are cardiotoxic, triacanthine has a cardiotonic action on the heart of the rabbit in
doses of 1/30 of the LD 5 0 . It produces an important and long-lasting vasodilatation
of the coronary arteries and is, in addition, antispasmodic and respiratory analeptic
(Quevauviller and Blanpin, 1961). For this reason Foussard-Blanpin et al. (1969)
considered the possibility of its clinical use for cardiovascular disorders.
In addition, triacanthine appears to stimulate erythropoiesis and has been
observed to act on experimental anaemia in rabbits (Foussard-Blanpin et al., 1969)
(see also under plants with antibiotic and antiparasitic action).
Hunteria eburnea Pichon syn. (Picralima gracilis Chev.) APOCYNACEAE

Hunteria elliotii (Stapf) Pichon syn. (Picralima elliotii (Stapf) Stapf, Polyadoa
elliotii (Stapf) Pichon)
Hunteria umbellata (Schum.) Hallier syn. (Carpodinus umbellatus Schum., Pic-
ralima umbellata (Schum.) Stapf, Polyadoa umbellata (Schum.) Stapf)
The bark of H. umbellata is used in Sierra Leone and the Ivory Coast as a bitter tonic
and febrifuge (Dalziel, 1937).
The stembark and rootbark of all three species have a closely related chemical
composition. They mostly contain indole alkaloids with cardiovascular effects. In
1978 Le Men and Olivier identified 34 alkaloids in H. eburnea of which 18 were in
the bark, 9 in the leaves and 7 in the seeds. In H. elliotii the authors reported 26
alkaloids of which 7 were in the bark, 12 in the leaves and 7 in the rootbark. Amongst
the bark alkaloids eburnamonine, eburnamine, hunterine, vincadifformine, isobur-
namine and eburnamenine were found, whilst in the leaves of both species corymine
and acetylcorymine, were reported. The leaves of H. elliotii also contain tetra-
hydroalstonine (Morfaux et al., 1978). Eburnamonine and eburnine are also found
in the seeds (Bartlett and Taylor, 1963; Bartlett et al., 1959,1963; Renner, 1963).
Eburnamonine, eburnamine and hunterine are sympathomimetic and have a strong
and lasting hypotensive action (Raymond-Hamet, 1955). Morfaux et al. (1969)
suggest that the hypotensive properties are mainly due to hunteramine (a quaternary
ammonium compound) and that eburnamonine seems to have a favourable effect on
the circulation in general. Vincamonine, which is less toxic than its antipode
eburnamonine, has recently been introduced in pharmacy (Le Men and Olivier,
1978).
40
Pausinystalia johimbe (Schum.) Pierre ex Beille syn. (P. macroceras Kenn.,

Corynanthe johimbe Schum.) RUBIACEAE
The longitudinally fissured bark of the trunk of this tall forest tree is considered in
the Cameroons to be an aphrodisiac and stimulant (Dalziel, 1937).
The bark of the tree contains the alkaloids yohimbine, mesoyohimbine and yohim-
binine as well as corynanthine (closely related to yohimbine but less toxic and more
active as a sympatholytic agent), alloyohimbine and ajmalicine (which has a
vasodilating effect on the coronary arteries, as mentioned earlier). The bark is used
to extract yohimbine; the main stem gives the best material but is not rich in alkaloids
until the tree is 15-20 years of age when it can contain 2-15% (Holland, 1929; Paris
and Letouzey, 1960; Poisson, 1964).
Yohimbine is sympatholytic and hypotensive and has a local anaesthetic action
similar to that of cocaine but it is not mydriatic (see Oliver, 1960). It is given in cases
of atherosclerosis as it dilates the walls of the small peripheral arteries, thereby
increasing the flow of blood and decreasing the blood pressure. It is interesting to
note that its action differs from that of reserpine, which is also hypotensive but not
sympatholytic.
The vasodilating action of yohimbine is particularly strong on the sex organs,
hence its aphrodisiac action. It is mainly used in the form of the hydrochloride,
which was in the British Pharmaceutical Codex in 1949, in the French Codex 1949
Table A, and in the Pharmacopoeia Helvetica, 1949 (5-20 mg daily) (Raymond-
Hamet and Goutarel, 1965).
Corynanthe pachyceras Schum. syn. (Pausinystaliapachyceras (Schum.) de Wild.,

Pseudocinchona africana Chev. ex Perrot) RUBIACEAE
The bark of the tree is used on the Ivory Coast as an aphrodisiac and antipyretic. It
contains corynanthine, the closely related corynanthidine and corynantheidine and
several other alkaloids (Poisson, 1964).
Corynanthine is 4-5 times less toxic than yohimbine whilst its sympatholytic effects
are twice as strong (Steinmetz, 1976). It has mild local anaesthetic action, inferior to
that of cocaine.
Mitragyna inermis (Willd.) Ktze. syn. (M. africana (Willd.) Korth, Uncaria inermis
Willd., Nauclea africana Willd.) RUBIACEAE
Mitragyna stipulosa (DC.) Ktze. syn. (Nauclea stipulosa D C , M. macrophylla
Hiern)
The bark and leaves of both species are used in Nigeria, Guinea and the Ivory Coast
for fever and diarrhoea and also as a diuretic and analgesic (Pobeguin, 1912;
Raymond-Hamet and Millat, 1934; Kerharo and Bouquet, 1950). The wood is used
in Nigeria for carving small objects as it is easy to work (Dalziel, 1937).
The oxindole alkaloids rhynchophylline and rotundifoline have been reported to be
present in the leaves and in the bark of the stem and roots of both M. inermis and M.
stipulosa (Ongley, 1953; Shellard and Alam, 1968). At first Raymond-Hamet and
Millat (1934) had named an alkaloid they isolated from M. inermis 'mitrinermine',
41
but it could be shown by Badger et al. (1950) that this alkaloid, when purified, was
identical with rhynchophylline, isolated earlier by these authors from M. stipulosa.
From M. stipulosa another oxindole alkaloid, mitraphylline, has also been obtained
whilst in M. inermis speciophylline was also found (Beckett et al., 1963; Shellard and
Sarpong, 1969; Shellard et al., 1976). A bitter heteroside, quinovin, which can be
split into quinovic acid and quinovose has been isolated from M. inermis as well
(Badger etal, 1950; Beckett*?* al., 1963).
In order to try to understand the biogenesis and translocation of these alkaloids,
the alkaloid distribution of three West African Mitragyna spp. was studied by
Shellard and Sarpong (1969; 1970). In the above-mentioned species as well as in M.
ciliata Aubrev. and Pellegr., the main stembark and rootbark alkaloid is rhyn-
chophylline and in M. stipulosa and M. ciliata the principal leaf alkaloid is
rotundifoline while in M. inermis it is isorhynchophylline. The authors conclude that
it would appear that the alkaloids are synthetized in the leaves and that conversion
of the leaf oxindoles (by dehydroxylation of rotundifoline to rhynchophylline) takes
place in the leaves before translocation to the root (Shellard and Sarpong, 1970). The
leaves of an Asian species of Mitragyna, M. speciosa, contain in addition to other
alkaloids mitragynine (methoxycorynantheidine), a hallucinogenic agent (Tyler,
1966).
Already in 1932 Blaise had reported the occurrence of a hypotensive alkaloid in
Mitragyna spp. It was confirmed later that rhynchophylline, mitraversine and
mitraphylline lower the blood pressure by decreasing the rhythm of the heart (Xiao,
1983), and that they also have a local anaesthetic action. Further, these alkaloids
strongly stimulate intestinal and uterine contractions and are toxic to protozoa
(Massion, 1934; Caiment-Leblond, 1957; Ansa-Asamoa, 1967).
Cryptolepis sanguinolenta (Lindl.) Schltr. syn. (Pergularia sanguinolenta Lindl.,

C. triangularis N.E.Br.) PERIPLOCACEAE
In Nigeria the macerated roots are used for gripe (colic) as a tonic and sometimes in
rheumatism and urogenital infections (Boakiji Yiadom, 1979).
The roots contain a quinoline-derived indole alkaloid, cryptolepine, which is violet
in colour, producing yellow salts (Gellert etal., 1951).
Cryptolepine has a marked hypo thermic effect; it also induces prolonged and
important vasodilatation, causing marked and durable hypotension (Raymond-
Hamet, 1937, 1938). It has a low toxicity (120 mg/kg produce death in guinea pigs
about 12 h after administration). An aqueous extract of the root has antimicrobial
activity against three urogenital pathogens (Boakiji Yiadom, 1979).
Physostigma venenosum Balfour FABACEAE

Ordeal tree of Calabar
The poisonous effect of the Calabar bean in trials is caused by its strong sedative
action on the spinal cord which results in paralysis of the lower limbs and death by
asphyxia, and, in large doses, in paralysis of the heart. It is used by the Bakwiris with
other drugs in the local treatment of articular rheumatism (Dalziel, 1937).
42
From the seeds an alkaloid, physostigmine or eserine, is obtained (0.15%); in

addition, the beans contain geneserine or eseridine and several other alkaloids like
eseramine and physovenine (which is also myotic) (Robinson and Spitteler, 1964).
Eserine is mainly used in ophthalmic medicine for its myotic action (1-2 drops of a
1:1000 physiological solution: British Pharmacopoeia, 1934, British Pharmaceutical
Codex, Italian Pharmacopoeia, French Pharmacopoeia, 1949, Pharmacopoeia Hel-
vetica, etc.), but it also dilates peripheral blood vessels and slows the pulse. The
alkaloid acts by inhibition of cholinesterase, thus allowing acetylcholine to exert its
full effect on the smooth muscles, glands and heart. Being antidotal to strychnine,
nicotine, curare and atropine, it was used in myasthenia gravis to improve peristalsis
in post-operative intestinal atony, but has been replaced by synthetic neostigmine
(Martindale, 1969).
Eseridine is used in dyspepsia and as eye drops in glaucoma (Oliver, 1960; Paris
and Moyse, 1967, Vol. 2). The solutions must be protected from air, light and
moisture; their oxidation can be delayed for some time by adding ascorbic acid
(Swallow, 1951).
Thalictrum rhynchocarpum Dill. & Rich. RANUNCULACEAE

The roots of most Thalictrum spp. contain alkaloids of the berberine group with an
aporphine nucleus, such as thalictrine (= magnoflorine), as well as flavonoids.
Some Thalictrum alkaloids like thaliadine, adiantifoline and thaliadanine from T.
minus and an alkaloid fraction from T. revolutum DC. have a powerful and prolonged
hypotensive effect (at 2 mg/kg) in dogs, cats and rabbits. Further, thaliadanine is
antimicrobial to Mycobacterium smegmatis (Patel et aL, 1963; Wan Tra Liao et al.,
1978).
Thalicmine (ocoteine) hydrochloride is also hypotensive in dogs and cats (1-2 mg/
kg given intravenously) and inhibits the blood pressure response to adrenaline at
1-3 mg/kg. Detailed information about the constitution of the West African species
was not available in 1976 (Farnsworth and Cordell, 1976); none seems to have
become available since then.
Carica papaya L. C ARICACE AE

Pawpaw, papaya
Originating from Tropical America, this tree is extensively grown for its fruit. In
West Africa the plant is mainly used as a diuretic (roots and leaves), anthelmintic
(leaves and seeds) and to treat bilious conditions (fruit) (Dalziel, 1937).
The milky sap of the unripe fruit yields a complex proteolytic enzyme, papain,
which is not destroyed by heating. The crude papain consists of two crystallized
enzymes, papain and chymopapain, as well as tryptophan, tyrosine and cysteine,
which all seem to be part of the crude enzyme preparation. The enzyme has
peptidase, coagulase (acting on milk casein), amylase, pectase and lipase action
(Kerharo and Adam, 1974). Vitamins and traces of an alkaloid have also been found
in the latex. This alkaloid from the pyridine group, called carpaine, has also been
reported in other parts of the plant and particularly in young leaves (0.28%) (Bevan
43
and Ogan, 1964). The seeds contain, apart from fixed oils, carbohydrates, etc.,
carpasemine (a benzylthiourea), benzyl senevol and a glucoside (Manske and
Holmes, 1950-71, vol. 11, p. 491; Watt and Breyer-Brandwijk, 1962).
Papain has an anticoagulant effect. Intravenous injection of a purified extract in the
dog (2 mg/kg) increases prothrombin and coagulation time threefold; an anticoagu-
lant action has also been noticed in rabbits, rats and mice, the maximum effect being
achieved half an hour after the injection (Chandrasekhar et al., 1961). Standardiz-
ation of the enzyme has been suggested (International Commission for the Standard-
ization of Pharmaceutical Enzymes, 1965). The maximum dose tolerated by rats and
mice was found to be 50 mg/kg, while a therapeutic action was observed with doses
of 1-2 mg/kg. Acute toxic effects at higher doses were similar to those observed with
heparin (Chandrasekhar etal., 1961).
The enzyme is also used as a digestive enzyme in dyspepsia and digestive troubles
(British Pharmaceutical Codex, 1950, French Pharmacopoeia, 1949, Indian Phar-
macopoeia) and has also been used successfully in peritoneal instillation to avoid
adherences. In addition, it is claimed to eliminate necrotic tissues in chronic
wounds, burns and ulcers (Ravina and Wenger, 1957; Rigaud et al., 1956).
(Crude papain is of considerable commercial importance. In addition to its
pharmaceutical applications, great quantities are used in the brewing industry
(chill-proofing beer), in the food industry (in pre-cooked foods and in meat-
tenderizing preparations), and in the manufacture of chewing gum. It also finds
application in the textile industry (shrinkage resistance and other treatment of wool
and wool-containing materials), and in the rubber industry to season latex (Oliver,
I960).)
In small doses carpaine slows down the heart and thus reduces the blood pressure.
Higher doses produce vasoconstriction. In addition the alkaloid has a spasmolytic
action on the smooth muscles (Henry, 1949).
In humans, carpaine hydrochloride, given orally in doses of 0.01-0.02 mg/day or
given subcutaneously in doses of 0.006-0.01 mg/day has a digitalis-like action and
Noble (1947) recommends its use in hypertension.
Anthelmintic and amoebicide actions of the alkaloid have been reported (Kerharo
and Bouquet, 1950; Kerharo and Adam, 1974), and the seeds are also considered to
be anthelmintic and carminative (Dar et al.91965).
Plants containing hypotensive non-alkaloidal constituents.
Anacardium occidentale L. ANACARDIACEAE

Cashew nut tree
The cashew tree, native of tropical America, is widely cultivated, its kernels and fruit
being much appreciated. In Nigerian local medicine the astringent infusion of the
bark and leaves is used as a lotion and mouthwash to relieve toothache and sore gums
and is given internally in dysentery (Dalziel, 1937).
44
The gum exuding from the bark is a mixture of bassorin and true gum (Dispensary
of USA, 1955). Cashew 'balsam' is composed of anacardic acid and its decarboxy-
lated derivates, anacardol, cardol and gingkol, which are aromatic phenols.
In the leaves, polyphenols (chiefly hydroxybenzoic acid) and flavonoids which are
heteromonosides (glucoside, rhamnoside, arabinoside or xyloside) of kaempferol
and in particular quercetin were found by Laurens and Paris (1976) and by Attanasi
and Caglioti (1970).
Ingestion of extracts of the leaves and bark has been found to reduce hypertension
and hyperglycaemia to normal values. The effects are believed to be due to
peripheral vasodilatation. The hypotensive effect was observed first in rats with
three different forms of experimental hypertension (Giono et al., 1971) (see also
under plants with antibiotic and antiparasitic action).
Morinda lucida Benth. syn. (Morinda citrifolia Chev.) RUBIACEAE

Brimstone tree
Stem, bark, roots and leaves are bitter and astringent and are used in Nigeria in the
treatment of fever, malaria, yellow fever, jaundice and dysentery (Dalziel, 1937;
Oliver, 1960).
Tannins, methylanthraquinones and a heteroside, morindin, have been reported in
M. lucida and allied species (M. geminata DC.) in varying amounts according to the
species and the geographical origin of the plant (Caiment-Leblond, 1957).
The use of a total extract of leaves and stembark of M. lucida is recommended by
Dang Van Ho (1955) for the treatment and prevention of hypertension and its
cerebral complications. Purified extracts produced a strong hypotensive action
which, however, when compared to the action of Rauvolfia vomitoria, proved to be
of shorter duration. Further, the extract showed a distinct diuretic and a slight
tranquillizing effect. In view of the complete absence of toxic side-effects, permitting
the use of strong and frequent doses, La Barre and Wirtheimer (1962) consider that
M. lucida may be very useful when strong doses are required to initiate the treatment
of hypertension. M. lucida bark and leaves have been proved to be effective in the
treatment of jaundice, thus justifying one of its local uses (Guedel, 1955).
Allium sativum L. LILIACEAE

Garlic is widely cultivated and finds broad applications in northern Nigeria (respirat-
ory and infectious diseases, worms, skin diseases, etc.) (Oliver, 1960).
The strong-smelling juice of the bulbs contains a mixture of mono- and poly sul-
phides. The main compound of these is allicin (diallyl disulphide oxide) which is the
result of spontaneous enzymatic degradation of alliin (S-allylcysteine sulphoxide).
Allicin is unstable and decomposes into poly sulphides (Schulz and Mohrman, 1965;
Augusti, 1974,1975,1976a, b).
The hypotensive effect in arterial hypertension of a tincture of garlic (20-25 drops
daily) is attributed to allicin. This constituent is also antidiabetic and bacteriostatic
(Bhandari and Mukerjee, 1959; Jain and Vyas, 1974). For more details on Allium see
Oliver-Bever and Zahnd (1979).
45
Sapindus trifoliatus L. SAPINDACEAE

L A native of tropical Asia, the plant is naturalized in many areas of West Africa. It is
used as a fish poison in India (Singh et al., 1978).
C The fruit of 5. trifoliatus contains saponins. Hederagenin-heterosides have been
identified by Takagi et al. (1980).
P Alcoholic extracts showed, when injected intravenously in cats in doses of 10-20 mg/
kg, a dose-dependent decrease in blood pressure and heart rate. Tests demonstrate
the direct action of the drug on the vascular smooth muscles to produce a
hypotensive effect (Singh et aL, 1978).
Mostuea hirsuta (Anders, ex Benth.) Baill. ex Bak. LOGANIACEAE

C The roots of related M. stimulans and M. buchholzii Engl. contain indole alkaloids
identical to, or closely related to sempervirine and probably gelsemine. The alkaloid
content of M. hirsuta seems poor (0.2%) in the roots (Bouquet, 1975). The LD 5 0 of
these alkaloids in guinea pigs is 15.4 mg and 250 mg, respectively (Paris and
Moyse-Mignon, 1949b; Gellert and Schwartz, 1951).
P In mice 600 mg of alkaloids per kg of body weight, given subcutaneously, produced
agitation and convulsions followed by death. The alkaloids were found to be
analgesic and cardiac depressant, stimulating respiration in small doses. They can
cause death through respiratory paralysis in higher doses, sempervirine being the
most toxic of the two. In the chloralosed dog a dose of 0.1-0.2 g of an extract of the
root of M. stimulans produces a prolonged fall in blood pressure and after a short spell
of tachycardia, cardiac and respiratory depressant effects (Chevalier, 1947).
It appears that the Mostuea spp. that were investigated, and no doubt also M.
hirsuta, have similar properties to Gelsemium and are used for the same indications as
this (Paris and Moyse, 1971, Vol. 3; Kerharo and Adam, 1974).
Adenia cissampeloides (Planch, ex Benth.) Harms syn. (Modecca cissampeloides

Planch, ex Benth., Ophiocaulon cissampeloides (Planch, ex Benth.) Mast)
PASSIFLORACEAE
L Used in southern Nigeria and Ghana as a fish poison and as a remedy for lumbago.
The Mano of Liberia use the plant to produce amnesia (Dalziel, 1937; Harley, 1941;
Watt, 1967).
C In the related South African A. digitata Engl. a toxalbumin and a cyanogenetic
glycoside were reported by Watt and Breyer-Brandwijk (1962).
P Pharmacological investigations showed that aqueous extracts of the Nigerian
climber had a graded depressor effect on the blood pressure of the anaesthetized cat.
The effect was neutralized by small doses of atropine. A second active principle
might be sympathomimetic with vasoconstrictive action (Adesogan and Olatunde,
1974).
Achyranthes aspera L. AMARANTHACEAE

L A common weed locally used in Nigeria as a diuretic and expectorant (Oliver, 1960).
C Chemical and pharmacological analyses have been undertaken on the Indian plants.
46
A betaine derived from Af-methylpyrrolidine 3-carboxylic acid was located by Basu

and called achyranthine (Basu etal., 1957; Kapoor and Singh, 1966). The seeds were
found to contain a saponin fraction composed of glycosides (glucose, galactose,
xylose and rhamnose) of the genin oleanic acid (Gopalachari and Dhar, 1958). Later
work led to the isolation of two pure saponins, Achyranth.es saponins A and B
(Hariharan and Ranjaswani, 1970).
Achyranthine has hypotensive, cardiac depressant, vasodilatating and respiratory
analeptic actions. It also has a spasmogenic effect on smooth muscles (guinea pig,
rabbit, rat) and is diuretic, purgative and slightly antipyretic (Neogi et al., 1970).
The diuretic action of the plant has been attributed to its high potassium content.
The total saponosides of the Indian plant significantly increase the tone and force of
contraction of isolated frog, guinea pig and rabbit hearts. The effect was quicker in
onset and shorter in duration than that exerted by digitoxin (Kapoor and Singh,
1966; Neogi et al., 1970; Gupta et al., 1972a, b). It is suggested that the increased
contractility caused by the saponin could be related to its phosphorylase activity
(Ram etal., 1971; Indian Council of Medical Research, 1976). It has also been noted
that an extract of the plant, when given orally (5 mg/kg), exerts a diuretic, purgative
and hypoglycaemic action in rats (Dhar etal., 1968; Neogi etal., 1970; Oliver-Bever
and Zahnd, 1979) and that it is also useful in treating subacute and mild reactions in
leprosy (Ojhaef al., 1966).
Group A2: hypertensives
Musa sapientum L. syn. (M. paradisiaca var. sapientum Ktze.) MUSACEAE

Banana
Analysis of the bracts of ten wild species of bananas has shown the presence of six
anthocyanidins (pelargonidin, cyanidin, delphinidin, malvidin, paeonidin and
petunidin). The ripe and unripe fruit also contains 5-hydroxytryptamine (= sero-
tonin) (Hood and Lowburry, 1954; Hegnauer, 1962-8; Sinhaetal., 1962). Further,
dopamine and noradrenaline (adrenaline precursors) have also been reported in
banana plants (Harborne et al., 1974, p. 1013). The three amino phenols are
sympathomimetic and in other plants (Sarothamnus scoparius Koch.) have proved to
have marked vasoconstrictive properties and to be hypertensive. Banana flowers also
have an oral hypoglycaemic action (Jain, 1968; Oliver-Bever and Zahnd, 1979).
Moringa oleifera Lam. syn. (M. pterygosperma Gaertn.) MORINGACEAE

Horseradish tree (native of India, cultivated throughout the tropics)
In Nigeria root and bark are considered to be antiscorbutic and are used externally
as counter-irritants (Dalziel, 1937). In India the root is used as a stimulant in
paralytic affections, epilepsy, nervous debility, hysteria, spasmodic affections of the
bowel and as a cardiac and circulatory tonic et al., (Chopra et al., 1956; Watt and
Breyer-Brandwijk, 1962; Ramachandran etal, 1980).
In the rootbark the sulphurated aminobases moringinine and spirochine have been
reported, as well as benzylamine (first called moringine) and glucotropaeoline.
47
Further, the root contains two antibiotic constituents, athomine and ptery-
gospermine; the latter is probably a condensation product of two benzylisothio-
cyanate molecules with one benzoquinone molecule (Kurup and Narasimha Rao,
1954; Hegnauer, 1962-8, vol. 5, p. 130; KondagboandDelaveau, 1974; Salujaera/.,
1978).
Moringinine has a sympathomimetic action similar to that of adrenaline; it produces
peripheral vasoconstriction, raises the blood pressure and acts as a cardiac stimulant.
However, Chopra et al. (1938) consider that the quantities present in the plant are
too small to make it of interest for cardiology. Moringinine also depresses the smooth
muscle fibres; it relaxes the bronchioles and inhibits the tone and movement of the
intestine in rabbits and guinea pigs (Das et al., 1957a, b).
Spirochine accelerates and amplifies the heartbeat in Man in doses of 0.035 g/kg
and has an opposite effect at a dose of 0.35 g/kg (Watt and Breyer-Brandwijk, 1962).
It can produce general paralysis of the CNS. Spirochine also has an antibiotic action,
mainly in gram-positive infections, and is used as an external antiseptic and
prophylactic in infected wounds (Chatterjee and Mitra, 1951).
Pterygospermine has a powerful antibiotic and antimycotic effect and athomine is
particularly active against the cholera vibrion (Kurup and Narasimha Rao, 1954;
Sen Guptas al., 1956; Das etal., 1957a, b; Kurup et al., 1957).
Group B: plants acting on vascular resistance (vitamin P action)
Citrus limonum. C. aurantium, C. decumana RUTACE AE

Largely cultivated
Citroflavanoids are extracted from the peel of citrus fruit (as a by-product of
fruit-juice preparation). They consist of a mixture of which the main constituents are
hesperidoside (rhamnoglucoside of hesperetol), naringoside and eryodictyoside
(flavanones). The peel also contains essential oils and vitamin C. The inconvenience
of the citroflavanones is their low solubility in water, which has led to research with
a view to finding more soluble hemisynthetic derivatives like Mg 2+ chelates
(Horhammer and Wagner, 1962; Ravina, 1964; Paris, 1971 etal., 1972).
Citroflavonoids control the permeability of the blood vessels by decreasing the
porosity of the walls and thus improving the exchange of liquids and the diffusion of
proteins. They are therefore used in complaints in which the permeability is
increased, such as venous insufficiency (varicose veins, haemorrhoids, capillaritis),
and in oedema and ascites in cirrhosis (Paris and Delaveau, 1977; Pourrat, 1977).
The increase in the resistance of the capillaries through the citroflavonoids is based
on a complex mechanism including the protective action of o-diphenols on
catecholamines participating in vascular solidity. When capillary resistance is
diminished, citroflavonoids can prevent bleeding in hypertensive or diabetic patients
(diabetic retinopathy) or in purpurea and where there is a tendency to haematoma
(Paris and Moury, 1964; Vogel and Strocker, 1966; Paris, 1977).
The citroflavonoids are also said to have anti-inflammatory, antihistamine and
diuretic actions and can cause dilatation of the coronaries (Paris and Delaveau,
1977).
48
Piliostigma reticulatum (DC.) Hochst. syn (Bauhinia reticulata D C , B. benzoin

Kotschy) CAESALPINIACEAE
Bauhinia purpurea L., B. tomentosa L., B. variegata L. (introduced spp.)
St Thomas tree
A poultice of the leaves and bark of Piliostigma is used in Senegal and northern
Nigeria as a haemostatic, and an infusion of the bark and buds of B. variegata is given
to control bleeding in haematuria and menorrhagia and as an astringent in diarrhoea.
The powdered bark of B. thonningii is applied to wounds and ulcers (Dalziel, 1937;
Kerharo and Adam, 1974).
In all species flavonoids (quercetol and kaempferol glycosides) have been found in
the leaves, bark and flowers. In B. variegata and B. tomentosa rutosides and
isoquercitroside have been reported; from B. tomentosaflowerpetals 4.6% of rutin
has been extracted (Visnawadham et al.9 1970; Duret and Paris, 1977). Piliostigma
contains tartaric acid and tartrates in fruit and leaves. In the leaves 5.9% free
(-)-tartaric acid and 0.5% quercitroside have been reported. The flavonoids seem to
justify their local use as coagulants.
Fig. 2.9(a). Adansonia digitata L., flower.

49
Baissea leonensis Benth. syn. (B. brachyantha Stapf) APOCYNACEAE

The leaves contain no alkaloids but they do contain flavonoids, mainly coumarins. A
new crystallized coumarin heteroside, baisseoside, which is a 6-rutinoside of
esculetol, was isolated in 1970 by Pousset et al. Other heterosides reported are
isoquercitroside, kaempferol 3-glucoside and kaempferol heteroside (Duret and
Paris, 1972).
Adansonia digitata L. (Fig. 2.9) BOMBACACEAE

Baobab, monkey bread
The fruit, seeds and leaves of the baobab are used in food and the bark provides fibre.
In West African local medicine all parts are used; they are said to be diaphoretic,
antipyretic, antidysenteric, emmenagogic, antifilarial, vulnerary, etc. (Sebire, 1899;
Dalziel, 1937; Oliver, 1960).
The leaves contain a mucilage consisting mainly of galacturonic acid and rhamnose,
free sugars, tannins, catechins and a dehydroxyflavanol, adansonia flavonoside.
They also contain calcium oxalate, potassium tartrate and sodium chloride. Bark
and roots also contain a mucilage as well as pectins and an antipyretic agent,
adansonin, said to have a strophanthin-like action (Merck Index, 1960; Oliver,
1960; Watt and Breyer-Brandwijk, 1962).
Fig. 2.%b). Adansonia digitata L., fruit.

50
Adansonia flavonoside showed low toxicity; mice tolerated 1 g/kg given subcu-
taneously. Given intravenously, 0.01 g/kg produced only slight hypertension in dogs
and decreased the permeability of the capillaries in rabbits, but to a lesser extent than
does rutoside (Paris and Moyse-Mignon, 1951).
Mangifera indica L. ANACARDIACEAE

Mango tree
Naturalized in West Africa. The bark and leaves have astringent properties and are
used in Nigeria as a lotion to relieve toothache, sore gums, sore throat, etc., or as an
infusion in diarrhoea and dysentery (Dalziel, 1937).
All organs are rich in tannins. In the leaves of the West African species four
anthocyanidins (3-monosides of delphinidin, petunidin, paeonidin and cyanidin),
leucoanthocyanins, catechic and gallic tannins, mangiferin (flavonic heteroside),
kaempferol and quercitin (both free and as glycosides) were reported (Jacquemain,
1970,1971).
In pharmacological tests anthocyanidins similar to those found in mango leaves
but extracted from Vaccinium myrtillus leaves increased the resistance and decreased
the permeability of capillary vessels, and have been successfully used for over 20
years in treating vascular troubles, eye complaints and diabetes (Pourrat, 1977). In
diabetic angiopathy they inhibit, or slow down, the modifications of the capillary
wall, and it is believed that the improvement obtained in diabetes with
anthocyanosides can well be due to recovery of the vascularization of the pancreas.
Excellent results were also obtained in retinopathy of hypertensive or diabetic
origin and anthocyanosides are in general a valuable aid in venous complaints,
capillary fragility, purpura, cirrhosis and in the prevention of haemorrhagic acci-
dents through the use of anticoagulants (Pourrat, 1977).
Feng et al.y (1964) noted that injection of an aqueous extract of leaves and stems
of Mangifera produces in dogs a distinct hypotensive action. In rabbits a similar
effect was obtained with an alcoholic extract (Feng et al., 1964). It seems that a
suitable fraction with vitamin P action should be easily obtainable from mango
leaves. Some toxic constituent may have to be eliminated first, as absorption of
preparations based on the leaves, stems and bark produces irritation of the stomach
and kidneys, and ingestion of the fruit in large quantities can produce shock
reactions (Ruben et al.91965).
The aqueous extract of the stembark showed favourable results in transplantable
cancer tumours. These have been reduced by 47% in adenocarcinoma 765, and by
53% in sarcoma 180 (Abbot et al.91966).
Sophora occidentalis L. syn. (S. nitens Schum. & Thonn., S. tomentosa (of FTA)
FABACEAE
The poisonous seeds of most Sophora spp. are used in East Africa as a poison for fish
and vermin (Dalziel, 1937). They contain 2% sophorin, which has proved to be
identical to cytisin and has emetic and cathartic actions (Henry, 1949).
The flowerbuds of the Asian 'Pagoda tree' (S. japonica) are rich in rutosides (15%)
and are used in industry for the extraction of the rutosides. These are also obtained
51
in quantity from the leaves of several Eucalyptus spp. and from buckwheat (Paris and
Moyse, 1967, p. 375).
No indications as to whether the flowerbuds of the African Sophora also contain
rutosides have been found.
Camellia thea Link syn. (Thea sinensis) TERNSTROEMACEAE

Tea plant
Tea is also cultivated in West Africa.
The leaves contain vitamin P constituents as well as vitamins C and B. The
flavonoids are rhamnoglucosides and rhamnodiglucosides of kaempferol, quercitin
and myrecetol. Further, catechols and tannins have been reported, as well as 2-4%
of alkaloids (caffeine and theophylline) (Roberts and Myers, 1959; Roberts and
Williams, 1959).
Tephrosia purpurea (L.) Pers syn. Cracca purpurea L., T. leptostachya DC.)
FABACEAE
L The plant is used in India as a deobstruent, diuretic and cough remedy, and also for
bleeding piles (Pandey, 1975).
C The roots, leaves and seeds contain tephrosin, deguelin and quercetin; the roots also
contain isotephrosin and rotenone, while 2.5% rutin is found in both the roots and
leaves (Krewson and Naghski, 1953).
P Rutin is increasingly used in capillary fragility and may be useful in the treatment of
the after-effects of atomic radiation. The roots, like those of T. vogelii and T.
densiflora, are ichthyotoxic but have only a weak insecticide action (Watt and
Breyer-Brandwijk, 1962, p. 656).
By improving the peripheral arterial circulation, rutin is also antihypertensive
(Paris and Moyse, 1967; Paris, 1977).
Teclea sudanica Chev. RUTACEAE

Paris and Etchepare (1968) found C-flavonosides in the leaves of T. sudanica. The
leaves are reported to have hypotensive action. They contain 0.5% alkaloids;
maculine, skimmianine and kokusaginine (Vaquette et al.91974).
Arachis hypogaea L. FABACEAE

The skins of the nuts contain bioflavonoids with vitamin P action. As other
constituents of the plant promote blood coagulation, its properties have been
described below.
Group C: plants promoting blood coagulation and formation
Arachis hypogaea L. FABACEAE

Peanut, groundnut, monkey nut
L The nuts are a valuable local food crop and are also exported on a large scale.
C Peanuts have a high lipid content and contain vitamins B l 3 B2 and B 3 as well as
proteins and phytosterols. Aflatoxins can be found mainly in groundnut cakes,
52
formed under the influence of certain fungi under faulty conditions of storage and
harvesting. They are toxic, substituted coumarins. The thin skins of the nuts contain
bioflavonoids, tannin, phlobaphen and flavanone (Tayeau and Masquelier, 1949;
Ravina, 1964; Adrian and Jacquot, 1968).
The presence of a haemostatic factor in groundnuts, first reported in 1960 (Boud-
reaux and Frampton, 1960), was later confirmed by several research workers. The
factor considerably improves the condition of patients with haemophilia. A daily
intake of 180 g of peanut flour, or of 14 g of an alcoholic extract, begins to produce
effects after as little as 48 h (Boudreaux and Frampton, 1960; Boudreaux et al.,
1960). This action has been attributed to a constituent similar to 5-hydroxytryp-
tamine (= serotonin in animal tissue and in particular in blood platelets and
produces vasoconstriction of the blood vessels), which also stimulates smooth
muscles (Boudreaux et al., 1960). However, the authors concerned differ as to where
the active constituent is located and its mode of action. Adrian and Jacquot (1968)
assume that this may be because in the groundnut there are different factors
influencing blood coagulation. Some authors consider that only certain forms of
haemophilia such as thrombopenic haemorrhage, chronic myelosis, vascular pur-
pura and metrorrhagia can benefit from this treatment, others also include
haemophilia A.
The groundnut skins contain, in addition, a lipoxidase and protease inhibitor
(Cepelak and Horacova, 1963; Narayanan et al., 1963), 7% pyrocatecholic tannins
and a chromogen of anthocyanins, closely related chemically to vitamin P. Injection
into guinea pigs of a solution equivalent to 1 mg of this chromogen doubles their
capillary resistance. It is very well tolerated; even doses of 20 mg produced no toxic
effect (Tayeau and Masquelier, 1949).
Further, an oestrogenic factor, not destroyed by refining, was found in the oil of
the nuts and a thermostable goitrogenic factor has been reported in the non-lipid
fraction (Buxton et al., 1954; Booth et al., 1960).
Terminalia laxiflora Engl. syn. (T. elliotii Engl. & Diels, T. sokodensis Engl.)
COMBRETACEAE
Terminalia avicennoides Guill. & Perr. syn. (T. lecardii Engl. & Diels, T. dic-
tyoneura Diels)
Terminalia macroptera Guill. & Perr. syn. (T. chevalieri Diels)
The powdered bark of T. macroptera and T. laxiflora is used in wound dressing and
in the treatment of piles for its haemostatic and healing effects, whilst a decoction of
bark and leaves is said to be diuretic. Antidiarrhoeic and a cholagogic action are also
ascribed to different Terminalia spp., which are often confused.
The bark of the three Nigerian species mentioned above contains laxiflorin (a
polyhydroxylactone), whilst in the stembark sitosterylpalmitate and trimethylellagic
acid are found. In the wood, terminolic, ellagic and tri- and tetramethylellagic acid
are reported (Ekong and Idemudia, 1967; Idemudia and Ekong, 1968).
Ellagic acid (a tannin depside of gallic acid) both reduces the bleeding time in rats
and shortens the normal coagulation time without producing any toxic effects
(Cliffton et al., 1965; Girolami et al., 1966). In vitro the acid does not seem to act on
53
sections of duodenum or uterus of rats (Bhargava et al., 1968; Bhargava and

Westfall, 1969). Chopra et al., (1938) reported a cardiotonic action in a number of
Indian Terminalia spp. including T. avicennoides. In Nigeria the aqueous extract of
the stembark and roots of this species proved to have the strongest antibiotic action
of the different Terminalia spp., mainly on Gram-positive organisms (Sarcina lutea,
Staphylococcus aureus and Mycobacteriumphlei) (Malcolm and Sofowora, 1969).
Canavalia ensiformis (L.) DC. FAB ACE AE

Olsen and Liener (1967) report hemagglutinin effects of the Jack bean through
concanavalin A. The seed of the bean is a source of urease, an enzyme which finds
use as a specific reagent for urea in biological chemistry.
Group Cj: Plants with a vitamin K action (haemostatic action).
Lawsonia inermis L. syn. (L. alba Lam.) LYTTHRACEAE

Henna, Egyptian privet, alkanna
The leaves are used in local northern Nigerian medicine to control perspiration, and
both leaves and roots are used as an emmenagogue and anthelmintic. The bark is
recommended as an astringent and is administered for jaundice and skin diseases. In
Arab medicine the root is considered useful in the treatment of hysteria and of
nervous diseases in general (Dalziel, 1937; Oliver, 1960).
The leaves contain lawsone, a 2-hydroxy-l,4-naphthoquinone (a colouring matter),
resin and hennatannin. They can be harvested from the second year onward and the
plant may live for 15 years (Latif, 1959).
The colouring matter is used for colouring oils and ointments. Henna also appeared
in the British Pharmaceutical Codex 1934 as a hair dye. Apart from the slight vitamin
K action and the antihaemorrhagic properties attributed to lawsone (Almquist and
Klose, 1939), it has powerful bactericidal effects comparable to those of sul-
phonamides and penicillin (Caiment-Leblond, 1957). The naphthoquinone is
mainly of interest, however, because of its emmenagogic and oxytocic actions. The
effect of a 10% extract on the uterus is comparable to that of pituitary gland
preparations (Latour, 1957).
Diospyros mespiliformis Hochst. ex DC. syn. (D. senegalensis Perr. ex DC.)

EBENACEAE
Swamp ebony, monkey guava
In northern Nigeria an infusion of the leaves is given for fever and dysentery and is
applied in wound dressings as a haemostatic. A decoction of the rootbark is given for
skin eruptions and also as an anthelmintic in human and veterinary medicine
(Dalziel, 1937; Oliver, 1960).
Many Diospyros spp. were found to contain hydroxynaphthoquinones such as
plumbagin (2-methyl-5-hydroxy-l,4-naphthoquinone), diospyron, diospyrol and
diosquinone. Plumbagin (originally found in Plumbago), occurs in the rootbark of
D. mespiliformis (0.9%) and of D. canaliculata de Wild. (D. xanthochlamys) (2.25%)
and also in the leaves of these species (traces and 0.12%, respectively). Further,
54
tannins, a saponin and a substance probably identical to scopolamine have been

repotted in both species (Kerharo and Bouquet, 1950; Paris and Moyse-
Mignon, 1949a).
In doses of 0.2 g/kg a rootbark extract of D. mespiliformis produces hypertension and
exaggerated respiration in dogs. The rootbark of all the species here noted and of
D. tricolor (Schum. & Thonn.) Hiern has an antibacterial action on staphylococci,
streptococci and diphtheria bacilli probably due to plumbagin. Besides the antibiotic
action, insecticide and anthelmintic properties have also been reported in the various
species of Diospyros (Paris and Moyse-Mignon, 1949a). As the naphthoquinones also
have a vitamin K action, their local application in wound dressing seems fully
justified (Fieser et aL> 1941).
Jatropha curcas L. EUPHORBIACEAE

Physic nut, Barbados nut
The oil of the seeds has a purgative action and is used all over West Africa in local
medicine as a remedy for dropsy, sciatica, paralysis and skin diseases (Dalziel, 1937).
The seeds contain 50% of a fixed oil, pinhoen oil, as well as a mucilage composed of
xylose, galactose, rhamnose, galacturonic acid and a toxalbumin, curcin (Bezanger-
Beauquesne, 1956; Mourgue et al.9 1961a, b). Glycosides have been detected in an
extract of the shell (Bose et al., 1961).
The mucilage fraction of the seed pulp reduces prothrombin time and coagulation
time. Its effect is comparable to that of Russel's viper venom used as a source of
thromboplastin. It is four times less active, however. On the other hand, the
toxalbumin fraction has been found to increase the prothrombin time (Bose et al.9
1961). Curcin has many features in common with ricin but is less toxic. The
purgative action of the seed oil has been confirmed. In addition the seeds have a
certain value as an insecticide. Fruits and seeds contain a contraceptive principle
(Mameesh, 1963). An ethanolic extract ofJ. curcas has shown confirmed in vitro and
in vivo action against P388 lymphocytic leukemia (Hufford and Oguntimein, 1978).
Group C2: plants with an antivitamin K action (haemolytic action).
Balanites aegyptiaca (L.) Del. syn. (Ximenia aegyptiaca L.,Agialida senegalensis v.

Tiegh., A. barteri v. Tiegh., B. zizyphoides Mldbr. & Schltr., A. tombouctensis v.
Tiegh.) ZYGOPHYLLACEAE
Desert date, soap berry tree, thorn tree
In Hausa medicine (northern Nigeria), roots and bark are used as a purgative and in
colic, and are considered ichthyotoxic and anthelmintic. The oil of the fruit kernels
is employed for the dressing of wounds and as an embrocation in rheumatism
(Dalziel, 1937; Oliver, 1960).
From the dried seeds, 48% of a fixed oil, Zachun oil, has been obtained, whilst the
seedcake contains 50% protein. The root, bark, fruit, leaves and seeds contain
saponins (Kon and Weller, 1939). In the seeds, 6.7% of a tetraglycoside of diosgenin
has been reported. The diosgenin content of the whole dried African plant was 5.6%
(Hardman and Sofowora, 1972). In the other parts of the plant the genin consisted
55
of two-thirds yamogenin and one-third diosgenin. B. aegyptiaca has been investi-

gated as a source of steroidal sapogenins for the hemisyn thesis of corticosteroids and
hormones (Marker, 1947; Hardman and Sofowora, 1972).
The root, bark, fruit pulp and seeds have been found to be lethal to fish and also to
freshwater snails, which act as an intermediate host for bilharzia, and to the minute
free stages of the parasite. The planting of Balanites alongside infested rivers to
combat bilharzia propagation was therefore recommended by Archibald in 1933.
Since then, other plants with stronger molluscicidal properties, such as Polygonum
senegalense have been reported (Dossaji et al.9 1977). Tephrosia and Jatropha curcas
(mentioned above) are also lethal to the molluscs. Antimicrobial properties were
reported by Malcolm and Sofowora (1969). The saponoside is strongly haemolytic,
with a toxicity to tadpoles similar to that of digitoxin, but less rapid in action. At a
concentration of 10~6 of the saponoside in water, the tadpoles survive for more than
24 h. On frog's heart, a dose of 1 mg given subcutaneously produces no apparent
digitalis effect; the isolated heart is stopped by a dilution of 10~3. Thus a digitalis-like
action exists but it is so weak as to be almost negligible (Caiment-Leblond, 1957).
In Schwenkia americana and in Carica papaya, described earlier, as well as in
Swartzia madagascariensis Desv. fruit (Beauquesne, 1947), the presence of
haemolytic saponosides has also been reported. In Swartzia these have been named
Swartzia saponosides A and B, the genin of them being swartzigenin. The drug is
ichthyotoxic and is strongly haemolytic (Beauquesne, 1947).
Group C3:plants with an anti-anaemic action.

Although a few plants have been recommended for the treatment of anaemia in local
West African medicine, their action has not been confirmed. No plants possessing a
proven anti-anaemic effect seem to have been reported, nor has mention been made
of folk acid or vitamin B12 contents in West African plants. Spinach, yeast,
Streptomyces griseus and S. aureofaciens seem to remain the only few, generally
known, vegetable sources of these compounds. In sickle cell anaemia, Zanthoxylum
zanthoxyloides has been used, as mentioned under the description of this plant.
The nervous system
In this chapter are described plants having a direct action on the central nervous
system (CNS) and those plants that are used in the treatment of mental and nervous
diseases, including those acting via the cholinergic and adrenergic systems.
The CNS, which is best considered as a whole, controls all sensory and integrated
motor activity. Plants which interefere with its function may be classified as follows:
I CNS stimulants
Analeptics, stimulants
Antidepressants, hallucinogens
II CNS depressants
General anaesthetics, narcotic analgesics
Analgesic-antipyretics
Hypnotics, sedatives and tranquillizers
Anticonvulsants and antiepileptics
III Peripherally acting depressants of the CNS
Local anaesthetics (on sensory nerves)
Neuromuscular blockers (curare action) (on motor nerves) and anticonvul-
sants
IV Those with cholinergic and adrenergic actions
Depressants acting on both autonomic nervous system (ANS) and CNS
terminals
Antispasmodics acting mainly on sympathetic terminals
Stimulants of the cholinergic and adrenergic systems
However, in practice no such clear classification can be made. Even a single plant
constituent can act on both the CNS and the ANS. The plants are therefore grouped
by the main resulting effect when both the CNS and ANS are involved. Also, most
plants have many different constituents and these often have divergent actions
(Table 3.1). In addition only a restricted number of the constituents may be known
and pharmacological screening has in many cases been carried out on extracts
containing several constituents in varying proportions or doses. An arbitrary
decision may therefore have to be taken, in many cases based on our very partial
57
knowledge about the plants, in considering the quantitatively and qualitatively most
important constituent(s) of the plant and the most frequently reported effects.
I still consider it important to classify the plants by their clinical indications, in
spite of the fact that the greatest amount of research is still to come, to keep in mind
the aim, and to see rapidly and more clearly which of the far too numerous
utilizations of each plant by local healers appear the most important and are
confirmed by scientific observations. The enormous treasure of natural remedies
should not be used in a haphazard way. A simple extraction might in some cases
enable a healer to increase or isolate a fraction with a certain action or to eliminate a
toxic constituent. The experience with the same plants in similar climates even in
different continents should not be ignored (although the amount or quality of the
constituents can vary and should be checked).
We saw in mentioning their mode of action in the Introduction (Chapter 1) that
the activity of drugs acting via the nervous system can be based on their interference
with the chemical mediators of nervous transmission (acetylcholine and
catecholamines) at their receptor level. Anticholinergic action can be localized:
(1) at the level of the parasympathetic terminals, thus producing antispas-

modic and antisecretory activities (used to prepare for anaesthesia) and
mydriasis in ophthalmology (atropine action);
(2) at the level of the sympathetic and parasympathetic ganglia;
(3) at the level of the neuromuscular junctions (curare action).
On the other hand, the drugs can interfere with the catecholamines (noradrenaline
and adrenaline) or the chemical intermediates in their synthesis (e.g. dopamine) in
the post-ganglionic sympathetic nerves and their terminals. This action is called
'adrenergic' action. The catecholamines are also involved in central activity. In this
field, the so-called 'antidepressant' drugs, for example, are supposed to act in
correcting the basic biochemical trouble of the depression which could be the
insufficiency of noradrenaline at the level of the encephalic synapses through
degradation of cerebral catecholamines. The enzyme responsible for intracellular
degradation of catecholamines is monoamine oxidase (MAO). The activity of this
enzyme is blocked by a group of drugs called monoamine oxidase inhibitors
(MAOIs), often found in the Rubiaceae (Table 3.2), which thereby inhibit the
inactivation of noradrenaline. Unfortunately, these prevent not only degradation of
cerebral catecholamines but also that of the catecholamines of the peripheral
sympathetic system and of certain substrates. Thus, the biochemical properties of
the MAOIs explain their long-lasting action, the numerous secondary effects
observed and the diversity of the accidents produced. Their effects are very difficult
to control and they are now seldom employed for psychiatric treatments. They
cannot be taken together with alcohol, or with food including biogenic amines
(especially tryptamine) or amino glucosidic antibiotics, in order to avoid attacks of
hypertension, nausea and cephalgia (Lechat et aL, 1978; Goodman and Gilman,
1980).
Table 3.1. More important constituents and divergency ofpharmacology of West African Menispermaceae speciesa
Part Local use

Plant used Constituents Chemical group of plant Pharmacology of constituents
Tricliseae
Triclisia dictyophylla Diels syn. Leaves Phaeanthine Bisbenzylisoquinoline Anaemia Muscular relaxation
A/,Af-Dimethylphaeanthine alkaloids (Guha Oedema of legs when introduced in the
Tiliacora tricantha Diels) Cocsuline et al. ,1979) bloodstream, muscle-nerve
Isotetrandrine transmission blocking ensues,
Stebisimine hence muscular relaxation in
Gilletine moderate doses
Trigilletimine
O-Methylmoschatoline Oxoaporphine alkaloids
Tridictyophylline Morphinan alkaloid
Triclisia patens Oliv. Leaves Phaeanthine Bisbenzylisoquinoline Phaeanthine and dimethyl
A/jTV-Dimethylphaeanthine alkaloids (Guha derivative have muscle
Pycnamine etal.,\919) relaxing and curarizing
Cocsuline action strongly increased
Aromoline Oxoaporphine alkaloids in methiodide
O-Methylmoschatoline
Triclisia subcordata Oliv. Phaeanthine Bisbenzylisoquinoline Tetrandrine has antitumour
Tricordatine alkaloids action
Fancholine
Tetrandrine
Cocsuline
Tiliacora dinklagei Engl. syn. Roots Nortiliacorine A Bisbenzylisoquinoline Anaemia Curare action of dimethiodide
(Glossopholis dinklagei (Engl.) Funiferine alkaloids (Guha Oedema of legs of funiferine and
Stapf) Tiliacorinine etal., 1979) nortiliacorine
Tiliageine
Dinklacorine
Tiliacora funifera (Miers) Oliv. Roots Funiferine Bisbenzylisoquinoline Antitumour (leukaemia)

Nortiliacorine A alkaloids
Leaves Tiliafunimine
Isotetrandrine
Thalrugosine =
Nortiliacorine A
Epinetrum cordifolium Mangenot & Root

Root Isochondrodendrine Curare alkaloids Anaemia Curare action
Miege (in Ghana and Ivory Coast) Cycleanine = (Debray etal., Oedema of legs Muscular relaxation
Dimethyl-0, o-isochondro- 1967) Cycleanine also has anti-
dendrine inflammatory and analgesic
Norcycleanine properties
Monomethyl-o-isochondro-
dendrine
Cocculeae
Cocculuspendulus(J. & G. Forst.) Leaves Cocsuline Bisbenzylisoquinoline Biliousness Antitumour action
Dielssyn. (C. leaeba (Del.) DC., Stems Penduline alkaloids Inermittent
Epibateriumpendulum (J. &G. Forst.)) Roots Sangoline = Aporphine alkaloids fever Sympatholytic
Oxyacanthine
Palmatine Bitter principles Fruit; intoxicating Stimulants
Columbin drink
Roots Coccutrine Erythrinan alkaloids Curare alkaloids
Dihydroerysovine
(Table continued)
Part Local use

Plant used Constituents Chemical group of plant Pharmacology of constituents
Cissampelos owariensis Beauv ex Roots Chondrodendrine Bisbenzylisoquinoline Antipyretic Hyatin dimethiodide

DC. (C.pareira) Isochondrodendrine alkaloids Diuretic 2.5 times more potent
Cissampelos mucronata Rich. Bark Cycleanine Abortive than tubocurarine
(partly C.pareira) Hyatinine Emmenagogue
Hyatine
Dicentrine
Dehydrodicentrine
Leaves Cissampareine Cissampareine, anticancer
Cissamine
Stephania dinklagei (Enkl.) Diels syn. Roots Dinklageine Isoquinoline and Given to barren Narcotic antitussive
(Cissampelos dinklagei Engl.) Stepharagine aporphine alkaloids women in Antibiotic (TB and leprosy)
Cory dine menorrhagia
Norcorydine Anthelmintic From related species:
Steporphine Sedative rotundine, narcotic
Af-Methylcorydine and hypnotic in
Af-Methylglaucine Vietnam war
Stepharine Proaporphine alkaloids
Rhigiocarya racemifera Miers syn. Roots O-Methylflavinanthine Morphine-like alkaloid Sleeplessness Analgesic
(R. nervosa (Miers) Chev.) Liriodenine
Palmatine Leafy twigs, seeds;
Menispermine aphrodisiac
Magniflorine Proaporphine alkaloid
Kolobopetalum auriculatum Engl. syn. Roots O-Methylflavinanthine Morphine-like alkaloid Sleeplessness Analgesic
(K. veitchianum Diels)
Tinosporeae
Chasmanthera dependens Hochst. Root Berberine Berbens alkaloids Bark tonic juice: Bitter 'tonic', inhibits Leish-
InCh.palmata: Isoquinoline group sprains, bruises mania tropica in concentrations
Columbamine gonorrhoea ofl: 80000
Jateorhizine
Palmatine
Leaves Colombin Bitter principles
Palmarin
Chasmanthin
Jateorhiza macrantha (Hook.) Root Palmatine Berberis alkaloids Burns, snake bites Bitter 'tonic'
Excell. & Mendonga syn. Leaves Columbamine Hypotensive
(J. strigosa Miers) Jateorhizine
Root Colombin Bitter principles
Tinosporine
Tinospora bakis (Rich.) Miers Root Palmatine Berberis alkaloids Cholagogue Antipyretic
Tinosporine Remittant fever Bitter 'tonic'
Colombin Bitter principles Emmenagogue
Penianthus zenkeri (Engl.) Diels syn. Stems, Palmatine Protoberberine alkaloids Local infections See Duzh etal. (1981)
(Heptacyclum Engl.) roots Jateorhizine
Magnoflorine Aporphine alkaloids Venereal diseases
a
As can be seen from this table, the Menispermaceae produce not only curarizing bisbenzyl isoquinoline alkaloids (Guha et al., 1979) (mostly asymmetric), which
act on the neuromuscular junctions, but also some isoquinoline alkaloids with a morphine-like structure (bisbenzyl isoquinoline + phenanthrene) and aporphines
and oxoaporphines with narcotic or analgesic activity. In addition they contain alkaloids of the berberine group (berberine, palmatine, chasmanthine, jateorhizine,
columbamine) which have an isoquinoline nucleus and were called 'bitter principles'. The latter are mostly found in the Tinosporeae andfinduse as stimulants
because of their bitter taste.
62 63
Table 3.2. More important constituents and divergency of pharmacology of West African Rubiaceae species with an action on the nervous system"
Plant Part used Active constituents Pharmacological properties

Borreria verticillata Aerial parts Borrerine, borreverine (tetra-/3-carboline Antibacterial, stimulant on rat uterus
(L.)Mey. nucleus)
Root Emetine (0.13%)?
Bark Iridoids (chromogenic heterosides)
Cinchona spp. Bark Quinine, quinidine and derivatives Antipyretic, antiarrhythmic, protozoicidal
CoffeaarabicaL. Seed Caffeine (purine base) Stimulant
Corynanthe pachyceras Bark Corynanthine, corynantheine, Mild local anaesthetic, hypo tensive,
Schum. {Pseudo- corynanthidine, corynantheidine, sympatholytic, less toxic than yohimbine
cinchona africana etc.
Chev. exPerrot)
Crossopteryxfebrifuga Bark Crossoptine = rhynchophylline Antipyretic (?), local anaesthetic, protozoicidal
(Afz.exG.Don.)Benth. Leaves Glycoside, j6-quinovine Slight hypo tensive, oxytocic
Feretia apodanthera Del. Stem- and Iridoids: feretoside, gardenoside, Antineuralgic and CNS depressant
rootbark apodanthoside (Bailleulela/., 1979,1980)
Leptactina densiflora Bark and Harmine derivatives Antispasmodic to smooth muscles
Hook. f. leaves Leptactinine (Persinos and Quimby, 1967a)
Leptactina senegambica
Hook. f.
Mitragyna inermis (Willd.) Bark and Rhynchophylline, rotundifoline Hypotensive, local anaesthetic,
Ktze. leaves protozoicidal
Mitragyna stipulosa (DC.) Bark and Mitraphylline, glycoside: /J-quinovin Stimulates intestinal and uterine contractions
Ktze. leaves
Morinda lucida Benth. Rootbark Methylanthraquinones Hypotensive, diuretic, stimulates ileum
Morinda longiflora G. Don. Leaves Glycoside morindin contractions
Morinda gentinata DC.
Nauclea latifolia Sm. Rootbark Harmane derivatives, angustine, naucle- Antipyretic ('African quinine' or Rio Nunez
Nauclea diderrichii (de Leaves fine,etc.;glucoalkaloids:cadambine, quinine), antidepressant
Wild. &Dur.) Merrill dehydrocadambine
Nauclea pobeguinii (Pob. ex Root Alkaloid and saponoside Antipyretic, abdominal pains, oxytocic
Pellegr.) Petit
Pawridiantha viridiflora Bark Harmane derivatives, pauridianthine, Antidepressant, antipyretic, protozoicidal
(Schweinf. exHiern) pauridianthinine (pyridine-harmanes)
Hepper
Pausinystaliajohimbe Bark Yohimbine, mesoyohimbine, Hypotensive, aphrodisiac, local anaesthetic,
(K. Schum.) Pierre ex yohimbinine,etc. sympatholytic
Beille
Uncaria africana G. Don. Bark Harmane derivatives, rhynchophylline in Sedative, antispasmodic
syn. (Uncaria talbotii related U. rhynchophylla
Wernh. partly)
"The Rubiaceae, a big, mainly tropical family, have constituents which act mainly on the ANS and the thermoregulating centres. Their compo-
nents are quinolines, isoquinolines, purine bases and indole alkaloids including the harmala alkaloids. Many have antipyretic and protozoicidal
actions, and often an antispasmodic effect on the striated muscles. Some have a stimulating action on the ileum and uterus. Local anaesthetic action
is also frequent. Most of the harmala alkaloids have monoamine oxidase inhibiting (MAOI) properties and some have been used in sequels of
encephalitis.
64
I CNS stimulants
Some plants producing central stimulation, like those containing xanthine
derivatives, stimulate the CNS, but they are also cardiac and respiratory stimulants,
produce diuresis and relax the smooth muscles.
Caffeine is mostly used only as a CNS stimulant, while theobromine and
theophylline are used more often for their effects on the myocardium. These
methylxanthines, especially theophylline, are competitive inhibitors of phos-
phodiesterase (the enzyme that inactivates cyclic AMP). Higher concentrations of
cyclic AMP cause tissue glycolysis and may increase metabolic activity and this may
explain the stimulant action (Burgen and Mitchell, 1972).
The most important region of stimulation by the strychnos alkaloids is the
medulla. These alkaloids have an analeptic action, i.e. they are sometimes employed
to overcome depression of the CNS due to overdoses of barbiturates, morphine and
similar compounds by stimulating the centres in the medulla, but a sufficiently high
dose of these drugs can produce generalized convulsions. Their use in electro-con-
vulsive therapy has not proved successful and, owing to their toxicity, their
therapeutic value is, on the whole, negligible (Burgen and Mitchell, 1972).
Strychnine is used in investigations on the mode of action of convulsant drugs.
Hallucinogens have been classified as stimulants by Burgen and Mitchell (1972)
although their effects are certainly not always of a stimulating nature: they produce
a phase of stimulation of the muscles and mind. This is used in mental therapy as
conflicts are revealed, resistance is overcome and introspection and insight increase.
However, these effects can be accompanied by visual and/or other hallucinations and
may be followed by depression. The effect varies with the individuals and may cause
permanent psychological damage in some and there is the possibility of the
development of serious dependence.
(a) Analeptics and convulsants

The Cola spp. have, like coffee, tea or mate a stimulant action due to the
presence of xanthine derivatives (Burgen and Mitchell, 1972). Ocimum canum
contains camphor: the analeptic action of this compound on the heart and respiratory
system is well known. Xanthones are also found in Anthocleista vogelii (Loganiaceae).
Centella asiatica (Umbelliferae) is reported to improve the mental ability and
behaviour of mentally retarded children through glycosides of triterpenic acids. The
reputation of Strychnos spp. as 'bitter tonics' may be due to a bitter taste with
stimulation of the taste papillae and, as a reflex action, hypersecretion of saliva and
gastric juices. Strychnine also has a strong convulsant and analeptic action and small
doses can produce nervous and skeletal muscle stimulation but higher doses cause
tetanus-like convulsions leading to death, (from spasmodic contractions of the
thorax and diaphragm). The use of strychnine has now been limited mainly to
investigations on the mode of action of convulsant drugs (Burgen and Mitchell,
1972). However, most of the West African Strychnos spp. also contain muscle
relaxant alkaloids (see below). Convulsant and sedative action is also noted in
Afrormosia laxiflora (Fabaceae). The plant is, however, very toxic.
65
Cola acuminata (Beauv.) Schott & Endl. syn. (Sterculia acuminata Beauv. & Oware,
C. pseudoacuminata Engl.) (Fig. 3.1) STERCULIACEAE
Cola nitida (Vent.) Schott & Endl. syn. (C. acuminata var. latifolia Schum.,
Sterculia nitida Vent. Jard. Malm., C. acuminata Engl.)
Kola nut trees
The trees begin to bear nuts when 5-6 years old and bear fully after about 10 years
(average annual yield is about 60 kg per tree). The nuts are used as a masticatory and
stimulant (Dalziel, 1937).
Kola nuts contain purines, about 2.5% caffeine, 0.023% theobromine, 1.618%
tannins and a considerable amount of fructose. The caffeine content is about the
same in the red and the white seeds. In addition the nuts contain two phenolic
substances kolatin and kolatein, catechols, (—)-epicatechol and kolanin, the latter
mainly in young nuts. Kola red is an anthocyanin pigment, phlobaphen, which
occurs through oxidation of the catechols (Michl and Haberler, 1954; Dublin,
1965); Goodman and Gilman, 1976, p. 359).
Fig. 3.1. Cola acuminata (Beauv.) Schott & Endl.

66
Caffeine excites the CNS at several levels and is a mental, skeletal muscle, respiratory
and cardiac stimulant. Theophylline and theobromine have similar action but are
more diuretic than caffeine. Because of the presence of catechols the action of kola is
more moderate and it also relaxes smooth muscle (Burgen and Mitchell, 1972,
pp. 41, 42). In high doses kola can nevertheless be dangerous: it can produce
over-excitement followed by depression as it conceals normal tiredness; smaller
doses produce a passing exciting action on the nervous system and increase the blood
pressure and the strength of the heartbeat. The seeds are exported to be used in the
preparation of soft drinks and medicinally for their stimulating and sustaining effect
in sport and intellectual work. For export the nuts are merely dried and put into
strong bags (Russel, 1955).
Ocimum canum Sims syn. (O. americanum L., O. hispidulum Schum. & Thonn.,
O. thymoides Bak.) LABIATAE
Hoary or American basil
The leaves are used in most areas of West Africa as an infusion in the treatment of
fevers and dysentery and also to relieve toothache. The leaves are strongly flavoured
and find use in flavouring and to repel mosquitos. In Guinea the leaves cooked with
groundnuts are given before parturition and as an emmenagogue.
The composition of the essential oil varies according to its origin. In East Africa the
oil contains 16-25% camphor (Beckeley, 1936) whilst in Central Africa methyl-
cinnamate predominates in the oil (Schimmel et al.91914); further citral and smaller
amounts of other essential oils have been reported (Paris and Moyse, 1971). During
the flowering period the amount of essential oil decreases in the leaves and increases
in the flowers, these proportions are inversed in the fruiting period (Kerharo and
Adam, 1974).
Camphor is an excellent cardiac and respiratory analeptic and is also a general
stimulant. The essential oil is antiseptic (Nickel, 1959) and is used as a pulmonary
antiseptic and expectorant. It has been recommended as a mild analgesic and
rubefacient for rheumatism and for pains in external use (Dalziel, 1937).
According to the Flora of West Tropical Africa (F.W.T.A.) the essential oil of O.
basilicum (botanically similar to O. canum) can contain up to 75% of estragol
(methylchavicol) and has sedative and antispasmodic effects (Kerharo and Adam,
1974).
Ocimum gratissimum L. (O. viride Willd., O. guineense Schum. & Thonn.)

LABIATAE
Tea bush
O. gratissimum is locally a familiar febrifuge and diaphoretic and is also regarded as
a stomachic and laxative (Dalziel, 1937).
The essential oil obtained from the plant differs entirely from that of O. canum. It
contains mainly thymol (32-65%) and eugenol.
The oil is used externally to keep mosquitos away but negative results have been
reported. Thymol is antiseptic, antitussive and antispasmodic (Paris and Moyse,
1971, p. 282).
67
Anthocleista vogelii Planch, syn. (A. kalbreyeri Bak., A. talbotti Wern.)

LOGANIACEAE
The seeds and bark are used in Nigeria for their antipyretic, tonic and purgative
action (Dalziel, 1937).
Three tetraoxygenated xanthones (l-hydroxy-3,7,8-trimethoxyxanthone, 1,7-
dihydroxy-3,8-dimethoxyxanthone and swertioside) have been isolated from the
leaves of A. vogelii collected in Zaire (Chapelle, 1974).
The medicinal properties attributed to the plant are believed to be due to the
synergistic activity of the xanthones (reported to have MAOI action by Suzuki et al.
(1981), tetraoxygenated xanthones (which have anticonvulsant properties) and
seco-iridoids (which are stimulants and stomachics) (Ghosal et al., 1973; Chapelle,
1974).
Centella asiatica (L.) urb. Hydrocotyle asiatica L. UMBELLIFERAE

Indian pennywort
An infusion of leaves and stems has been used in India for the treatment of leprosy
and other skin diseases, and as a diuretic (Indian Pharmaceutical Codex). Large
doses are said to have a narcotic effect.
Asiaticoside, a glycoside of a genin composed of a pentacyclic triterpenic acid, was
isolated from the Madagascar plant by Bontemps (1942). Bhattacharya and Lythgoe
(1949) found no asiaticoside in the Sri Lankan plant, but reported the presence of a
related compound, centelloside, and the triterpenic acids centoic and centellic acid
(Boiteau et al., 1949; Boiteau and Ratsimamanga, 1956; Oliver, 1960). Appa Rao et
al. (1969) found in Indian plants two free terpenic acids, brahmic and isobrahmic
acid, two saponins, brahmoside and brahminoside (tri- and tetraglycosides of
brahmic acid) and also betulic acid and stigmasterol. The saponins were found to be
different from asiaticoside found in the Madagascar plants. Dutta and Basu (1967)
had isolated and identified asiatic acid in an Indian variety of Centella asiatica and the
presence of asiaticoside, meso-inositol and oligosaccharide of centellose in this
variety has also been reported. Finally, it has been shown that, depending on the
habitat, the saponins can be of two types, the more common one containing
asiaticoside and medacanoside, and the less common one showing the additional
presence of arabinose in the saponins, thus forming brahmoside and brahminoside.
Sapogenins and flavonoids were the same in both varieties (Rao and Seshadri, 1969).
Asiaticoside had been found to be active in the treatment of leprosy (by dissolving
the waxy coating of Mycobacterium leprae whilst an oxidized form, oxyasiaticoside,
inhibited the growth of tubercle bacillus in vitro and in vivo (Boiteau et al., 1949). In
clinical trials, Appa Roa et al. (1969, 1973) studied the effect of the plant on the
general mental ability of mentally retarded children and its anabolic effect on normal
healthy adults. They found that in 30 mentally retarded children (free from epilepsy
and other neurological conditions) a significant improvement in both general ability
and behavioural pattern was obtained when the drug was administered for a period
of 12 weeks. In 43 normal adults the mean levels of blood sugar, serum cholesterol,
total protein and vital capacity were increased by the drug and the mean levels of
blood urea and serum acid phosphatase were decreased (Appa Rao et al., 1973).
68
Strychnos alkaloids. These are known to be analeptic and convulsant and are
medullary stimulants. As analeptics they were used to overcome depressions due to
overdoses of barbiturates or morphine, but this is now mostly abandoned because of
their high toxicity. They act on the spinal cord by antagonizing or blocking
postsynaptic inhibitions. Brucine has a similar action to strychnine but is fifty times
less toxic. Picrotoxin, obtained from the Indian Anamirta paniculata, is a medullary
stimulant in small doses and is used in preference to strychnine to counteract
barbiturate and bromide poisoning. The West African Dioscorea dumetorum (Dio-
scoreaceae) has a picrotoxin-like convulsive action on the medulla.
Strychnos spp. LOGANIACEAE

L The local uses of the Strychnos spp. vary greatly. Some, like S. usambarensis,
S. camptoneura, S. splendens and 5". angolensis, seem not to be used in local medicine.
The seeds of S. densiflora were used in trial by ordeal and the fruits of S. aculeata as
a fish poison (Dalziel, 1937). The alkaloids of the latter species were studied by
Mirandaal. (1979).
C Among the West African Strychnos spp. only a few were found to contain small
quantities of alkaloids with convulsant effects, whereas muscle relaxing alkaloids
seem to be present in more West African spp.
The first isolation of a convulsive alkaloid from African Strychnos spp. was
achieved by continual pharmacological screening for convulsive and muscle relaxant
effects in the East African S. icaja Baill. (Sandberg et al., 1969a, b). This led also to
the detection of 4-hydroxystrychnine in that species. From the rootbark of 5 .
aculeata Sol., Sandberg et al. (1969b) isolated strychnofendlerine and N-
acetylstrychnosplendine as well as traces of brucine. The muscle-relaxing effects
seem to be limited to extracts of the seeds and the pericarp of the fruit and was later
considered to be weak.
As a result of further screening, new tertiary indole alkaloids with a pronounced
muscle-relaxant effect but producing clonic convulsions in high doses were found in
other species (Sandberg and Kristianson, 1970; Sandberg et al., 1971; Verpoorte
and Bohlin, 1976; Rolfsen and Bohlin, 1978).
In 1975 Bouquet and Fournet (1975b) reported that the only African Strychnos
spp. with over 0.5% of total alkaloids were S. camptoneura Gilg & Busse, S. splendens
Gilg, 5. angolensis Gilg and 5. usambarensis Gilg.
P Verpoorte and Bohlin (1976) screened 11 African Strychnos species for muscle
relaxant and convulsant effects. They reported strong muscle relaxant effects in
S. usambarensis, »S. afzelli Gilg, S. barteri Sol. and 5. longicaudata Gilg whilst in S.
aculeata Sol., S. malacoclados Wright and S. spinosa only a weak effect was noted.
Further details are given on five of the very many West African Strychnos spp.
Strychnos camptoneura Gilg & Busse syn. (Scyphostrychnos talbotti Moore, 5". psit-
taconyx Du vign.) LOGANIACEAE
C Sandberg et al. (1971), in studying the muscle relaxant properties of stem- and
rootbark collected in the Cameroons, found 11 alkaloids, the main ones being
69
serpentine and alstonine. Koch et al. (1972) and Garnier et al. (1974) found five new
alkaloids in the bark of specimens from the Ivory Coast; these were identified as
retuline, camptine, camptoneurine, camptinine and Af-oxyretuline.
Verpoorte and Sandberg (1971) reported muscle relaxant activity in the stem- and
rootbark of S. camptoneura Gilg & Busse.
Strychnos usambarensis Gilg syn. (S. micans Moore, 5. cooperi Hutch. & Moss)
LOGANIACEAE
Oxindole and bis-indole alkaloids have been reported in S. usambarensis. Alkaloids
of this type were formerly known in certain species of Rubiaceae and Apocynaceae
but their presence has now been detected in Loganiaceae. The alkaloids found in the
bark and leaves of S. usambarensis in the Congo have been identified as harmine,
strychnofoline, 2-isostrychnofoline, strychnophylline and isostrychnophylline. In
addition, the presence of 18,19-dihydro-usambarine, usambaridine and their
dihydro-derivatives strychnobaridine, strychnopentamine and isomers has been
reported (Angenot, 1978; Angenot etal., 1970,1973,1975,1978a, b). Usambarine,
usambaridine and strychnambarine have been isolated from the leaves, the two
former are indole alkaloids biogenetically derived from two tryptamines and one
monoterpene (Koch et al.,1973).
The indole alkaloids showed both convulsant and curarizing muscle relaxant activity
(Angenot era/., 1970,1975).
Strychnos dolichothyrsa (Gilg) Onochi & Hepper LOGANIACEAE

In the stembark of this climber, the following alkaloids were found: bisnordihydro-
toxiferine, bis-nor-C-curarine, bis-nordihydrotoxiferine-Af-oxide, and
bis-nordihydrotoxiferine-di-Af-oxide (Verpoorte and Svendsen, 1976; Verpoorte,
1980, 1981). In the stems and leaves only traces of alkaloids were found (Bouquet,
1970).
From the stembark of Strychnos decussata, a tertiary alkaloid has been isolated
which has a pronounced muscle relaxant activity both in vivo and m vitro. The
blockade effect of this alkaloid, decussine, is not antagonized by synstigamine
(Bisset and Phillipson, 1970, 1973; Olaniji and Rolfsen, 1980; Rolfsen et al.,
1980a, b).
Strychnos spinosa Lam. syn. (S. lokua A. Rich.,S. laxa Solered.,S buettneriGilg,
5. spinosa var pubescens Bak., 5. djalonensis Chev.) LOGANIACEAE
Locally this species is used mainly in colitis, entero-colitis and diarrhoea (roots and
bark); the root powder is sold in the markets in Senegal as a stomachic (Oguakwa et
al., 1980).
Lofgren and Kinsley (1942) found no alkaloids in the seeds, stems and leaves and the
different parts of the plant were found to be non-toxic to mice and guinea pigs. More
recently, Mathis and Duquenois (1963) found, by using two-dimensional thin-layer
chromatography, 0.009% of alkaloids in the pericarp and 0.012% in the fruit plus
seed. In 1980, Oguakwa et al. reported the presence of akagerine and 10-hydro-
70
xyakagerine in the leaves. Akagerine had already been reported in S. panamensis

(Marini Bettolo et al., 1970).
P The toxicity of the plant appears to be very low. Verpoorte and Bohlin (1976) report
only weak muscle relaxant effect.
Strychnos dinklagei Gilg LOGANIACEAE

L The plant, which is found in Liberia, Ghana, Guinea and the Ivory Coast, is used in
local medicine in the treatment of diseases of the mouth, the kidneys and the heart
(Oguakwaefa/., 1980).
C Traces of alkaloids have been found in the leaves but they are more abundant in the
bark. In the stembark, ellipticine has been found as the main alkaloid. It is the first
time that a non-corynane, strychnine-type of alkaloid has been isolated from a
Strychnos sp. (Michel et al., 1980). Akagerine and derivatives were also found in S.
dinklagei (Oguakwa et al., 1980).
P Ellipticine had been shown to have slight convulsive properties (Sandberg et al.,
1971; Verpoorte and Svendsen, 1976). Fractionation led to the discovery of five
alkaloids with a convulsive action. In addition to the already known akagerine, four
new indole alkaloids were isolated including O-methylakagerine, which produced
strychnine-like convulsions but which is less potent than akagerine (Verpoorte and
Bohlin, 1976; Oguakwa^ al., 1980).
Dioscorea dumetorum (Kunth) Pax. syn. (Helmia dumetorum Kunth, Dioscorea

buchholziana Engl.) DIOSCOREACEAE
Bitter yam or cluster yam
L The tuber is used as a food only in cases of scarcity and requires to be sliced and
steeped long before use to eliminate the poisonous alkaloid dioscorine, which
produces CNS paralysis. It is said to have caused death when eaten during famine in
the Sudan. In Senegal, the tuber is sometimes used externally as a rubefacient.
C The dried tubers contain, besides dioscin, the genin of which is diosgenin, small
quantities of other steroid sapogenins and a convulsant alkaloid, dihydrodioscorine
(Bevan et al., 1956; Bevan and Hirst, 1958). Nigerian yams also contain 83.3% of
glucides and 9.9% of proteins. Diosgenin has been much used as a starting
compound in the synthesis of hormones, corticosteroids, etc. (Oliver-Bever, 1972).
P The LD 50 in mice of a water-soluble extract of the tubers from the Congo (containing
6.2% of dihydrodioscorine) is 15.5 mg/20 g, and the convulsant dose ED 50 is
12.5 mg/20 g. In the cat, the extract produces a long-lasting hypotension when
injected intravenously in doses of 100 mg/kg. The total extract produces a contrac-
tion of the smooth muscle fibres of the intestine both in vivo and in vitro (Bevan et
al., 1956). In small doses (30 mg/kg) in the cat or monkey, Schlag et al. (1959) have
noted a desynchronization of the cortical electrical record lasting over 0.5 h. With
higher doses (200 mg/kg) there are progessive convulsive impulses preceded each
time by an increase in the arterial pressure and of the intestinal peristalsis which,
according to the authors, indicates an excitant action of the drug on the cerebral
cortex. In mice the LD 50 of dioscorine is 65 mg/kg. Dioscorine produces first clonk
then tonic convulsions and in concentrations of 10~5 M it reduces the response to
71
acetylcholine of the isolated intestine of the cat and of the duodenum of the rabbit
(Bevan et al., 1956). Dioscin is less toxic; the LD 5 0 is 100 mg/kg in mice. It has a
picrotoxin-like convulsive action and the effect on the blood pressure of the cat and
on the isolated ileum of the guinea pig is distinct although less pronounced than that
of dioscorine (Broadbent and Schnieden, 1958; Correia da Silva et al.> 1962).
Afrormosia laxiflora (Benth. ex Bak.) Harms syn. {Ormosia laxiflora Benth. ex

Bak.) FABACEAE
False Dalbergia
The local medicinal uses of the leaves, bark and roots ofAfrormosia are based on their
analgesic and antipyretic actions. The root is said to increase the intoxicating effect
of palm wine, and to be slightly intoxicating if taken by itself. The plant was formerly
used in arrow poisons and as an ingredient in a complex prescription taken to impart
strength or stimulus 'when undertaking a journey or other enterprise' (Dalziel,
1937).
The stembark of the Nigerian plant contains 6.7% of total bases including six
alkaloids. The three main alkaloids are non-quaternary; the main constituent of
these is Af-methylcytisine (a quinolizidine derivative), a second is probably
ammodendrine. Three minor alkaloids are also non-quaternary and a quaternary
fraction is almost entirely composed of choline (Bevan and Ogun, 1964). In the
heartwood of the related A. elata, afrormosine (a dimethoxyhydroxyflavone) has
been reported, and in the bark catechuic tannins (Caiment-Leblond, 1957). The
related Ormosia dasycarpa Jacks, and O. coccinea Jacks, contain two alkaloids,
ormosine and ormosinine, which have a physiological action smaller than that of
morphine (Caiment-Leblond, 1957).
Af-Methylcytisine is very toxic to mice, which can only tolerate a dose of 1 mg,
producing long-lasting sedation. Higher doses (4 mg) produce severe ataxia and
convulsions followed by death within 5 min. In anaesthetized rabbits doses of 2 mg
produce a prolonged increase in blood pressure (Raymond-Hamet, 1954; Bevan and
Ogun, 1964). The constituent appears to have a cytisine-like action, paralysing the
ganglia after a short stimulation.
Tinctures of the rootbark and the isolated total alkaloids show a distinct hyperten-
sive action when injected intravenously to the chloralosed dog (Kerharo and
Bouquet, 1950; Caiment-Leblond, 1957). Tests on cytotoxicity were negative but a
certain insecticidal effect was observed and the toxicity for mice (10 g/kg killed 40%)
is high. The extracts are much less toxic to daphnia and fish (Kerharo and Bouquet,
1950).
For those plants with a stimulant action on the CNS already described in Chapter
2 see Table 3.3
(b) Antidepressants and hallucinogens

The drugs with these properties have been treated by Burgen and Mitchell
(1972) under CNS stimulants. It should, however, be stressed that antidepressant
and MAOI action is usually related to anticholinergic activity and it is not possible
Table 3.3. Plants with stimulant action on the nervous system which are described in Chapter 2
Plant Family Active constituent Part(s) used Action on nervous system References
Achyranthes aspera Achyran thine Seeds Respiratory analeptic CNS. Chapter 2 and Massion
Amaranthaceae (1934)
Holarrhenafloribunda Triacan thine Respiratory analeptic CNS. Chapter 2 and
Apocynaceae Quevauviller and Blanpin
(1961)
Mostua hirsuta Alkaloid closely related Roots Convulsant, sedative and CNS. Chapter 2 and Chevalier
Loganiaceae to sempervirine analgesic (1947)
Erythrophleum Cassaine Bark, seeds Convulsant, medulla Chapter 2
guineense stimulant, treatment of
Fabaceae dental and facial
neuralgia
Physostigma venenosum Physostigmine Seeds Stimulant in myasthenia Inhibits cholinesterase, see
Fabaceae gravis Chapter 2
73
to make a rigorous distinction between ANS and CNS activities. However, a number
of these drugs may prove useful in the treatment of certain forms of mental illness.
Unfortunately, these effects can be accompanied by secondary effects, by visual or
other hallucinations, and may be followed by depression.
Securinine and phyllochrysine, alkaloids found in Securinega virosa and
Phyllanthus discoideus (Euphorbiaceae), are mainly muscular stimulants which have
been shown to be successful in re-establishing mobility in cases of paralysis and
paresis and in mental patients. Indole alkylamines and MAOIs (/3-carbolines) have
been reported in Pauridiantha viridiflora and other Rubiaceae which also act on the
ANS, e.g. Nauclea diderichii and N. latifolia and Borreria verticillata. All of these
plants have been found to have a stimulant effect in post-encephalitic conditions.
Antidepressant action is also attributed to Justicia insularis (Acanthaceae).
Stimulating to the CNS in small doses but narcotic and hallucinogenic in large
doses are Tabernaemontana crassa, through ibogaine; Cannabis sativa, through
tetrahydrocannabinols and Myristica fragrans, through myristicin (also a MAOI).
Datura metel and Datura spp. containing hyoscyamine and hyoscine are sedative in
psychomotor agitation like the other hallucinogens, and the alkaloids are used as
pre-anaesthetics. They mainly act, however, via the ANS (anticholinergic with
blockade of muscarinic receptors).
Securinega virosa (Roxb. ex Willd.) Baill. syn. (Phyllanthus virosus (Roxb. ex

Willd.), Fluggea microcarpa Blume, S. microcarpa (Blume) Pax & Hoffm. ex
Aubrev., F. virosa (Roxb. ex. Willd.) Baill.) EUPHORBIACEAE
5. virosa is widely used in Senegalese local medicine. A decoction of the roots is given
mainly for disorders of the liver, the gallbladder, the kidneys (including stones), the
bladder and the genitals. It is also recommended in many tribes to Bilharzia patients
(Kerharo and Adam, 1974). The Hakims in India use S. virosa as a cure for diabetes
mellitus (Watt and Breyer-Brandwijk, 1962).
Numerous alkaloids have been isolated from the leaves, rootbark and stembark of
this and closely related species. Paris et al. (1955) isolated a crystalline alkaloid which
they called fluggeine, together with choline. Fluggeine was later identified as
hordenine by Iketubosin and Mathieson (1963), who also isolated norsecurinine
from the Nigerian plants. Securinine, first isolated from S. suffruticosa in 1956 by
Muraveva and Bankovski, was later also found in S. virosa. In addition, norse-
curinine (1.6%), dihydrosecurinine (0.06%) and virosecurinine (1.14%) were iso-
lated from the rootbark, viroallosecurinine from the leaves and virosine (di-
hydrosecurinine) from the roots (Kjaer and Friis, 1962). Considerable differences
have been observed in the alkaloid content of the male and female plants, and in the
different parts of the plants (Chatterjee and Bhattacharya, 1964; Saito etal., 1964a,
b; Satoda et al., 1972). The presence of thioglycosides has been reported in several
botanically allied species, e.g. in the Indian Putranjeva roxburghii Wall.,
glucocochlearin, glucoputranjevin and glucojeaputin were found, and later, glucoil-
comin (Kjaer and Friis, 1962). The same glycosides ofS. virosa have been found in
the fresh leaves, stems and roots and some may also exist in other Securinega spp. as
74
the hypoglycaemic action appears to be related to the presence of thioglycosides

(Chatterjee and Roy, 1965; Oliver-Bever and Zahnd, 1979). inS. virosa leaves rutin
has also been reported.
Securinine was found to have an action similar to strychnine (Quevauviller et al.,
1967). In pharmacological and clinical trials, Tourova (1957) noted that the alkaloid
stimulates the CNS, including the spinal cord. In clinical trials with the nitrate (200
cases), Tourova (1957) observed that a rapid re-establishment of motility was
produced, and hence it seems indicated in paresis, paralysis in poliomyelitis and
diphtheria, and in apoplectic paresis and paralysis. The use of securinine is also
indicated for impotence, decrease of cardiac activity, functional amaurosis, asthenia
consecutive to extenuating diseases and ocular nerve atrophy. The drug was
administered either by mouth (10-20 drops daily of a 1:250 solution of securinine
nitrate) or subcutaneously (1 ml of a 1:500 solution daily). With these doses, no
secondary effects have been noticed but overdosage produces a painful tension in the
nape of the neck, face muscles and other muscle groups. In China securinine is used
in the treatment of facial paralysis and of neurasthenia (Xiao, 1983). It has also
shown promising results in the treatment of multiple sclerosis in man (Chang, 1974).
Chang compares it with strychnine with regard to toxicity and pharmacological
activity and reports that although both are powerful stimulants of the CNS, the LD 5 0
of securinine in rats following intravenous administration is 26-fold higher than that
of strychnine (Chang, 1974).
Phyllanthus discoideus (Baill.) Mull. Arg. syn. (P. discoides Mull. Arg., Cicca
discoidea Baill., Fluggea klaineana Pierre ex. Chev., F. obovata var. luxurians Beille)
EUPHORBIACEAE
An extract of the bark of this small tree is used as a purgative and antipyretic and
topically in ophthalmias (Oliver, 1960).
From the rootbark the alkaloids phyllalbine, securinine, phyllochrysine (allo-
securinine), phyllanthine (methoxysecurinine) and phyllanthidine have been iso-
lated (Janot et al., 1958; Parello et al, 1963; Parello, 1966; Foussard Blanpin et al.,
1967). Earlier, securinine had been found in Securinega suffruticosa by Muraveva and
Bankovski (1956). Bevan etal. (1964) have reported in Nigerian species 0.4%, 0.2%
and 0.06% of securinine in the rootbark, stembark and leaves, respectively, as well
as the minor alkaloid allosecurinine. The phyllanthine formerly reported has been
shown to be identical with methoxy securinine.
Securinine was shown by Tourova (1957) to have a stimulating action on the CNS
comparable to that of strychnine. It increases reflex activity and breathing as well as
muscular tone and the blood pressure. It was used by Tourova (1957) in various
neuropsychic complaints with satisfactory results (see Securinega virosa). It has been
reported to be ten times less toxic than strychnine. The action of phyllochrysine,
securinine and phyllalbine have also been investigated in France. Phyllochrysine
and securinine are sympathomimetic and excite the CNS. Securinine, however, is
more toxic, does not act on the medulla and produces more violent convulsions
(Quevauviller et al., 1965). Phyllochrysine does not have local anaesthetic, analgesic
or antispasmodic activity. Phyllalbine chloride has a LD 5 0 in mice of 10 mg/kg when
75
given intravenously and of 45 mg/kg when given subcutaneously. It mainly stimu-

lates the suprarenal glands, producing secretion of adrenaline, has peripheral
sympathomimetic properties and slightly inhibits monoamine oxidase (MAO)
(Quevauviller and Blanpin, 1959; Quevauviller etal., 1965, 1967).
Pauridiantha viridiflora (Schweinf. ex Hiern) Hepper syn. (Urophyllum viridiflorum

Schweinf. ex Hiern) RUBIACEAE
The bark of a related species, P . lyallii (not found in West Africa), has long been used
as a remedy for fever and malaria (Pousset et al., 1974).
From the bark of P . viridiflora growing in the Congo, the following have been
isolated: harmane (0.08%); pauridianthine (0.007%) and its isomer pauridianthinine
(of pyridine-harmane structure), as well as an anthraquinone and a glycoside,
lyaloside (Pousset et al., 1971; Bouquet and Fournet, 1975a; Leveque et al., 1975).
P. canthiflora Hook., another species found in West Africa, has been shown to
contain only traces of alkaloids (Bouquet, 1970). Harmane and related alkaloids
(j8-carbolines) have been found in several other African species (P. lyallii, P.
callicarpoides) (Pousset et al., 1971, 1974). Harmine and related alkaloids were first
detected in Peganum harmala L. (Rutaceae) from India (Henry, 1949). Harmane is
l-methyl-9//-pyrido-3,4,6-indole and harmine is its 7-methoxy derivative. The
configuration of these alkaloids shows a close relationship with that of serotonin
(5-hydroxytryptamine) and tryptamine.
The antipyretic and protozoicidal actions of P. lyallii have been confirmed by
Pousset et al. (1974) and the chemical composition of P . viridiflora could justify the
same activities. Harmane and its derivatives have similar properties to quinine
alkaloids. They are also protozoicidal and are also said to be coronary dilators and
oxytocics.
The harmala alkaloids are able to elicit or exacerbate abnormal reactions such as
are shown in schizophrenia or in ethanol intoxication and some of their effects are
reminiscent of productive symptoms in these cases (Hofer et al., 1950). Thus an
isomer of harmaline (6-methoxyharmalane) is a powerful serotonin antagonist, and
it is suggestive that the highest concentrations of serotonin have been found in the
pineal glands of schizophrenics (Mclsaac et al., 1961; Wooley, 1962; Naranjo,
1967). MAO-active alkaloids can alter 5-hydroxytryptamine and noradrenaline
metabolism in the brain, producing enhancement of the serotonin effect on body
temperature and counteraction to reserpine (Pletscher et al., 1959).
The harmala alkaloids have been used in sequels of encephalitis (Hill and
Worster-Drought, 1929; Cooper and Gun, 1931; Naranjo, 1967). In large doses they
cause tremors and clonic convulsions. Harmine, harmaline and harmol are MAOIs
(Burger and Nara, 1965; Slotkin et al., 1970); harmine and harmaline show a short
duration of MAO inhibition as compared to the early MAOIs (hydrazine deriva-
tives). Pretreatment with harmaline can therefore reduce undesired secondary
effects of these in blocking the MAO molecule receptors (Rommelspacher, 1981).
The harmala alkaloids are cholinergic and antagonistic to benzodiazepines (which
are anxiolytic, anticonvulsive, muscle-relaxing and sleep-inducing). They are a
group of substances with a broad spectrum of activity differing from compound to
76
compound and require further research (Holmstedt, 1967; Rommelspacher, 1981).

The LD 50 of harmaline given subcutaneously, is 120 mg/kg for rats and mice; that of
harmine is 200 mg/kg. The human therapeutic dose of harmine, given perorally, is
300-400 mg (Usdin and Efron, 1976).
Nauclea latifolia Sm. syn. (N. esculenta (Afz. ex Sab.) Merrill, Sarcocephalus
esculentis Afz. ex. Sab., S. sassandrae Chev., S. sambucinus Schum., S. russeggeri
Kotschy ex Schweinf.) RUBIACEAE
African peach, guinea peach, doundake
In Nigerian local medicine, the fruit is sometimes dried and used in the treatment of
piles and dysentery. Eaten in excess the fruit acts as an emetic. The bitter bark has
been widely used locally, in the form of an infusion or decoction, as a tonic and
antipyretic. It is called' African quinine'. In Northern Nigeria, a cold infusion of the
bark is taken as a diuretic and anthelmintic, and to regularize bowel functions. The
stembark has been used as a haemostatic, N. latifolia is also a timber tree and
frequent intoxication (headaches and nausea) of the workmen cutting up the trees
may be attributed to an alkaloid, found in the leaves, which has a marked and
cumulative cardio-inhibiting action (Caiment-Leblond, 1957). The root of N.
pobeguinii is prescribed in local medicine in Senegal as a powder for abdominal pains
and as an oxytocic in the form of a decoction (Kerharo and Adam, 1974).
Different indolo-quinolizidine alkaloids and glyco-alkaloids have been isolated from
the rootbark. The former have been identified and named angustine, angustoline,
angustifoline, nauclefine and naucletine (Dimitrienko et al.9 1974; Hotellier et al.,
1975). The glyco-alkaloids have been identified as cadambine and 3-a-dihydro-
cadambine. These two alkaloids have also been reported to be present in the leaves
of N. diderrichii (de Wild. & Dur.) Merrill in Senegal (McLean and Murray, 1970).
Patel and Rowson (1964) noted the presence of heterosides in the rootbark of N.
latifolia and Hotellier et al. (1977) isolated a precursor from it called strictosamide,
which is closely related to vincoside lactam. The simultaneous presence of indolo-
quinolizidine alkaloids and of corresponding heterosides seems to indicate a biogene-
tic relationship in this family of Rubiaceae; similar observations had already been
made concerning N. diderrichii and Pauridiantha leyallii Brem. (Leveque et al.,
1975). The leaves of N. latifolia yield 0.8% of alkaloids, including naufoline and
angustine, and the same two glyco-alkaloids which had been reported in the rootbark
(Hotellier et al., 1979). Harmane, pyridine and indole-pyridine alkaloids have been
isolated from N. diderrichii (de Wild. & Dur.) Merrill, which is also found in West
Africa (McLean and Murray, 1970).
In the guinea pig an intraperitoneal injection of an aqueous extract of the leaves and
bark of N. latifolia collected in Nigeria equivalent to 6 g/kg produced a lowering of
the rectal temperature of 2°C, which lasted for several hours, and in dogs an aqueous
extract of the leaves was reported to have distinct hypothermic action and to produce
a sudden decrease of the carotid pressure followed by the opposite effect and by renal
vasoconstriction (Raymond-Hamet, 1937). A non-identified (possibly indolic)
alkaloid isolated from the roots in Portuguese Guinea by Almeida et al. (1963)
77
produced an inhibiting effect on smooth muscles and was anticholinergic (Correia da

Silvan al. ,1964).
Cardio-inhibiting and cardiotonic activity of extracts of the leaves and bark were
reported by Patel and Rowson (1964). The leaves of N. latifolia have anticancer
action against transplantable sarcoma 180 tumours and against Lewis lung car-
cinoma, producing a reduction of 43% and 53% respectively (Abbott ex al., 1966).
Justicia insularis Anders syn. (Adhatoda diffusa Benth., J. galeopsis Anders,

Siphonoglossa macleodiae Moore) ACANTHACEAE
The plant does not seem to be used medicinally in West Africa. In the Kumaon
region (India), it is used as an antifatigue and stimulating plant (Ghosal et al., 1979a,
1981).
In India and Japan a number of Justicia spp. have been screened as they produce a
large number of aryl-naphthalide lignans with antidepressant properties. Thus,
J. prostata has been shown to contain the prostalidins A, B, C and tetrochinensin
(4-aryl-2,3-naphthalidine lignan). In J. hayatai var. decumbens and J. procumbens
var. leucantha (from Formosa and Japan) a number of aryl-naphthalide lignans
(sesamin, asarin, sesamolin) and in J. simplex a new lignan, simplexolin, have been
recorded (Ghosal etal, 1979a, b, 1981).
Pharmacological screening of these lignans revealed significant action on the CNS in
animals. The prostalidins A-C produced a mild antidepressant action in albino mice
and rats. The action was potentiated by carpacin, which itself showed only a weak
sedative action. The combined active constituents have a low toxicity (Ghosal et al.,
1979b). Another biological activity reported for bicyclo-octane lignans is the reversal
of sickling and crenation in erythrocytes by plant extracts containing similar
constituents (Sofowora et al., 1975).
Tabernaemontana crassa Benth. syn. (7\ durissima Stapf, Conophatyngia durissima

(Stapf) Stapf) APOCYNACEAE
Tabernaemontana pachysiphon Stapf var. pachysiphon syn. (Conopharyngia
pachysiphon (Stapf) Stapf)
A decoction of the leaves of T. crassa is taken in West Africa as a tonic, appetizer and
aphrodisiac whilst the juice of the bark is used in the treatment of leprosy and for
wound disinfection (Kerharo and Bouquet, 1950).
In Nigeria and Ghana, the rootbark of T. pachysiphon is used as an infusion in the
treatment of manias (Ainslie, 1937;Irvine, 1961;Watt, 1967). The rootbark of some
species is said to be strongly sedative (Watt, 1967).
In the roots and bark of T. crassa, indole alkaloids, isovoacangine, conopharyngine,
conodurine, conoduramine and coronaridine, and in the seeds, voacamidine,
coronaridine-hydroxyindolenine, tabersonine and coronaridine have been reported
(Dass et al., 1967). Although coronaridine is closely related to ibogaine (Gorman et
al., 1960), the narcotic alkaloids found in T. iboga, such as ibogaine, ibogamine and
tabernanthine (Tyler, 1966; Pope, 1969), could not be detected in T. pachysiphon or
T. crassa (Taylor, 1957; Dickel et al., 1958). By thin-layer chromatography, Patel et
78
al. (1967) could detect in the bark of Nigerian T. pachysiphon c. (cultivated)

coronaridine, conopharyngine and voacangine plus small amounts of a number of
non-identified alkaloids. Conopharyngine and ibogaine were reported in T. con-
torta (Stapf) Stapf. All known Tabernaemontana spp. thus appear to be characterized
by ibogamine-type alkaloids (Haller and Heckel, 1901).
T. crassa Benth, when intraperitoneally injected (suspension of a crude extract) in
rats, produced decreased motor activity and muscle relaxant effects: the pupil of the
eye was dilated and there was blanching of the ears. Death occurred 30 min after
injection of 250 mg/kg (Sandberg and Cronlund, 1982).
T. crassa and T. pachysiphon have been reported to be stimulants of the CNS and
to be hallucinogenic in large doses (Marderosian, 1967). They increase and extend
the hypertensive action of adrenaline and also have local anaesthetic activity
(Schneider and Sigg, 1957; Raymond-Hamet and Vincent, 1960; Paris and Moyse,
1971, p. 81). Coronaridine hydrochloride, isolated from the roots of the Indian T.
heyania, but also present in the above-mentioned species, has been shown to prevent
pregnancy in rats when administered 1-5 days post coitum (Mehrotra and Kamboj,
1978).
Cannabis sativa L. var. indica Lam. CANNABINACEAE

The plant is nowadays subject to government restrictions in most West African
countries (Nigeria, Ghana, Senegal, etc.). Formerly, it was used as an antidote to
snake poison and to treat malaria and blackwater fever (Hager's Handbuch, 1972,
Vol. Ill, p. 652).
The narcotic resin is obtained from the dried flowering or fruiting tops or from the
green shoots (the quality varies with the district from which it comes). The resin
exudes from the surface during growth and is collected by pressing the tops or
flailing the stems. It contains cannabinol, cannabidiol and several isomeric tetra-
hydrocannabinols, which are the chief active principles. The two main
psychomimetically active components are the (—)transkl- and (-)transA6-isomers
(Kettenes-van den Bosch et ah,1980). In addition, cannabigerol, cannabichromene
and cannabitriol have been reported. The amount of exudate is low in temperate
regions and high in warmer regions. Choline, trigonelline and a coumaric glycoside
have also been found in the tops (Gaoni and Mechoulam, 1964; Schulz, 1964;
Farnsworth, 1969; Turner et al.,1980). Ten flavonoid glycosides have been isolated
by column and paper chromatography. One was found to be the acyl derivative of
apigenol, the others are O-glycosides and C-glycosides (vitexine, isovitexine and
orientine) (Paris et al., 1976).
Cannabis has been used in veterinary medicine as a sedative in the treatment of
equine colic (Merck Index, 1976, item 1748) and in man as an analgesic and hypnotic
and in the treatment of depressive mental conditions (Paris and Moyse, 1967). The
analgesic effect is considered to be a consequence of its general effect on the cerebral
cortex (Kettenes-van den Bosch et al., 1980). It is rarely prescribed even in the
countries where its medicinal use is still authorized. It is known under many local
names such as ganjah, bhang or charas in India, marihuana in North America,
hashish (purified alcoholic extract) in North Africa, kif in Morocco, takrouri in
79
Tunisia, dagga in South Africa, etc. Its production and use has been forbidden in 74
countries since 1956 and the 1961 New York Convention (Paris and Moyse, 1967).
When ingested or (more frequently) inhaled as smoke, the drug first produces a
state of euphoria, intellectual excitement and indifference to surroundings, then
come illusions, loss of the notion of time and space, hallucinations, incoordination
of movements and drowsiness but not complete unconsciousness. The psycho-
mimetic effect is more rapid with smoking than with ingestion (Hager's Handbuch,
1972; Paton, 1975).
Toxic effects of prolonged use of C. sativa include lassitude, indifference, lack of
productive activity, insomnia, headaches, nystagmus, increased susceptibility to
infections, gastrointestinal disturbances, sexual impotence and personality changes.
The slow and prolonged hypotensive action of the drug, and its interaction with
catecholamines in the peripheral system, suggest the possibility of an interaction
with the brain amines being responsible for the behavioural effects observed (Arora
et al., 1976). Kettenes-van den Bosch et al. (1980) write: 'Investigation as to the
therapeutic potential of (—^ransA^tetrahydrocannabinol as an anticonvulsant,
anti-emetic, antiglaucoma, anticancer and analgesic drug have started only recently
and the results to date have not been convincing, adverse effects and the development
of tolerance have been the limiting factors.' Hence they consider that further
investigations are required.
The antibacterial activity of the essential oil of C. sativa was assessed on
Staphylococcus aureus, Streptococcus faecalis, Mycobacterium smegmatis, Pseudomonas
fluorescens and Escherichia coli. The oil was found to be active on Gram-positive
bacteria and has been used against Gram-positive bacteria in cases of resistance
against penicillin (Fournier et al., 1978). The antibacterial agent appears to be
cannabidiolic acid (Farnsworth, 1969).
Myristica fragrans Houtt. MYRISTICACEAE

Nutmeg
Myristica fragrans has been introduced into various parts of West Africa as a spice.
Essential oil of nutmeg is used externally for rheumatism and internally as a
carminative (Oliver, 1960).
The essential oil is associated in the nut with a solid fat. The oil contains pinene,
camphene, borneol, geraniol and eugenol and in the last portions of the distillate,
myristicin (methylene-dioxy-methoxyallylphenol) belonging to the phenyliso-
propylamines. In addition, elemicin and safrol have been reported (Gottlieb, 1979).
The varying proportions of these substances explain the differences in pharma-
cological action of various samples of nutmeg oil (Shulgin et al. in Efron et al., 1967,
pp. 202-14).
The oil is an aromatic stimulant and in high doses it has convulsant and oxytocic
properties. Doses of between 0.2 and 1 g/kg induce dose-dependent light-to-deep
sleep in young chicks. In man, the seeds and arils have in some cases hallucinogenic
properties (Truitt, 1967; Weil, 1967) although this effect is contested by Shulgin
(1966). The ingestion of about 5 g of the seed (about one large nutmeg) can lead after
a few hours to a more or less severe physical collapse, weak pulse, hypothermia,
80
clamminess of the extremities, giddiness, vertigo, nausea and a feeling of congestion

and pressure in the chest or abdomen. For about 12 h there is an alternation of
delirium and stupor, usually resolved by heavy sleep. For several days there may be
headaches, dryness of the mouth, tachycardia and perhaps spells of dizziness
(Weiss, 1960). Myristicin has been said to be effective in quietening hysteric or
delirious patients. The LD 50 in rats is less than 1 g/kg. Myristicin has been shown to
be a MAOI in vitro and in vivo (Truitt, 1967). It may by degradation undergo
transamination, producing 3,4,5-trimethoxyamphetamine; more rapid biodegrada-
tion of pure myristicin, in contrast to a slow release, might suggest a greater
efficiency of the crude drug (Weil, 1965; Shulgin et al, 1967; Truit, 1967; Forrest
and Heacock, 1972).
Datura metel L. syn. (D.fastuosa L. var. D. alba (Nees) C. B. Cl.) SOLANACEAE

Datura stramonium L. including!), tatula L.
Datura innoxia Mill. syn. (D. metel Chev. Berh.)
Datura Candida (Pers.) Safford syn. (Brugmansia Candida Pers., D. arborea Ruiz &
Pavon)(Fig. 3.2)
In tropical West Africa, Datura spp. are used in native beer or in palm wine to add a
stupefying or narcotic effect. Thus, a drink made from the seeds of D. metel is given
as an intoxicant to Fulani youth to incite them in the Sharo contest or ordeal of
manhood (Dalziel, 1937). A decoction of the seeds has been used for eye diseases
(Pobeguin, 1912).
The main alkaloids, present in all species, are the parasympathetic alkaloids atropine
((±)- hyoscyamine), (—)-hyoscyamine and hyoscine (scopolamine). They are found
mainly in the flowers and leaves, and, to a lesser extent, in the seeds.
Nor scopolamine, meteloidine, hydroxy-6-hyoscyamine and tiglic esters of dihy-
droxytropane have been reported as secondary alkaloids (Shah and Khanna, 1963,
1964,1965a, b; Shah and Saoje, 1967). D. metel is the species richest in hyoscine, the
leaves containing approximately 0.5% of total alkaloids of which three-quarters
consists of hyoscine. The total alkaloid content of D. stramonium leaves is roughly the
same, but of this over two-thirds is hyoscyamine/atropine. In D. innoxia leaves
hyoscine predominates, whilst in the seeds it is the hyoscyamine/atropine fraction
which predominates. It was shown that in young leaves of D. metel hyoscyamine is
the main alkaloid, but in adult leaves it is hyoscine. In D. stramonium, however, the
proportions are inverted and hyoscyamine predominates in adult leaves (Jentzch,
1953). Hyoscine is formed in the leaves by epoxidation of hyoscyamine. Long and
intense exposure of the plants to light produces an increase in the hyoscine content.
The amount of alkaloids present also varies with the origin of the plants and can be
increased by various methods, such as deflowering, mutations, fertilizers, etc. (Paris
andCosson, 1965; Karnickand Saxena, 1970a, b). Balbaaetal. (1979) could increase
the percentage of active constituents in D. tatula by more than 100% above the
control level through the use of fertilizers.
Datura spp. are very toxic and their alkaloids can produce delirium with vertigo and
hallucinations. The three main Datura alkaloids have both peripheral and central
actions. By local application to the eye, (—)-hyoscyamine and atropine cause a
81
pronounced and long-lasting mydriasis due to paralysis of the circular muscle of the
eye. They also paralyse the ciliary muscle. The mydriasis produced by hyoscine is of
shorter duration but quicker in onset than that produced by atropine. These
alkaloids are therefore used as eye drops to dilate the pupil and to paralyse
accommodation. They antagonize the activity of the parasympathetic nerves inner-
vating smooth muscles, the glands and the heart by blocking the action of acetyl-
choline at the post-ganglionic nerve endings (anticholinergic effect) and can be used
in conditions where paralysis of the parasympathetic activity is desired, such as
bronchial and intestinal spasms. They are constituents of many asthma powders and
Fig. 3.2. Datura Candida (Pers.) Safford.

82
sea-sickness and anti-chronic bronchitis preparations. Hyoscine also has spasmolytic

and peripheral antispasmodic action, but depresses the CNS, whilst atropine
stimulates the CNS, and it is a useful sedative and hypnotic for patients with
psychomotor agitation, delirium tremens, paralysis agitans and Parkinson's disease.
It also finds a use, generally associated with morphine, as a pre-anaesthetic or for
relieving withdrawal symptoms in morphine addiction. A subcutaneous injection of
1 mg in adults can induce stupor, confusion of mind and loss of will power, and is
reported to have been used for 'brainwashing' (Fattorusso and Ritter, 1967; Karnick
and Saxena, 1970b; Lechatera/., 1978).
II Plants with a depressant action mainly via the CNS

The plants of this group often have a simultaneous activity in several
sections. This applies particularly to those having analgesic, narcotic, sedative,
hypnotic and antipyretic activity: each effect may be the predominating consequence
of a general action on the cerebral cortex (Turner and Richens, 1978).
Narcotic analgesics cause unconsciousness and produce sleep through aboliton of
the reflexes, including the sense of pain, by paralysing the nerve centres. They cause
respiratory depression and a reduction in the motility of smooth muscles (causing
constipation, spasm of the sphincter of Oddi and bronchoconstriction). Most
narcotics have at first a short stimulating action on the nervous system but then cause
a depression with dumbness and stupefaction. An example of a powerful analgesic is
morphine. Minor analgesics can abolish the sensation of pain without producing loss
of consciousness. Some may have, in addition to the analgesic action, antipyretic or
anti-inflammatory activity.
Hypnotics produce sleep (without abolishing the reflexes). Sedatives and tranquil-
lizers decrease watchfulness and calm down motor activity and agitation, and
tranquillizers more particularly weaken exaggerated emotional reactions and
attenuate restlessness. Even in strong doses they are not hypnotic but some relax
skeletal muscles (Lechat et al.> 1978). These drugs are used especially in alleviation
of the symptoms of schizophrenia and allied disorders and have also been called
'anxiolytics'.
Anticonvulsants lower the excitability of certain central neurones and thus are
used to inhibit or diminish the excessive nerve impulses in epileptic convulsions.
Different forms of epilepsy (petit and grand mal, psychomotor epilepsy) are caused
by lesions of the psychomotor connections in the cortical regions of the brain. They
are characterized by convulsions, loss of consciousness and changes in the electro-
cardiogram. In seizures the central inhibition is suppressed and abnormal nerve
impulse activity occurs in small feedback loops (Burgen and Mitchell, 1972).
Antiepileptics act by central inhibitory processes.
Antipyretics regulate the body temperature by reducing hyperthermia to normal
values. A raised temperature induces peripheral vasodilatation and increased perspi-
ration in an attempt to restore the temperature to normal. The exact mechanism by
which antipyretics regulate this process is still not known. A number of plants
originally studied for their antipyretic effects have ultimately been shown to act on
83
the cause of the fever and have antimicrobial, antimalarial or anti-inflammatory

activities. A few, however, like some Holarrhena and some Funtumia spp. containing
alkaloids (see Chapters 2 and 5) and perhaps some containing palmatine and related
alkaloids (see below), may have true antipyretic-analgesic action. Many plants in
this group show several depressant activities simultaneously. Those described in
Chapter 2 (The cardiovascular system) are listed in Table 3.4.
Rhigiocarya racemifera and Kolobopetalum auriculatum (Menispermaceae) are
reported to have analgesic effects attributed to o-methylflavinanthine which has a
structure similar to that of morphine. Two other Menispermaceous plants,
Jateorhiza macrantha and Tinospora bakis, are reported to depress the CNS and to
have antipyretic and hypotensive activity. Khaya senegalensis (Meliaceae) is a
sedative, anticonvulsant and antipyretic(P). Sedative and analgesic action is shown
by Andira inermis (Fabaceae) and sedative and spasmolytic effects alongside a
respiratory excitant action (due to nupharine) in Nymphaea lotus (Nymphaeaceae).
Anogeissus leiocarpus (Combretaceae) has CNS antidepressant activity. Elaeocarpus
sphaericus and Passiflora foetida have been noted to possess, respectively anticonvul-
sant and hypnotic and anticonvulsant and sedative properties. Antispasmodic action
was also reported in Guiera senegalensis. Spasmolytic and hypnotic action was found
in Alstonia boonei (Apocynaceae), which also has cholinergic properties. A sedative
effect on the CNS and a stimulant action on the medulla has been found in Waltheria
indica (Sterculiaceae) and sedative and anticonvulsant actions have been reported for
Piper guineense (Piperaceae). The essential oil of Anacardium occidentale has tranquil-
lizing and antispasmodic properties.
Although in all these plants several chemical constituents have been identified, it
is not always clear which components are responsible for the various activities.
Rhigiocarya racemifera Miers syn. (R. nervosa (Miers) Chev.)

MENISPERMACEAE
Kolobopetalum auriculatum Engl. syn. (K. veitchianum Diels)
In Sierra Leone the root of R. racemifera is scraped and put in palm wine. Both plants
are used for sleeplesness (Dalziel, 1937).
From these two species, 0-methyl-flavinanthine has been isolated. This compound
has a structural formula very similar to that of morphine (Gyang et al., 1964). In
R. racemifera, the alkaloids liriodenine, palmatine, menispermine (Af-methyl-
isocorydine) and magnoflorine have also been found (Mehrotra and Kamboj, 1978;
DwumaBadu etal., 1980).
o-Methyl-flavinanthine has been reported to have a morphine-like inhibitory action
on the peristaltic reflex of the guinea pig's isolated ileum and on the contractions of
the guinea pig's ileum obtained by coaxial electrical stimulation (Gyang etal., 1964;
Gyang and Kosteilitz, 1966). The depressant effect was dose-dependent and the
dose-response was more reproducible with the alkaloid than with morphine. The
effect was not antagonized by nalorphine (Noamesi and Gyang, 1980). o-Methyl-
flavinanthine has been shown to have an analgesic activity equivalent to one-fifth that
of morphine. Reduction of the ketonic group to an alcohol may increase the analgesic
action (Tackie et al., 1974c).
ants with depressant action on the ANS and CNS which are described in Chapter 2
Active constituent Part used Action on nervous system References

itoria Reserpine Rootbark Sedative, tranquillizing See Chapter 2
xicana Protopine, berberine Leaves, stems, seeds Antispasmodic, sedative See Chapter 2
oribunda Conessine Root-and stembark Sedative, tranquillizing, See Chapter 2

CNS depressant, Quevauvill
antipyretic, analgesic (1960); Gouta
85
Jateorhiza macrantha (Hook.) Exell & Mendonca MENISPERMACEAE

This species is closely related to J. palmata (Calumba root) which is naturalized in
Ghana and locally used as a bitter tonic and in the treatment of dysentery in Indian
(Oliver-Bever, 1968).
The root contains, in addition to colombin, related substances such as chasmanthin
and palmarin. It also contains 2-3% of alkaloids of the berberine group: colom-
bamine, jateorhizine and palmatine (Chopra et al., 1956; Barton and Elad, 1956,
1962).
The alkaloids colombamine, jateorhizine and palmatine depress the CNS, and when
injected intravenously are hypotensive in the frog. Palmatine, the most active, acts
mainly on the respiratory system and the blood pressure. The two others increase the
intestinal tonus (see Tinospora bakis) (Paris and Beauquesne, 1938; Henry, 1949).
Calumba root (J. palmata), used as a stimulant for patients with atonic dyspepsia,
contains no tannins, so it can be prescribed with iron salts. However, its use has been
mainly limited to veterinary medicine (Martindale, 1958) as it has occasionally been
reported to produce toxic phenomena such as vomiting, paralysis of the CNS and
depression of the respiratory centre (Paris and Moyse, 1967, p. 180).
Tinospora bakis (A. Rich.) Miers syn. (Cocculus bakis A. Rich.)

MENISPERMACEAE
The bitter roots were sold in Senegal as a remedy for remittent and 'bilious' fevers
and also as an emmenagogue and cholagogue. In India, the plant was in the Indian
Pharmaceutical Codex as a bitter tonic and the root as an antidysenteric. The plant
has been called 'Indian quinine' (Dalziel, 1937).
The roots contain palmatine and 2-3% of columbin (Beauquesne, 1938). Different
bitter heterosides (picroretin = picroretinoside, tinosporide and cordifolin) and the
glycosides giloin and giloinin have been reported to be present in T. cordifolia in
India (Paris and Beauquesne, 1938; Paris and Moyse, 1963).
The root can produce toxic effects: vomiting and depression of the respiratory
centre. Columbin, in small doses, increases the secretion of the bile and of the glands
of the stomach and intestines; at higher doses it produces fatty degeneration of the
liver (Biberfeld, 1910). Toxicity trials on the total alkaloids have shown that 5 mg/kg
are not toxic for guinea pigs whilst 100 mg/kg produce death within 20 min (without
convulsions). In the chloralized dog, an injection into the internal saphenous vein of
10 mg of total alkaloids produces immediate hypotension followed by recovery to
normal within minutes. In experimental hyperthermia in guinea pigs, the tempera-
ture is lowered in a more spectacular way than with quinine sulphate. Palmatine
shows a stronger antipyretic effect than the total alkaloids and it lowers the blood
pressure and depresses the CNS (frog and mammals). It paralyses the respiratory
centre even more than morphine (Beauquesne, 1938; Paris and Beauquesne, 1938).
It is supposed that the antipyretic effect is due, like that of berberine, to paralysis of
the peripheral vessels and to the resulting heat dispersion, and not to its toxicity
towards microorganisms (Kerharo and Adam, 1974, p. 556). T. cordifolia has also
been found to have hypoglycaemic and diuretic effects (Namjoshi, 1955).
86
Khaya senegalensis (Desr.) Juss. syn. (Swietenia senegalensis Desr.) MELIACEAE

Dry zone mahogany, Cail cedrat.
L In Nigeria, Senegal and Guinea the bark is used locally mainly as an antipyretic and
tonic. Moreover, medicinal and veterinary uses of the bark as an anthelmintic
(taenia), an emmenagogue (abortifacient) and as an emetic have also frequently been
reported (Dalziel, 1937).
C The bark contains a bitter principle, first called 'calicedrin', which later proved to
be a mixture of different components (Moyse-Mignon, 1942). On further investi-
gation these were found to consist of several triterpenoids with a lactone or
epoxide function and a furan ring. 6-Desoxy-3-destigloyl-swietenin and its acetates
have been isolated from all parts of the plant. The bark, in addition, contains
nimbosterol Q3-sitosterol), 7-diacetyl-7-oxo-gedunin, methyl angolensate, methyl-
6-hydroxyangolensate and 6-desoxy-3/3-destigloyl-12/3-diacetoxy-swietenin. In the
rootbark, methyl-6-hydroxy-angolensate has been reported, and in the root,
khayasine. In the heartwood, khayasine and derivatives, methyl-angolensate and
7-diacetyl-oxogedunin have been found. In the seeds, khivorine- and swietenine-
derivatives have been found (Bevan et al., 1963, 1965; Adesogan et al., 1967;
Adesogan, 1968; Adesogan and Taylor, 1968). Kerharo and Adam (1974) suggest
the adoption of a new nomenclature based on a common nucleus, which can be
named methyl-meliacate, more so as the composition varies in samples of different
regions.
Similar bitter principles were found in K. ivorensis Chev. (K. klainei Pierre ex
Pellegr., K. caudata Stapf ex Hutch. & Dalz.) (Adosogan & Taylor, 1970; Aspinal
and Bhattacharjee, 1970). Further chemical investigation of stembark extracts of the
two species by spectral, analytical and chromatographic methods led to identification
of the sterols campestrol, stigmasterol and sitosterol and of the coumarins aesculetin
and scopoletin. K. ivorensis was found to contain mainly scopoletin and scoparone
and only traces of aesculetin and umbelliferone whilst in K. senegalensis scopoletin
was the major coumarin next to aesculetin and only traces of scoparone were found.
Scopoletin could also be isolated from the fruit (Adesina, 1983).
P Subcutaneous or intraperitoneal injections of calicedrin (0.05 g/kg) produce a
distinct hypothermic effect (temperature reduction of 2-3°C) on experimental
hyperthermia in guinea pigs (Moyse-Mignon, 1942; El Said et al., 1968). In dogs,
calicedrin produces slight hypertension. An antibiotic action of an aqueous extract
of the stems against Sarcina lutea and Staphylococcus aureus was reported, and in a
dilution of 1:10000 calicedrin kills Paramecia within 20 min (Malcolm and Sofow-
ora, 1969).
Crude hydroethanolic extracts of the stembark of K. ivorensis and K. senegalensis
caused depression, sedation and reduced locomotor activity in mice. The coumarins
scopoletine and scoparone have recently been found to have antipyretic, analgesic
and anticonvulsant activities (Adesina and Ette, 1982; Adesina, 1983; Ojewole,
1983b).
Andira inermis (Wright) DC. FABACEAE

Dog almond or wormback
L The bark has been used in Northern Nigeria for trial by ordeal in the same way as
87
Erythrophleum. It is a dangerous poison in large doses, causing vomiting with drastic

purgation, delirium and narcosis (Ainslie, 1937; Dalziel, 1937). In Senegal, the roots
are used as an anthelmintic and in the treatment of mental diseases (Kerharo and
Adam, 1974).
The bark contains andirine, Af-methyltyrosine ()8-(p-hydroxyphenyl)-a-A/r-
methylaminopropionic acid). Extraction of the heartwood produced an isoflavonoid
as well as biochanine A (a trihydroxy-isoflavone), small amounts of fatty acids with
long ramified chains and /3-sitosterol (Cocker et al., 1962, 1965). y-Aminobutyric
acid was found in extracts of leaves and stems (Durand et al., 1962).
The bark extracts are considered narcotic (Watt, 1967) and also have some insecti-
cidal action (Heal and Rogers, 1950).
Nymphaea lotus L. syn. (N. liberiensis Chev. and other spp.) NYMPHAEACEAE
A narcotic use of the rhizomes existed in ancient Egyptian and Mayan rituals
(Oliver-Bever, 1961; Emboden, 1981). In West Africa, the rhizome is a food of
scarcity. The seeds are used by the Hausas (Northern Nigeria) in eruptive fevers. In
Sierra Leone, an eye lotion is prepared from the leaves, an infusion of stems and roots
is used as an emollient and diuretic, and a decoction of the flowers as a narcotic and
sedative. In the Ivory Coast a decoction of Nymphaea is taken for coughs and
bronchitis (Oliver, 1960).
A number of alkaloids have been recorded from the flowers and rhizomes of different
Nymphaea spp. The chief alkaloids are nymphaeine, nymphaline, nupharine and a-
and /3-nupharidine. Quercitin has been reported to be present in the leaves (Chopra
et al., 1956; Hegnauer, 1962-68, Vol. V, p. 441). Delphaut and Balansard (1941)
observed confusion concerning the reported constituents and their botanical origin.
They studied 'nupharine' from N. alba L. (not growing in West Africa) and this was
found to consist of nelombine, nupharidine, nymphaeine and a-nupharidine.
The rhizomes of N. alba were tested on mice, eels and dogs, and in all cases there
was a narcosis that terminated in somnolence (Delphaut and Balansard, 1941).
Convulsions induced by strychnine could be counteracted by N. alba rhizomes, and
these were characterized as antispasmodic and sedative by Delphaut and Balansard
(1943). These workers found that nymphaeine is mainly localized in the rhizomes of
N. lotus; its minimum effective and lethal doses for frogs are 30 and 50 mg/kg,
respectively, and in mice and pigeon 60 and 80 mg/kg, respectively; warm-blooded
animals die from central respiratory paralysis. Nymphaline, found in the flowers,
acts as a cardiac glycoside. Nupharine, also found in the flowers, produces paralysis
of the cerebrum when administered to frogs, mice, rats, guinea pigs and pigeons; it
acts also as a respiratory excitant and causes death by respiratory poisoning. Two
un-named alkaloids found in the flowers and roots show sedative action in small
doses (Chopra et al., 1956, p. 177). More recently the pharmacology of a number of
Nymphaea alkaloids was studied by Dimitrov (1965), who reported sedative,
spasmolytic and hypertensive properties. N. tuberosa is very active against
Mycobacterium smegmatis (Su et al., 1975).
Anogeissus leiocarpus (DC.) Guill. & Perr. syn. (Conocarpus leiocarpus D C ,
A. schimperi Hochst. ex Hutch. & Dalz., A. leiocarpus var. Schimperi (Hochst. ex
Hutch, and Dalz.) Aubrev.) COMBRETACEAE
88
L A decoction of the leaves is used in Nigeria for ablutions in the treatment of skin
diseases and itch and is considered to be an antidiarrhoetic. The powdered bark is
applied to wounds and ulcers and in some regions an infusion of the bark is given as
a febrifuge and the bark or seeds as a vermifuge (mainly for tapeworm in horses and
donkeys) (Dalziel, 1937).
C The leaves, roots and bark contain 17% tannins. In the gum exuding from the trunk
20% uronic acids have been found. These produced, via hydrolysis, 12% (+)-xylose,
32% (-)-arabinose, 5% (+)-galactose, 2% (+)-mannose, 20% of oligosaccharides
and traces of rhamnose, ribose and fucose (Aspinal and Christensen, 1961). The
stembark of A. latifolia grown in India contains sitosterol, flavellagic acid, 3,3',4-tri-
O-methyl ellagic acid, quercitin, myrecitin and procyanidin along with gallotannins,
shikimic acid, quinic acid and free sugars. It also contains alanine and phenylalanine
(Bhakuni era/., 1970).
P A. leiocarpus appears to contain a non-toxic CNS depressant principle (Fong et al.,
1972). The related A. latifolia Wall, has been found to have CNS depressant action
to counteract an amphetamine hyperactivity test in mice (Bhakuni et al., 1969b).
Elaeocarpus sphaericus Schum. syn. (E. ganitrus Roxb.) TILIACEAE

L In traditional Indian medicine the fruits of the plants were used in mental diseases,
epilepsy, hypertension, asthma and liver diseases (Bhattacharya et al., 1975b). The
plant has been introduced in West Africa.
C A fixed oil has been obtained from the seeds of E. serratus L. (Chopra et al., 1956).
P Bhattacharya et al. (1975b) noticed a prominent CNS-depressant effect of the
water-soluble portion of the 90% ethanol extract of the fruit. The effect was
characterized by potentiation of hexobarbitone hypnosis and morphine analgesia
and by anticonvulsant and anti-amphetamine activities. In addition, cardiostimu-
lant, smooth muscle relaxant and choleretic activities were reported. These effects
were partly based on a direct musculotropic effect or were mediated through
/3-adrenoreceptor stimulation (Bhattacharya et al., 1975b).
Passiflora foetida L. PASSIFLORACEAE

P. edulis Sims and related spp.
Stinking passion flower
L P. edulis and related spp. are cultivated in West Africa for their fruits. P. foetida has
fruits which are edible when ripe, but before maturity the leaves and green fruit
contain a cyanogenetic glucoside (Dalziel, 1937). A decoction of the leaves and roots
is regarded in the Antilles as an emmenagogue and useful remedy in hysteria. The
leaves were applied as a dressing for wounds (Sebire, 1899). In India, a decoction of
the leaves is used in the treatment of biliousness and asthma (Chopra et al., 1956).
C From the aerial parts of P . incarnata, Neu (1954, 1956) isolated indole derivatives
and identified harmane. Traces of harmine and harmol were reported by Lutomsky
and Wrocinski (1960) who, in addition, isolated flavonic derivatives by paper
chromatography (Paris, 1963; Paris and Moyse, 1967, p. 458).
P P. incarnata was registered in the French Pharmacopoeia, 1937, for its sedative and
antispasmodic properties. The extract of the plant shows antispasmodic activity on
89
the rabbit intestine and is synergistic to papaverine and antagonistic to barium

chloride and pilocarpine-induced effects. It decreases motility in mice and rats
(Paris, 1963; Paris and Moyse, 1963).
Guiera senegalensis Gmell. COMBRETACEAE

The dried pounded leaves are taken by women after childbirth to increase lactation
and as a general tonic and blood restorer after any exhausting conditions. In Sokoto,
the plant has the reputation of preventing leprosy and the leaves are applied
externally for skin diseases. In Bornu, the roots are powdered, boiled and used as a
remedy for diarrhoea and dysentery (Dalziel, 1937). Certain tribes in Senegal and
Guinea use the leaves like those of certain species of Combretum for the treatment of
colds, bronchitis and fever (Dalziel, 1937).
For the first time, indole alkaloids (harmine and tetrahydroharmine) have been
found in a member of the Combretaceae. They are present in the roots (Combier et
al., 1977). The ash of roots and leaves is rich in mineral elements. Mucilage, gallic
and catechuic tannins, flavonoids, amino acids and alkaloids (0.2% in the roots and
0.15% in the leaves) have also been reported (Koumare et al., 1968).
Plants collected in Senegal and Mali showed a depressive action on the CNS. In
addition, anti-inflammatory and antitussive actions (mainly of the leaves) were
noted; an antidiarrhoeic effect was particularly spectacular in rats infected with
parasites. Kerharo et al. (1948) report the spectacular effects of the treatment with
G. senegalensis in an epidemic of choleriform diarrhoea with gallbladder infection in
Upper Volta.
Alstonia boonei de Wild. syn. {A. congensis Chev. & Aubrev.) APOCYNACEAE
Pattern wood, stool wood
In Nigeria the bark of A. boonei, which is the most common variety ofAlstonia in the
country, is widely used as an antipyretic in the treatment of malaria, and sometimes,
together with the leaves and roots, in external applications for rheumatic pains.
Smearing the latex on Calabar swellings caused by filaria has also been recom-
mended. In Ghana a decoction of the bark is given after childbirth to help the
delivery of the placenta (Dalziel, 1937; Irvine, 1961).
The bark of A. boonei contains echitamine (the main alkaloid), two echitamidine
derivatives and a lactone boonein (Marini Bettolo et al., 1983). The yield of total
alkaloids varies with the location: in Ghana, it is 0.38-0.56%; in Nigeria, 0.18-
0.31%; in the Cameroons, 0.11% (Goodson and Henry, 1925; Monseur and van
Bever, 1955). The triterpenes /3-amyrin and lupeol have been reported in the bark
and ursolic acid has been found in the leaves of A. boonei (Kucera et al., 1972,1973).
In the flowers of an Indian species, A. scholaris, a number of indole alkaloids have
been reported, the major one being picrinine, which was found to possess a CNS
depressant action in rats and mice (Dutta et al., 1976).
The reputation of Alstonia spp. as antimalarial agents was such that A. scholaris and
A. constricta bark had formerly been included in the British Pharmacopoeia, 1914.
The antimalarial action could not be confirmed in many tests carried out by
numerous authors on birds, monkeys and human beings (Henry, 1949, p. 720). It
90
was noted, however, by some that the bark of A. scholaris produced a fall of
temperature in human patients and while this lasted the patients appeared relatively
free from symptoms (Chopra et al., 1938). This antipyretic action and the fact that
these drugs were used in days when the diagnosis of malaria was not always accurate
may account for doubtful results and earlier use (Henry, 1949, p. 720).
Echitamine was reported to lower carotid pressure and increase the renal output
(Raymond-Hamet, 1934, 1941; Esdorn, 1961). More recently, Kucerzetal. (1973)
and Marquis (1975) observed that echitamine causes a fall of the blood pressure in
hypertensive cats. Later, however, Marquis and Ojewole (1976) noticed that the
hypotensive effect occurred only occasionally after a first intravenous injection of
6 mg/kg and thought that the diuretic action on saline-loaded dogs and cats may
explain this hypotensive action. Ursolic acid, at first considered an inert compound,
was found to act on the electrolytic balance. Doses of 3 mg produced a sodium
retention equivalent to that of 3 /xg DOCA (desoxy-cortisone) and a considerably
higher potassium retention in adrenalectomized rats (Wenzel and Koff, 1956;
Marquis and Ojewole, 1976). These authors also reported that echitamine in
particular potentiated the barbiturate sleeping time of mice and rats and enhanced
the lethality of strychnine. Echitamine contracts the isolated toad rectus abdominis
preparation and its action was enhanced by increasing concentrations of acetyl-
choline and reversed by physostigmine on the isolated rat hemi-diaphragm. This
action could be an undesired side-effect in native malaria treatment with decoctions
or infusions of the bark although the plant has been said to have a relatively low
toxicity. The ineffectiveness of echitamine treatment against a strain of Plasmodium
berghei was noted (Marquis and Ojewole, 1976).
The spasmolytic and hypotensive actions of echitamine have recently been
confirmed by Ojewole (1983a). The alkaloid also blocked the neuromuscular
transmission in various muscle-nerve preparations examined. The author was able
to show that the depressor effect is unlikely to be mediated via a cholinergic
mechanism or histamine Hj-receptor stimulation.
In Indian Alstonia spp. several alkaloids with a CNS action have been reported,
thus picrinine was said to potentiate hexobarbitone hypnosis and morphine analgesia
(Dutta et at., 1976), and alstovenine from A. venenata (not in West Africa) was in low
doses a MAOI and in high doses a marked CNS stimulant. Venenatine, also from A.
venenata, has, on the contrary, a reserpine-like action. It potentiates the hexobarbital
sleeping time, antagonizes amphetamine toxicity, morphine analgesia and the
anticonvulsant action of diphenylhydantoin, is synergistic with reserpine and can
reduce the pressor response to tyramine but not to adrenaline (Bhattacharya et al.,
1975a).
Waltheria indica L. syn. (W. americana L.) STERCULIACEAE

In northern Nigeria and in Togo a decoction of the root is frequently given to
children to strengthen their resistance against fever, etc., and the Hausas also
recommend a root decoction to produce immunity. In Togo and also in India the root
is used in a cough medicine, and in Senegal it is used for the healing of wounds. In
Cay or (Senegal) it is sometimes used as an antiepileptic.
91
An original analysis of the plant only revealed mucilage, tannins and sugars (Dalziel,
1937). Later, unidentified alkaloids were reported to be present in the leaves and
rootbark. Finally, three alkaloids were isolated from whole plants from the Ivory
Coast. These were called adouetines x, y and z. These alkaloids are of a particular
type, and were named 'basic peptides' by Goutarel. Of the four nitrogen atoms in the
molecule only one is basic, the three others are present in peptide linkages (Pais et
aL, 1963).
Pharmacological studies have been carried out with the amidosulphonate of
adouetine z. The LD 50 in mice is 52.5 mg/kg. The drug behaves as a sedative of the
CNS and a stimulant of the medulla. In the dog it produces hypertension slows down
the heartbeat (compensatory reflex?) and has a relaxing action on the smooth muscle
fibres of the intestine (Blanpin et aL, 1963).
Piper guineense Schum. & Thonn. syn. (P. leonense D C , P . famechonii DC.)
PIPERACEAE
West African black pepper or Ashanti pepper
The black berries are a much-used spice. The pepper is used externally as a
counter-irritant or in a stimulating ointment, and internally as a stomachic and
carminative. The pulverized grains are useful as an insecticide.
Chromatographic analysis of the fruits has revealed the amides piperine, N-iso-
butyloctadeca-fraws-2-fraws-4-dienamide, sylvatine, Aa,/3-dihydro-piperine, tricho-
stachine and a new naturally occurring amide, Aa,/3-dihydro-piperlonguminine
(Addae-Mensah et aL, 1977a, b). In the roots, piperine, trichostachine, and in the
leaves, dihydrocubebin, a new naturally occurring lignan, have been reported
(Dwuma Badu, 1975d). Earlier, 0.2% of a lignan derived from shikimic acid,
aschantine and another lignan, which has been named yangambine, had been
reported by Hanzel et al. (1966). An essential oil composed of terpenes (phellan-
drene, pinene, limonene has been obtained from the berries (1-2.4%) (Dwuma Badu
etaL, 1975d, 1976a; Tackier aL, 1975a; Rainaâ/., 1976).
Some of the constituents have been reported to have antimicrobial, anticonvulsant,
antihypertensive, sedative, tranquillizing and insecticidal properties (Fong, 1972;
Addae-Mensah et aL, 1977a, b). Small quantities act as a gastric stimulant and
carminative, increase the flow of saliva and gastric juice, have diuretic and diaphore-
tic properties and act as a nervous stimulant. They also have bactericial and
insecticidal action. In high doses, they are irritating to the skin and mucosae and can
produce convulsions and haematuria (Paris and Moyse, 1967, Vol. II, p. 113). A
derivative based on piperine, isolated from P. nigrum seeds is used in Chinese
medicine as an antiepileptic (Xiao, 1983).
Anacardium occidentale L. ANACARDIACEAE

(See also Chapter 2.)
An essential oil obtained by steam distillation from the leaves of A. occidentale
produced in rats, in doses of 150-300 mg/kg of a 5% oil emulsion given intraperi-
toneally, a dose-related decrease of spontaneous motor activity and potentiated
92
sodium pentobarbitone-induced hypnosis. Rota rod performance was decreased and

further investigations suggested a CNS depressive action of tranquillizer type
similar to, but lower than that of chlorpromazine. The essential oil possesses,
however, an additional analgesic action (Carg and Casera, 1984).
Sedation, decreased spontaneous motor activity, loss of muscle tone, potentiation

of barbitone sleeping time and ether anaesthesia were also seen with the xanthones
from Calophyllum inophyllum Guttiferae (see Chapter 5).
Ill Peripherally acting depressants of the CNS

(a) Local anaesthetics
Local anaesthesia is a selective inhibition of conduction in the afferent or
sensory nerves and endings resulting in the loss of the sensations of pain, pressure
and temperature in localized areas of the body, especially the skin and mucous
membranes. Local anaesthetics may act by preventing the liberation of acetylcholine
from the preganglionic nerve endings thus blocking nerve conduction when applied
locally. In low concentrations local anaesthetics mainly prevent the generation and
production of nerve impulses. Their site of action is the cell membrane which they
depolarize in changing the permeability to potassium and sodium ions. They can
produce a depressant effect on the heart and a relaxation of the smooth muscles,
which can be explained by the ganglioplegic action but can also be due to a direct
stabilizing effect on the axonic membrane (Lechat et al., 1978, pp. 582-3). Local
anaesthetics are broken down in the liver to non-toxic constituents. Overdoses may
lead to tremor, restlessness and convulsions (Burgen and Mitchell, 1972; Turner
and Richens, 1978).
The local anaesthetic activity of cocaine from Erythroxylum coca (Erythroxylaceae)
has long been known. Local anaesthetic action has also been recorded in Cassia absus
(Caesalpiniaceae) through chaksine and isochaksine. The majority of the other
plants with local anaesthetic action seem to act through the ANS. The local
anaesthetic activity of Jatropha podagrica is attributed to tetramethylpyrazine and
that of Erythrophleum guineense to cassaine. Indole alkaloids with local anaesthetic
action have been reported in Mitragyna spp. (Rubiaceae) (mitraphylline), Pausiny-
stalia johimbe (Rubiaceae) (yohimbine) and Voacanga africana (Apocynaceae) (voa-
cangine) and a local anaesthetic steroid alkaloid has been noted in Picralima nitida
(Apocynaceae).
Erythroxylum coca Lam. ERYTHROXYLACEAE

Cocaine plant
Cultivated in West Africa (Hutchinson and Dalziel, 1954, p. 356), the astringent
leaves are used locally in India as a stimulant and masticatory (Chopra et al., 1956,
P. in).
The leaves contain the alkaloid cocaine which is also present in the bark and seeds.
In India, the leaves contain 0.4—0.8% of total alkaloids, largely cocaine (methylben-
zoylecgonine), but also other pseudotropanol derivatives such as cinnamylcocaine,
93
truxillines and tropacocaine (benzoylpseudotropanol), as well as some monocyclic

Af-methylpyrrolidine derivatives (Henry, 1949, pp. 93-104; Paris and Moyse, 1967,
p. 283-4).
Cocaine has pharmacological actions on the nervous and cardiovascular systems
similar to those of other local anaesthetics but it blocks the uptake of catecholamines
into nerve terminals and so has sympathomimetic properties. It produces surface
anaesthesia on the eye and mydriasis. Despite vasoconstrictive properties it is readily
absorbed from mucous membranes and is used for anaesthesia of respiratory
passages (bronchoscopy) but more suitable drugs are now available. Cocaine
stimulates the CNS and has been used as a stimulant in neurasthenia but must be
given under strict medical control as it is habit-forming. It produces a short spell of
intellectual stimulation and euphoria followed by depression. Large doses cause
convulsions followed by central paralysis and finally by failure of respiration
(Burgen and Mitchell, 1972; Turner and Richens, 1978).
When E. coca leaves (or powder) (5-10 g) are taken orally by human subjects
cocaine is immediately detected in the blood by gas chromatographic mass spec-
trometry. It reaches peak concentrations after 40 min to 1 h and persists in the
plasma for more than 7 h (Holmstedt et al., 1979).
Cassia absus L. CAESALPINIACEAE

Four-leaved senna
The seeds are used in West Africa as a fomentation in ophthalmias and are also used
to treat ringworm infections. The leaves are used in Northern Nigeria and in Togo
as a dressing for ulcers and swellings believed to be of venereal origin. In India the
leaves are employed to treat asthma and the seeds are used for the treatment of
ringworm and ophthalmias (Chopra etal., 1956; Oliver, 1960).
The seeds contain a fixed oil and a toxalbumin absin, similar to abrin from Abrus
precatorius, as well as two alkaloids, chaksine and isochaksine. /3-Sitosterol and
/3-sitosterol glucoside are found in the seed oil (Oliver, 1960; Qureshi et al., 1964).
Chrysophanol, aloe emodin, chaksine and isochaksine have been isolated from the
roots and in addition to the two alkaloids, quercitin and rutin have been found in the
leaves (Siddiqui and Ahmad, 1935; Oliver, 1960; Krishna Rao et al., 1979).
The pharmacology of chaksine and isochaksine has been extensively studied by
Pradhan et al. (1953), Bukhari and Khan (1963) and Khan et al. (1963). Both
alkaloids proved to have a local anaesthetic action on guinea pig skin when
administered intradermally. The action is inferior to that of procaine, which proved
to be 3.6 times more active than chaksine and 1.7 times more active than isochaksine.
The anaesthetic action was confirmed in Man. By intradermal injection they
produce histamine-like reactions. Chaksine and isochaksine also have distinct
hypotensive and depressant effects on the parasympathetic nerve terminals of the
bronchi, intestines and bladder (an action comparable to atropine) and also have a
ganglioplegic and curariform action, isochaksine being generally somewhat less
active than chaksine. Thus, both have a general depressive action on the CNS and
the neuromuscular junctions (Pradhan et al., 1953). Strong anti-5-hydroxytryp-
94
tamine action has also been reported. The LD 50 for chaksine given perorally to mice
was around 70 mg/kg; in frogs it was 100 mg/kg. Chaksine and isochaksine also have
an antibacterial action (Gupta and Chopra, 1953). Chaksine inhibits the growth of
Staphylococcus aureus and of Bacillus haemolyticus at dilutions of 1:100000 (Cheema
and Priddle, 1965).
Jatropha podagrica Hook. EUPHORBIACEAE

A native of Central America, this species is much cultivated in West Africa. The local
medicinal uses in Ghana and Nigeria are as an antipyretic, diuretic, choleretic and
purgative; stems and roots are used as chewing sticks (Irvine, 1961). J. curcas seed
oil is used in local medicine in dropsy, sciatica, paralysis, worms and skin diseases
(Oliver, 1960).
Tetramethylpyrazine has been obtained from the stem of J. podagrica. This
substance had formerly been reported to be present in fermented soya beans, cocoa
beans and tobacco smoke (Odebiji, 1978). In J. curcas a toxalbumin (curcin) and
small quantities of glycosides have been reported (Chapter 2, this volume).
Tetramethylpyrazine demonstrated antibacterial activity (Odebiji, 1978). In anaes-
thetized cats it produced depressor effects, reduced the heart rate and blocked
neuromuscular transmissions and appeared to have a spasmolytic activity on smooth
muscles (Ojewole, 1980; Ojewole and Odebiji, 1980). Further studies confirmed
blockage of adrenergic and cholinergic transmission by tetramethylpyrazine. The
compound depressed and abolished the electrically evoked contractions of the chick
oesophagus, rabbit duodenum and guinea pig vas deferens in vitro. It also inhibited
the electrically induced contraction of the rat isolated hemi-diaphragm and of the
cat's nictating membrane in vivo. Apart from its possible central effects, and those
on the cardiac muscle and blood vessels, it could be suggested, from the results
obtained in this study, that the hypotensive effect in experimental animals is likely
to be contributed to by, or mediated via, its local anaesthetic (membrane stabilizing)
activity. Through this action, the drug probably acts to block sympathetic and
parasympathetic neurones and ganglia (Ojewole, 1981).
Tetramethylpyrazine has a number of other pharmacological actions. A main
central effect was found to be tranquillization and sedation (Ojewole and Odebiji,
1984).
In China, tetramethylpyrazine originating from plants is used in the treatment of
occlusive cerebral vessel diseases such as cerebral embolism (Xiao, 1983).
Plants having local anaesthetic action which are described in Chapter 2 (The
cardiovascular system) are listed in Table 3.5.
(b) Neuromuscular blockers (curare action) and anticonvulsants

Plants which act on the neuromuscular junctions do so through the curare
alkaloids. When introduced into the bloodstream the curare alkaloids act by
interrupting the transmission of the nerve impulse at the neuromuscular junctions
thus producing a profound and progressive paralysis of the voluntary movements.
Continued administration leads to paralysis and finally death through paralysis of
Table 3.5. Plants with local anaesthetic action which are described in Chapter 2
Plant Family Active constituent(s) Part(s)used Action on nervous system References

Picralima nitida Akuammine, akuammidine Stem-and rootbark Local anaesthetic: stembark Adrenergic action:
Apocynaceae equivalent to cocaine, Chapter 2
rootbark threefold that of
cocaine hydrochloride
Voacangaafricana Voacangine Stem-and rootbark Local anaesthetic and Adrenergic action:
Apocynaceae analgesic Chapter 2
Pausinystaliajohimbe Yohimbine Bark Local anaesthetic Adrenergic action:
Rubiaceae Chapter 2
Corynanthepachyceras Corynanthine Bark Mild local anaesthetic Adrenergic action:
Rubiaceae Chapter 2
Mitragyna stipulosa Mitraphylline, Rootbark Local anaesthetic CNS
Rubiaceae rhynchophylline
96
the diaphragm. Many curare alkaloids have to be injected as they are not absorbed
from the intestine and the injection produces a short-lasting reversible effect as the
concentration of the alkaloids in the plasma is reduced by half every 13 min. A
secondary effect of the curare alkaloids is the lowering of the arterial blood pressure,
caused in some cases through the liberation of histamine and in others by ganglionic
blockade. In small doses the curare alkaloids provide the muscular relaxation needed
in abdominal and thoracic operations, in endoscopy and in painful spasmodic
conditions found in tetanus and strychnine poisoning (Burgen and Mitchell, 1972;
Lechat et al., 1978). The relaxation spreads down from the head to the abdomen and
members and affects the diaphragm last. However, on complete relaxation of the
abdominal muscles already 50% of the respiratory muscles are involved. Hence the
use of these blockers requires ventilation and precautions (Lechat etal., 1978).
Curare-like compounds act as antagonists to acetylcholine by competing for the
acetylcholine receptors, but other forms of curare can be acetylcholine-mimetic
occupying the actual site of acetylcholine on the neuromuscular junctions and these
forms are slowly destroyed by cholinesterase (Lechat et al., 1978).
Some of the South American, Japanese and Indian species of the Menispermaceae
are the chief sources of curare alkaloids. They have been used as arrow or hunting
poisons and were prepared in pots or bamboo tubes according to the region, as
opposed to Strychnos curare, which was prepared in calabashes and is more toxic.
The main alkaloids of curare are asymmetric bis-benzylisoquinoline (or bis-coc-
laurine) alkaloids such as (+)-tubocurarine, stereoisomeric (—)-chondrodendrine,
((—)-bebeerine = buxine = pelosine) and also (+)- and (—)-isochondrodendrine,
chondrofoline and oxyacanthine. Of all these, (H-)-tubocurarine appears to be the
most important and the South American Chondrodendrons remain its main source.
Most of the West African members of the Tricliseae and Cocculeae tribes contain
curare alkaloids derived from bis-benzylisoquinoline, although not in large
amounts. Cissampelos owariensis, C. mucronata, Cocculus pendulus, Tiliacora
dinklagei, Triclisia dictyophylla and Epinetrum cordifolium have all been shown to have
neuromuscular blocking action.
Erythrina alkaloids, with the exception of erythroidine, have neuromuscular
blocking and CNS depressant and smooth muscle relaxant activities. They have the
advantage of being active if taken orally but their action is short-lasting as they are
tertiary bases and lose part of their activity through transformation into quaternary
bases (which are 10-12 times less active). Their toxicity is high, however, and they
have therefore now been mostly replaced by other drugs. West African Erythrina
spp. with active constituents are E. senegalensis, E. excelsa and E. sigmoideae.
Curariform activity is also reported in two further Fabaceae, Mucuna pruriens and
Desmodium gangeticum.
Cissampelos mucronata A. Rich. syn. (C. pareira of F.T. A.) MENISPERMACEAE

Velvet leaf
Cissampelos owariensis Beauv. ex DC. syn. ( C pareira L. var. owariensis (Beauv.
ex DC.) Oliv., C. robertsonii Exell.) (Fig. 3.3)
Pareira brava
97
The roots of both species (which are often confused) are used locally as an
emmenagogue, abortifacient, antipyretic and diuretic. A decoction of the leaves is
used as a light purge. In India, the leaves are used as a local application for itch
(Oliver-Bever, 1968). The roots of C. owariensis are known in commerce as Pareira
brava.
Fliickiger and his co-workers isolated from the roots of C owariensis, 0.5% of the
alkaloid bebeerine, which was later separated into two stereoisomeric forms and a
neutral crystalline substance, deyamitine (Oliver-Bever, 1968). The alkaloids of the
West African C. owariensis were examined by Dwuma Badu et al. (1975a), who have
reported dehydrodicentrine, dicentrine, cycleanine, insularine and isochondroden-
drine. In Portuguese Africa, Ferreira et al. (1965) isolated from the roots of
C. mucronata, isobebeerine ((+)-isochondrodendrine), hyatine ((±)-bebeerine) and
hyatinine. In India, hyatine and hyatidine (±)-4'-O-methylbebeerine) and curine
((-)-bebeerine) were also found in the local C. mucronata, and in total eleven
quaternary and five tertiary alkaloids were detected (Srivastava and Khare, 1964;
Boissier et al., 1965; Bhatnagar and Popli, 1967; Bhatnagar et al., 1967;
Roychoudhury, 1972).
The curarizing activity of C. mucronata was tested on toad recto-abdominal striated
muscle and on rat isolated nerve-diaphragm preparations of rats (Correia da Silva
and Pavia, 1964). Some curarizing action was observed, which was greater in the
methachloride and methiodide derivatives of hyatine. Hyatine methiodide was 2.5
times more active than (+)-tubocurarine. The activity of the hyatine derivatives on
blood pressure and respiration was greatest in those with the highest curarizing
Fig. 3.3. Cissampelos owariensis Beauv. ex DC.

98
potency and decreased in parallel with the neuromuscular activity (Pradhan and De,
1959; Sen and Pradhan, 1963; Bhatnagar et al., 1967, 1971; Basu, 1970). Another
bis-benzyl isoquinoline alkaloid isolated from the bark of C. mucronata, cissam-
pareine, was found to have significant and reproducible inhibitory action against
human carcinoma cells of the nasopharynx in cell culture (Kupchan et al., 1965).
Cocculus pendulus (J. & G. Forst.) Diels syn. (C. leaeba (Del) D C , Epibaterium
pendulum J.R. & G. Forst.) MENISPERMACEAE
The small red fruits are used by the Arabs to make an intoxicating drink. The roots
of the plant are used in Nigeria as an antipyretic and in Senegal as a cholagogue and
diuretic (Dalziel, 1937; Kerharo and Adam, 1974).
The roots contain a bitter principle, colombin, and three alkaloids, pelosine (Chopra
et al., 1956), palmatine and sangoline (oxyacanthine) also found in Berberis
(Beauquesne, 1938). Chemically, pelosine is believed to be identical with bebeerine
or chondrodendrine, but slightly controversial opinions exist (Henry, 1949). Pal-
matine is a phenolic base belonging to the protoberberines whilst sangoline is a
bis-benzylisoquinoline alkaloid. The stem and leaves contain, besides mineral
elements such as potassium, sodium, magnesium, iron, aluminium, copper and
zinc, two new bases, penduline of a biscoclaurine type and a bis-benzylisoquinoline
alkaloid, an isomer of trilobine, cocsuline (Bhakuni et al., 1970; Gupta et al., 1970;
Joshi et al., 1974; Bhakuni and Joshi, 1975). In addition to the tertiary phenolic
alkaloids, the rhizome of Cocculus trilobus has been found to contain cocculine and
cocculidine (Wada et al., 1967) and two erythrinan alkaloids, which were named
coccutrine and dihydroerysovine (Ju-Ichi et al., 1978). The Chinese drug Hang-
Fang-Chi is obtained from C. laurifolius, C. diversifolius and C. japonicus, which
have alkaloids related to those of C. sarmentosus, C. trilobus and C. hirsutus. An
insecticidal alkaloid, cocculidine, has been obtained from C. trilobus (Oliver-Bever,
1968).
Colombin and palmatine have strong stomachic and bitter tonic action, and Cocculus
root has been used as a tonic in a similar way to Chasmanthera root. The root extract
had a relaxant and antispasmodic effect on the rat ileum and stimulated the uterus of
the albino rat. Toxicity was low; up to 40 mg/kg given intravenously and 100 mg/kg
given orally produced no toxic effects in rabbits and albino rats. A solution of the
alkaloids has a cardiotonic action which is five times that of the total extract and is
comparable to that of 50-100 fxg of digoxin (Das et al., 1964). Sangoline produced
long-lasting hypotension in dogs and, in doses of 0.1-0.2 g, clonic convulsions and
death through paralysis of the respiratory centre in rabbits (Henry, 1949; Das et al.,
1964). Palmatine has similar paralysing action and is also strongly hypo tensive. An
extract of the stems and leaves of Cocculus pendulus has a distinct anticancer action.
In sarcoma 180 it produces a 60% reduction, and in Lewin's lung carcinoma, 50%
reduction, of the number of tumours compared to control animals (Abbot et al.,
1966). The extract also has an anticancer activity against human epidermal car-
cinoma of the nasopharynx in tissue culture (Bhakuni et al., 1969b).
99
Tiliacora dinklagei Engl. syn. (Glossopholis dinklagei (Engl.) Stapf)

MENISPERMACEAE
Tiliacora funifera (Miers) Oliv. (Troupin includes T. warnecki Engl. ex Diels. and
T.johannis Exell. in this species).
Both plants have been used in local medicine in Ghana in the treatment of gastric
fevers and menstrual irregularities (Tackie and Thomas, 1968).
The major alkaloid obtained from the roots of T. funifera is the bis-benzyl-
isoquinoline biphenyl base, funiferine. Isotetrandrine, thalrugosine (nortiliacorine
A) and a new imino-bis-benzylisoquinoline alkaloid, tiliafunimine, have been
isolated from the leaf extract (Tackie and Thomas, 1968; Tackie et al., 1973b, c,
1975b; Ayim et al., 1977; Dwuma Badu et al., 1977). In T. dinklagei roots, in
addition to nortiliacorine A and funiferine, tiliacorinine, tiliageine and dinklacorine
(which later could be identified as a positional isomer of tiliacorine) have been found
(Tackier al., 1974d, 1975b; Dwuma Badu et al., 1976b, 1979).
Funiferine and nortiliacorine have weak antimalarial and antimicrobial activities,
but their dimethiodides have a potent neuromuscular blockade action of the curare
type (Tackie et al., 1979). Using the isolated phrenic nerve diaphragm preparation
of the rat, it has been shown that they are slightly less potent than (+)-tubocurarine
in vitro but more potent than gallamine; this also applies to phaeanthine, a
bis-benzylisoquinoline alkaloid from Triclisia (see below) (Boissier etal., 1963; Ansa
Asamoah and Gyang, 1967). Tackie et al. (1973b) noted that funiferine dimethiodide
has a slightly higher activity than tubocurarine hydrochloride. Funiferine has been
shown to have some activity in P-388 lymphocytic leukaemia and to inhibit the
growth of the acid-fast bacillus Mycobacterium smegmatis (Geran et al., 1972).
Triclisia dictyophylla Diels syn. (T. gilletti (de Wild.) Staner, Tiliacora trichantha
Diels) MENISPERMACEAE
Triclisia patens Oliv.
Triclisia subcordata Oliv. syn. (Tiliacora subcordata Chev.)
The Triclisia have various local medicinal uses such as the treatment of oedema of the
legs, anaemia, diarrhoea, 'joint pains' and in the case of T. patens, of malaria (Oliver,
1968).
From leaf extracts of T. dictyophylla, the bis-benzylisoquinoline alkaloids cocsuline,
isotetrandrine, stebisimine, gilletine (a menisarine-cocsuline type alkaloid), trigil-
letimine, tricordatine and tridictyophylline have been isolated, as well as phaean-
thine and Af,Af-dimethylphaeanthine (Dwuma Badu etal., 1975b, Spiff et al., 1981).
In the leaves of T. patens, phaeanthine, A/Âf-dimethylphaeanthine, cocsuline,
pycnamine and aromoline were found to be present, as well as an oxo-aporphine
alkaloid, O-methylmoschatoline, which is also present in T. dictyophylla (Dwuma
Badu etal., 1975c). In T. subcordata the dimeric isoquinoline alkaloids fanchinoline,
tricordatine, cocsuline, tetrandrine and phaeanthine have been reported (Kronlund
et al., 1970; Tackie et al., 1973a, 1974a; Dwuma Badu et al., 1975b, c, 1978;
Sandberg, 1980; Spiff et al., 1981).
Phaeanthine has been shown to have one-ninth of the curarizing potency of
100
(+)-tubocurarine. The activity of the dimethiodide is greater and dimethylphaean-

thine is also an effective skeletal muscle relaxant. Antitumour tests revealed a weak
antitumour activity for phaeanthine, no activity for isotetrandrine and slight activity
for fanchinoline, a 6-hydroxy analogue of tetrandrine. Methylation with
diazomethane of fanchinoline produced tetrandrine with significant antitumour
action (Guinaudeau et al., 1975).
Epinetrum cordifolium Mangenot et Miege MENI SPERM ACE AE

The local uses of this plant are the treatment of anaemia and of oedema of the legs
(Debray, 1966; Debray etal, 1966).
In this species, which is also a member of the Tricliseae tribe, Debray et al. (1966)
identified cycleanine (a dimethyl-o-o-isochondrodendrine), norcycleanine (a mono-
methylisochondrodendrine) and isochondrodendrine.
The alkaloids of E. cordifolium have curare action, producing muscle relaxation.
Cycleanine also has anti-inflammatory and analgesic properties (Debray, 1966;
Debray et al., 1966; Bouquet and Cave, 1971; Guinaudeau et al., 1975).
Erythrina senegalensis DC. FAB ACE AE

Erythrina vogelii Hook. f.
Erythrina excelsa Bak. syn. (E. sereti de Wild.)
Erythrina sigmoidea Hua syn. (E. dybrowski Hua, E. erythrotricha Harms)
Erythrina mildbraedii Harms syn. (E. altissima Chev.)
In Northern Nigeria the bark of Erythrina spp. is chiefly used in the treatment of
jaundice, as an infusion for gonorrhoea and as a diuretic for horses. In Ghana the
bark is recommended as an emmenagogue, and in Guinea it is given to women after
childbirth (Dalziel, 1937). In Senegal the bark is considered a remedy for dysentery
and colitis (Kerharo and Adam, 1974).
The first curarizing Erythrina alkaloid was obtained in 1937 by Folkers and Major
from the seeds of E. americana (Folkers and Unna, 1939). It was named erythroidine
and was subsequently shown to be a mixture of two isomers, a- and /3-erythroidine
(Folkers and Koniuszy, 1940; Folkers et al., 1941). In a systematic investigation of
50 species of Erythrina, all were shown to contain alkaloids with curariform activity
(Raven, 1974). Many of the species examined contained as their main alkaloids
erysodine, erysovine (11-methoxyerysodine), erysotrine and erysopine. In addition,
11-hydroxy-erysodine and erythroline have been mentioned (over 30 alkaloids are
known). A number of the alkaloids have phenolic groups, others such as
erysothiopine and erysothiovine are in the form of sulpho-acetic esters (Paris and
Moyse, 1969, p. 404; Hargreaves et al., 1974) or of glycosides and are only liberated
by hydrolysis. A variation in the alkaloid content of different samples of seeds of the
same species collected at different times and locations has been noted (Barakat et al.,
1977). Alkaloids are present in the roots, stems, leaves, heartwood and flowers of
most species but in smaller quantities than in the seeds (Krukoff, 1977; El Olemy et
al., 1978; Staunton, 1979). Games et al. (1974) indicated that in E. senegalensis
erysodine represented 75% of the total alkaloids and oxo-erysodine 9%; in E. excelsa
101
48% of the total alkaloids is represented by erysodine and 35% by erysovine and in
E. sigmoidea 43% of the total alkaloids is erysodine, 28% is erysovine and 21% is
erythraline. The seeds from E. mildbraedii collected in Nigeria contain mainly
erysodine, and to a lesser extent erythraline and erysopine (El Olemy et aL, 1978).
In addition, secondary Erythrina alkaloids and in most species hypaphorine have also
been reported (Games et aL, 1974).
The cur arizing action, based upon the grams of frog curarized per gram of seed, has
been examined by Folkers and Unna (1939). This relationship was 20000 for E.
senegalensis and 44000 for E. sigmoidea. Erythroidine and its more potent derivative,
dihydroerythroidine, have been used as muscle relaxants in a number of clinical
applications such as the control of convulsions, in the shock therapy of psychiatric
patients and as an adjunct to general anaesthesia to produce the muscular relaxation
desirable in some surgical operations (Folkers et al., 1941; Bhattacharya et al., 1971).
The alkaloids have the advantage of being active if taken by mouth but are less active
than curare. They are quaternary bases and their action is less lasting as they lose
their activity through bio transformation to ternary bases. They have, however, now
been replaced by other drugs because of their high toxicity. Neuromuscular
blocking, smooth muscle relaxant, CNS depressant, hydrocholeretic and anticon-
vulsant effects are also described (Bhattacharya et al., 1971; Ghosal et aL, 1972; El
Olemy et al., 1978). In general, it was reported that erysothiovine and erysothiopine,
the sulpho-acetic esters of erysovine and erysopine, possess greater activity than the
free alkaloids (El Olemy et aL, 1978).
Stephania dinklagei (Engl.) Diels syn. (Cissampelos dinklagei Engl.)

MENISPERMACEAE
The roots are used by local West African healers as a sedative, an anthelmintic and
an antimenorrhagic (Dalziel, 1937) and also in the treatment of infertility (Tackie et
aL, 1974b).
Analysis of the roots has revealed six alkaloids of the aporphine and isoquinoline
group. Cory dine (also found in several species of Papaveraceae and in the rootbark
of some Zanthoxylum spp.) is the most abundant as 0.27% are found in the roots
(Tackie et aL, 1974b). Dinklageine, norcorydine, stephanine, steporphine and
stephalagine have also been reported and most of them identified by thin-layer
chromatography (Paris and Le Men, 1955; Ray et al., 1979a). Dinklageine shows
many structural analogies with biscoclaurine (from Cocculus laurifolius) but has a
higher melting point. In addition, 7V-methyl-glaucine and Af-methylcorydine have
been reported in 5". dinklagei roots (Dwuma Badu et al., 1980).
Another alkaloid fraction of S. dinklagei (possibly a mixture of isocorydine and
decentrine) has been reported to be an excitant of the CNS, acting on the cerebral
but not the medullary centres. On the ANS it has a peripheral and central
sympathetic action (Quevauviller and Sarasin, 1967).
Cory dine produces slight narcosis, slows down the heart and respiration rates and
causes emesis in warm-blooded animals. As with other aporphines small doses have
sedative and hypnotic action (Henry, 1949). S. dinklagei is said to be used as an
102
antitussive (Tackie et al., 1979). An infusion of the roots of S. dinklagei has distinct
antispasmodic properties in the isolated rabbit intestine at concentrations of l%o and
above. At 4%o, there is a drop of tone and arrest of peristalsis. In the intestine of the
guinea pig contracted by acetylcholine or barium chloride, decontraction is
immediate with a concentration of 5%o (Paris and Le Men, 1955). Several Asiatic
species of Stephania contain coclaurine and related alkaloids. Rotundine from S.
rotunda was used as a narcotic and hypnotic in the Vietnam war. Rotundine and
(+)-isocorydine are considered to be spasmolytic and analgesic in Chinese medicine
(Xiao, 1983). From 5. cepharantha Japanese workers isolated cepharanthine, used in
Japan for the treatment and prophylaxis of tuberculosis and leprosy (Biichi, 1945).
Cycleanine from S. glabra (Caucasus) in addition has anti-inflammatory properties
(Khanna et al., 1972) and epistaphine from the aerial parts of S. hernandifolia (India)
was found to possess significant adrenergic neurone blocking activity, like
guanethidine (Ray et al., 1979b).
Desmodium gangeticum (L.) DC. var. gangeticum syn. (Hedysarum gangeticum L.)
FABACEAE
In India the plant is regarded as an antipyretic and anticatarrhal (Dalziel, 1937). The
leaves are used in Liberia to bathe a child having convulsions (Harley, 1941).
Twelve alkaloids consisting of carboxylated and decarboxylated tryptamines, /3-car-
bolines and /3-phenylethylamines have been isolated from different parts of
D. gangeticum at different stages of its development (Ghosal and Bhattacharya,
1972). The aerial portion of the plant contained 2-indole-3-alkylamines, Af-methyl-
tetrahydroharmine and 6-methoxy-2-methyl-/3-carboline. The alkaloid content in
fresh material was three times that found in the dried plants (Ghosal and Bannerjee,
1968).
The total alkaloid fraction of the stems and leaves of D. gangeticum collected in India
exhibited curariform activity on the rectus muscle of the frog (Bhattacharya and
Sanyal, 1976). The total alkaloid fraction also has an inhibitory effect on the isolated
frog heart, and a relaxant effect on the smooth muscles of the rabbit and dog and on
the isolated rat uterus. It is non-toxic and has a mild diuretic effect as well as an
inhibiting action on respiration (Prema 1968; Ghosal and Bhattacharya, 1972). The
aerial portions of the plant were reported to have anticholinesterase activity and to
induce smooth muscle stimulant, CNS stimulant and depressor responses. The
roots of the plant produce a nicotine-like effect on the dog intestine and on the
carotid blood pressure. This has been attributed to the presence of catecholamine
releasers, tertiary phenylethylamines and candicine. In addition, the aqueous
extract of the roots has shown anti-inflammatory, antibacterial and antifungal
activities.
Mucuna pruriens (L.) DC. var. pruriens FABACEAE
Cowhage, cow-itch
The spicular hairs of the pods penetrate the skin, causing intense irritation. They
have been used in Senegal as an anthelmintic prepared as an electuary with treacle or
honey (Sebire, 1899).
103
It has been shown that the hairs contain 5-hydroxytryptamine (serotonin) and that
the itching produced by the hairs is due to the liberation of histamine in the
epidermal layer of the skin (Broadbent, 1953; Bowden et al., 1954). In the leaves,
fruits and seeds, four indole-3-alkylamines (A/^JV-dimethyltryptamine, two deriva-
tives and bufotenine), a 5-oxindole-3-alkylamine and a /3-carboline have been
reported as well as choline (Ghosal et al., 1971). In the seeds a sterol, a fatty acid, two
alkaloids, mucunine and mucunadine, and two water-soluble bases, prurienine and
prurieninine had previously been found (Majumdar and Zalani, 1953) and L-DOPA
has been obtained from the seeds (Bell et al., 1971; Ghosal et al., 1971).
The indole bases have been shown to have an unspecified spasmolytic action on
spasms induced in smooth muscles by acetylcholine, histamine or oxytocin. Two of
them, 5-methoxy-A/Â^dimethyltryptamine and 5-oxyindole-3-alkylamine, pro-
duce a block of a tubocurarine type and indole-3-alkylamine causes blockade of the
striated muscle of the frog abdomen. In the anaesthetized dog, 5-oxindole-3-
alkylamine and 5-methoxy-Af, JV-dimethyltryptamine cause severe depression of
respiration and the blood pressure with spasm of the bronchi, which can lead to
death. In the rat, to the contrary, they induce hyperactivity (Ghosal et al., 1971). In
view of the presence of L-DOPA and serotonin in the plant, its possible use in
Parkinson's disease has been suggested (Bell and Jansen, 1971). The plant also has a
hypoglycaemic and cholesterol lowering effect (Pant et al., 1968).
IV Plants with cholinergic and adrenergic actions

Plants with a depressant or stimulant action on the nervous system that
have been described in Chapter 2 (CV) are mentioned after those described below.
The plants listed first are those acting on mixed receptor sites affecting both
autonomically and centrally innervated organs and tissues.
Acetylcholine liberated from motor nerve terminals transmits the nerve impulse
across a synaptic gap to the end plate region of skeletal muscle cells. Acetylcholine
also acts as a neurotransmitter at Renshaw cells in the spinal cord, at autonomic
ganglia and at motor terminals on smooth muscles.
Cholinergic drugs can act on muscarinic or nicotinic receptors. The action on
muscarinic receptors resembles the effect of stimulating the parasympathetic nerv-
ous system and can be blocked by atropine. The effects on the nicotinic receptors are
blocked by curare. Among the neurological complaints treated by anticholinergic
plants is Parkinson's disease, which is characterized by involuntary movements and
a depressive state. It is attributed to a disturbance in the functioning of the Corpus
striatum in the brain controlling muscular tonicity. It was shown that acetylcholine
stimulates the extrapyramidal nerve cells and tropane alkaloids with anticholinergic
action were therefore used in the treatment of this condition. Further observations
showed that the dopamine concentration was reduced in the Corpus striatum of
patients with idiopathic and post-encephaletic Parkinsonism, numerous trials with
L-DOPA were carried out and this was considered to be a drug of choice (Turner and
Richens, 1978).
The use of tropane alkaloids with anticholinergic action in the treatment of
Parkinsonism explains the use in neurology of several spp. of Solanaceae, e.g. Datura
104
spp., with (-)-hyoscyamine (see encephalic stimulants); Solarium nigrum with

solanine, which has anticholinesterase action and which is also analgesic and sedative
to the CNS; and Withania somnifera, which also has sedative and narcotic action on
the CNS. Boerhavia diffusa (Nyctagynaceae) is parasympatholytic and anticonvul-
sant and analgesic to the CNS. Tetrapleura tetraptera andSecuridaca longepedunculata
have sedative, tranquillizing and anticonvulsant properties which could be attri-
buted to oleanolic acid glycoside. Anthodeista procera and A. djalonensis are hypoten-
sive and also sedative and analgesic, probably through swertiamarin.
The aporphine alkaloids of many Annonaceae, e.g. Uvariopsis guineensis, Enantia
chlorantha, Isolona campanulata, Polyalthia oliveri, Annona muricata and
Pachypodanthium staudtii, show different degrees of antispasmodic activity, some-
times accompanied by sedative action on the CNS. Some of these plants have found
use in the treatment of mental disease, e.g. Enantia chlorantha, with isocorydine, in
paralysis agitans and Polyalthia oliveri, with oliveroline, has anti-Parkinson activity
in mice. In Isolona campanulata isochondrodendrine and curine are found as well as
aporphine alkaloids. In Stephania dinklagei (see above) isocorydine and other
aporphine alkaloids have also been reported.
Antispasmodic action on the ANS was found in Euphorbia hirta used in the
treatment of asthma; the active constituent is probably shikimic acid. Uncaria
africana (Rubiaceae) is said to have antispasmodic and sedative action. Alchornea
cordifolia contains a sympatholytic alkaloid which is used as a spasmolytic and the
flowers of Grewia bicolor and spp. contain a sedative essential oil, farnesol.
Pentaclethra macrophylla (Mimosaceae) and Newbouldia laevis (Bignoniaceae) are
anticholinergic and have been used locally in the treatment of epileptic fits in
children. Lantana camara (Verbenaceae) reported as an antispasmodic, has proved
to be too toxic.
Stimulant action on the ANS was noted with Cissus quadrangularis (Vitaceae)
(cholinergic), Sida cordifolia (Malvaceae) (adrenergic) and Crateva religiosa (Cap-
paridaceae) and perhaps with Borreria verticillata (Rubiaceae) and Cardiospermum
halicacabum (Sapindaceae).
(a) Depressants acting on both ANS and CNS terminals
Solanum nigrum L. syn. (S. nodiflorum Jacq., S. guineense (L.) Lam.)

SOLANACEAE
The berries are used in India in the treatment of fever, diarrhoea and eye diseases
(Chopra et al.9 1956). In Nigeria a decoction of the leaves is said to be diuretic and
laxative and that of the young shoots is given in the treatment of psoriasis and skin
disease (Dalziel, 1937).
In the fruit, solanine has been found (especially in the green fruit). Hydrolysis of
solanine produces glucose, rhamnose and solanidine. In addition, heterosides
derived from spirosolane (the genin being solasodine) are present: solasonine,
solamargine and solanigrine (Henry, 1949; Paris and Moyse, 1971).
In the French Pharmaceutical Codex 1937, S. nigrum is used in 'Huile de Jusquiame'
105
and a poultice of the leaves is used in France as an emollient and antineuralgic and
has a slightly narcotic action (Paris and Moyse, 1971, p. 190). Solanine is reported to
be a cytostatic and a cholinesterase inhibitor in vitro (Manske and Holmes, 1950-71,
Vol. 10, p. 116). It is also considered to be analgesic for migraine and gastralgia, and
a nervous sedative for paralysis agitans and for chronic pruritus in certain skin
diseases (Denoel, 1958, p. 899). It is also said to have antimitotic action (Danneberg
and Schmal (1953) quoted in Paris and Moyse (1971). Solasodine is antagonistic to
tachycardia provoked by adrenaline (Sollmann, 1957, p. 669).
Withania somnifera L. Dunal syn. (Physalis somnifera L.) SOLANACEAE

In West African local medicine, both roots and leaves are used internally, and the
freshly pounded leaves also externally, against fever, chills, rheumatism, colics, etc.
The juice of the plant is said to be diuretic and emmenagogic. In local medicine in
East Africa, the root is considered to have narcotic and antiepileptic actions (Pichi
Sermoli, 1955). In India, the bruised leaves and ground root are used as a local
application to painful swellings, carbuncles and ulcers as the root and leaves are
considered to be sedative and the root has been included in the Indian Phar-
macopoeia and Codex for its narcotic and sedative properties (Chopra el al., 1956;
Oliver, 1960).
The roots contain choline, tropanol, pseudotropanol, 3-tigloyl-hydroxy-tropane,
cuscohygrine, (±)-isopelletierine, anaferine and anhygrine. In the leaves, with-
aferine (5,6-epoxy-4/3,22,27-trihydroxy-l-oxo-5/3-ergosta-2,24-dien-26-oic acid 8-
lactone) has been detected (Khanna el a/., 1963; Schwarting el al., 1963; El Olemy
and Schwarting, 1965; Lavie el al., 1965). Although the total alkaloid content
appears high, the alkaloids resinify during extraction and the yield in pure sub-
stances is low. Schroter el al. (1966) isolated withasomnin (4-pheny 1-1,5-
trimethylenepyrazole) from the roots.
Withasomnine showed distinct sedation in mice and induced sleep and narcosis in
higher doses. The acetone-soluble fraction of the leaves, when given perorally, had
a mild depressant effect (tranquillizer-sedative type in dogs, albino rats and mice).
It exacerbated the convulsions produced by metrazol but protected against supra-
maximal electroshock seizures in rats. It had no analgesic activity in rats and
produced hypothermia in mice. There was potentiation of barbiturate-, ethanol- and
urethane-induced hypnosis in mice which could not be antagonized by lysergic acid
diethylamide and dibenzylene. The two other fractions had no significant
neuropharmacological actions and were devoid of irritant effect on mucous mem-
branes (Prasad and Malhotra, 1968). The effect of the total extract on the smooth
muscles, cardiovascular system, respiration and skeletal muscles had been studied
earlier by Malhotra el al. (1960a, b). Other authors obtained no therapeutically
useful sedation in animal tests. Watery, 50% methanol or absolute methanol extracts
with and without pre-extraction in amounts up to 1 g/kg neither reduced the central
activity nor affected rats in motility tests. Even with doses of 5 g/kg the different
Withania extracts produced no sedation (Fontaine and Erdos, 1976). Withaferine
has been reported to have antitumour action and to delay the onset of arthritis in rats.
106
It is also antibiotic towards Gram-positive organisms and certain fungi (Shohat,

1967).
BoerhaviadiffusaL. syn. (partlyB. repensvar. diffusa(L.)Hook.,partlyB. adscen-

dens Willd.) (Fig. 3.4) NYCTAGYNACEAE
Hog weed, Punarnava
The plant is used in local medicine to treat convulsions and as a mild laxative and
febrifuge. The roots and leaves are considered to have an expectorant action, to be
emetic in large doses, and are of use in the treatment of asthma. The thick roots,
softened by boiling, are applied as a poultice to draw abscesses and to encourage the
extraction of guinea worms (Dalziel, 1937).
An alkaloid, punarnavine (0.04% in the roots), has been extracted, as well as
boerhavic acid, reducing sugars, potassium nitrate and tannins including
phlobaphens (Oliver, I960; Singh and Udupa, 1972a). Extracts fromi?. diffusa and
B. repens are official in the Indian Pharmacopoeia as a diuretic (Chopra et al., 1956).
In addition a nucleoside, hypoxanthine-9-L-arabinofuranoside, has been isolated
from the roots of B. diffusa (Ojewole and Adesina, 1983).
Intravenous injection of punarnavine produces a distinct and lasting rise in the blood
pressure of cats, with marked diuresis (Chopra et al.9 1956). Clinically, doses of
4-16 g of a liquid extract prepared from the fresh plant produced diuresis in 33
patients with oedema and ascites and seemed extremely active particularly in cases
of cirrhosis of the liver and chronic peritonitis (Chopra and Ghosh, 1923). Mudgal
(1975) confirmed the diuretic effect and also reported anti-inflammatory activity.
Fig. 3.4. Boerhavia diffusa L.

107
An active anticonvulsant principle was localized in the roots of B. diffusa

(Adesina, 1979). Test solutions were prepared by methanpl extraction of the roots,
dissolution in water of the residue after evaporation, extraction with petroleum ether
and lyophylization of the water-soluble portion. Intraperitoneal injections of this
extract have shown anticonvulsant as well as analgesic properties on male albino
mice with leptazol-induced convulsions. While the control animals died from
convulsions within 2-3 min, a 1 g/kg dose of the extract gave 20% protection, and
with 1.5-2.0 g/kg doses all animals were protected for over 10 min, 60% eventually
dying (Adesina, 1979).
Further tests with the nucleoside isolated from the roots showed that, like inosine
and adenosine, it relaxes the isolated coronary artery of the goat contracted with
potassium chloride. The action, like that of inosine, is thought to be 'a direct
vasodilator effect, not involving vascular adenosine receptors' (Ojewole and
Adesina, 1983). (Also see Singh and Udupa, 1972b, c.)
Tetrapleura tetraptera (Schum. & Thonn.) Taub. syn. (Adenanthera tetraptera

Schum. & Thonn., T. thonningi Benth.) (Fig. 3.5) MIMOSACEAE
An infusion of the fruit is used in Nigeria as a tonic and stimulant. The bark is used
in Ghana as a purgative and in Guinea and Senegal as an emetic. Elewuda mentions
that the fruits, with other parts pf the plant, are used as an anticonvulsant drink
(Adesina and Sofowora, 1979).
Fig. 3.5. Tetrapleura tetraptera (Schum. & Thonn.) Taub.
Tet ret pleura, tetraptera.

108
Bouquet (1972) reported the presence of saponosides and perhaps of tannins in the
rootbark of the plant collected in the Congo, but found no flavonoids, quinones,
cyanogenetic glycosides or steroids. Later Adesina and Sofowora (1979) isolated
oleanic acid triglycoside and Ojewole (1983b) obtained scopoletin, a coumarin, from
the fruit.
Alcoholic as well as aqueous extracts of the fruits have been found to exhibit marked
tranquillizing properties on male albino mice and to cause lowering of their body
temperature. Oral doses of an alcoholic extract of the fruit sedated mice within 30-40
min after intraperitoneal injection of a convulsant drug (leptazol) and over 60% of
the animals were protected (Adesina and Sofowora, 1979).
Anti-bronchoconstrictive and anti-arrhythmic effects of scopoletin were recently
demonstrated in vivo and in vitro (Ojewole, 1983b). Scopoletin and tetramethyl-
pyrazine (see Jatropha podagrica) were found to protect guinea pigs from, and to
suppress ouabain-induced arrhythmias, increasing the functional refractory period
of the myocardium in the same way as quinidine. They also relax acetylcholine-,
5-hydroxytryptamine- and histamine-induced contractions of the guinea pig isolated
tracheal muscle (Ojewole, 1983a).
The inhibitory effects of scopoletin on electrically induced contractions, relax-
ations and twitches of cholinergically and adrenergically innervated muscle prep-
arations are thought to be linked with the non-specific spasmolytic action of the
coumarin, and also probably to be exerted via its local anaesthetic (membrane
stabilizing) activity (Ojewole, 1983b, c).
Securidaca longepedunculata Fres. (Fig. 3.6) POLYGALACEAE

Violet tree, wild wisteria, Senega root tree
Pieces of root covered with bark are sold in Hausa markets (Northern Nigeria) as a
charm and a medicine. In small doses this is a drastic purgative and the powdered
root causes violent sneezing. The root is used as a taenifuge and anthelmintic in
French Guinea and Senegal. The seeds are rich in oil and are given medicinally for
febrile and rheumatic conditions (Dalziel, 1937; Oliver, 1960; Kerharo, 1970).
The roots have been shown to contain saponin (0.4%) and 4% methyl salicylate. A
systematic examination of roots gathered in Angola indicated 27% lipids and 0.36%
protides, tannins and steroids. Hydrolysis of the saponoside produced a steroid
genin and glucose. Methyl salicylate was present as a monotropitoside similar to
gaultherin; the sugars were glucose and xylose (Kerharo, 1970).
The saponin was reported to have a certain ichthyotoxicity (Prista and Correia Alves,
1958). The LD 50 lies around a concentration of 0.018% for small sweet water fish
remaining for 24 h in the solution, and all fish died after 24 h in a concentration of
0.024% (Fraga de Azevedo and Medeiros, 1963). Securidaca is one of 24 plants used
in treating convulsions in children. Oral administration of a decoction of the root
produces a sedative effect and several hours of sleep. The active factor appears to be
oleanolic acid glycoside; this is also found in Tetrapleura tetraptera which has the
same sedative properties (Adesina and Sofowora, 1979; Sofowora, 1980).
109
Anthocleista procera Lepr. ex Bureau syn. (A.frezoulsii Chev., A. nobilis Lepr.)

LOGANIACEAE
Anthocleista djalonensis Chev. syn. (A. kerstingiiGilg ex Volkens, A. procera Chev.)
Anthocleista nobilis Don. syn. (A. parviflova Bak.)
Cabbage tree
The seeds and bark of these species are used locally in Nigeria for their antipyretic,
stomachic and purgative actions. Watt (1967) reported that the Abrous (Ghana)
prepare a decoction of the leaves of A. nobilis Don. with lemon as a remedy for
epilepsy (Irvine, 1961). In Casamance (Senegal) the decoctions are used as a diuretic
(Kerharo and Adam, 1974).
From the dried leaves of A. procera, 5% of a bitter monoterpenic heteroside,
swertiamaroside or swertiamarin, has been obtained in the Ivory Coast and in
Nigeria. It has been proved to be the precursor of an earlier-found indole alkaloid in
the leaves and roots, gentianine or erythricine, which is formed from the former by
treatment with ammonia (Canonica, 1962; Lavie etal., 1963; Plat etaL, 1963; Koch
et al., 1964). Gentianine (1%) in crystal form has also been isolated from the dried
leaves (Koch, 1965). Another crystallized compound, anthocleistine, a triterpenic
Fig. 3.6. Securidaca longepedunculata Fres.

110
pentacyclic acid, was obtained by Taylor-Smith (1965) from the NigerianA. procera.
No swertiamarin was found in the leaves of A. djalonensis (Poisson et al., 1972).
The leaves of a non-West African species (A. rhizophoroides) which also contains
swertiamarin were found to decrease nervous excitability and to have a cardio-
moderating action (Poisson et al., 1972). Gentianine (also found in the Gentianaceae)
has low toxicity. The LD 50 of extracted dried leaves in mice is 500 mg/kg subcutane-
ously and 0.5-1.3 g/kg perorally (Steinegger and Weibel, 1951; Koch, 1965). It is
hypertensive in small doses but hypotensive in higher doses, resulting in a reversible
decrease in the blood pressure, which with very high doses may become irreversible.
It also has an inhibitory action on the isolated frog heart, and on the guinea pig ileum
which has been stimulated by histamine or by acetylcholine (Steinegger and Weibel,
1951). Gentianine has a distinct analgesic action in the rat (Keng-Tao Liu et al. in
Koch, 1965). One of the main interests of gentianine lies in its antihistamine and
anti-inflammatory actions, which have been demonstrated on rats and guinea pigs.
Thus, an intraperitoneal injection of 90 mg/kg prevents or considerably reduces the
swelling of the rats' hindlegs when the injection is carried out prior to a subcutaneous
injection of 0.1 ml of ovalbumin or formol, which in the control animals causes a very
slow receding inflammation of the articulations. The injection of gentianine also
protects the guinea pig against a histamine-containing aerosol. In the anti-inflamma-
tory tests, gentianine is more effective than chloroquine and cortisone (Chen-Yu
Sung et al., 1958; Hsiu-Chuan Chi et al., 1959). Gentianine does not influence the
growth of yeast, Candida albicans, Staphylococcus aureus, Bacillus coli orB. anthracis,
nor does it influence the asexual cycle of Plasmodium gallinaceum (Ghosal et al.,
1973). An aqueous extract of A. djalonensis was investigated by Adesogan and
Olatunde (1974) and produced a rise in blood pressure in cats and an increase in tone
and amplitude of movements of rabbit duodenum preparations.
Uvariopis guineensis Keay syn. (Uvaria spectabilis Chev. ex Hutch. & Dalz.)
ANNONACEAE
Guinaudeau et al. (1975) report that from the rootbark of this tree, oxo-aporphines
and open aporphines (uvariopsamine, uvariopsamine-Af-oxide, uvariopsine and
ushinsunine) have been obtained by Leboeuf and Cave (1972a).
The total alkaloids of the powdered root of U. guineensis have antispasmodic
properties similar in strength to those of papaverine but longer lasting. They have
little effect on the CNS (slight analgesic and antipyretic action) but have a sym-
patholytic action on the ANS, producing vasodilatation, and hypotension and a
slight stimulating effect on the secretion of the gallbladder. These observations are
in agreement with the findings for the rootbark (Quevauviller et al., 1977). In
general, the aporphine alkaloids can produce emesis by stimulation of the vomiting
centre. In smaller doses they can have hypotensive, digestive, diuretic and/or
antispasmodic activities. They also have been reported to have sedative and slight
hypnotic action on the CNS. However, the different constituents vary considerably
in their actions and their respective effects also vary according to the dose used
(Guinaudeau et al., 1975).
Ill
Enantia chlorantha Oliv. ANNONACEAE

African yellow wood
Bark extracts are used in local medicine in different West African countries as an
antipyretic and are also applied to ulcers and as a haemostatic to wounds (Dalziel,
1937).
The main alkaloids from the root- and stembarks are quaternary protoberberines:
palmatine, bebeerine, jatorrhizine and columbamine. Two oxyaporphines (O-
methyl moschatoline and lysicamine) have also been isolated from the bark of the
roots. In the leaves, flavonic heterosides and the alkaloids atherospermine and
argintinine and the phenanthrene alkaloids (open aporphines) have been reported
(Leboeuf and Cave, 1972b; Hannoniere et al., 1975). From the leaves of
E. polycarpa, Leboeuf and Cave (1972b) isolated 1.8% of total alkaloids of which the
the main alkaloids, L-(+)isocorydine (aporphine group), had been previously
reported in species of Stephania and in the families Papaveraceae and Rutaceae but
never in such high proportion.
Palmatine has been shown to have an antipyretic effect as well as a depressive action
on the arterial blood pressure and the nervous system (Beauquesne, 1938).
Isocorydine, which is also present in several other species of Annonaceae, induces
(like bulbocapnine) catalepsy. This led to its use in the treatment of diseases in which
involuntary movement is a symptom as in the case in paralysis agitans and St Vitus
dance (Raymond-Hamet, 1936; Henry, 1949, p. 313).
Isolona campanulata Engl. & Diels syn. (/. leonensis Sprague and Hutch., / . sou-
breana Chev. ex Hutch. & Dalz.) ANNONACEAE
In the Ivory Coast, the bark of the roots and stem is given during pregnancy and for
the treatment of bronchial infections, skin diseases, fever, haematuria and bilharzia
(Oliver, 1960).
The bark of the roots and trunk contains 0.2% and 0.3% of total alkaloids,
respectively. Six aporphine alkaloids have been isolated and identified: anonaine,
nor-nuciferine, oliveridine, oliverine, Af-oxy-oliverine and liriodenine. Two of the
alkaloids, oliverine and oliveridine, are present in major amounts. In addition, there
are two neutral constituents, a triterpene (polycarpol) and an indole-terpene. In the
stembark isochondrodendrine and curine have been reported. The species is thus
characterized by virtue of its containing aporphine alkaloids and showing an analogy
in its composition with some Enantia spp. (Leboeuf and Cave, 1972b; Nicto et al.,
1976; Hockemiller etaL, 1977, 1978).
In view of the alkaloids reported, an antispasmodic effect on the skeletal muscles and
a depressive action on the ANS can be expected.
Polyalthia oliveri Engl. syn. (P. acuminata Oliv.) ANNONACEAE

The Mendes tribe are said to use a decoction of the bark for blackwater fever. In
Liberia, an infusion of the bark is used as an anthelmintic and in the Cameroons, a
cold infusion of the bark is drunk for stomach troubles (Dalziel, 1937).
Eleven aporphine alkaloids and some terpenes were found in the rootbark and leaves
of this small tree. The main alkaloids of the rootbark are oliveridine and oliverine,
112
whilst in the leaves mainly oliveroline has been reported (Hannoniere et al., 1974,
1975).
Oliverine has been shown to have antihypotensive action whilst oliveridine is only
hypotensive through relaxation of the vascular smooth muscles, comparable in this
to the effect of papaverine. Oliveroline has antiparkinson activity in mice (distinct
dopaminergic effect). This activity is weaker in oliveridine and non-existent in
oliverine, thus indicating that methylation of one OH group (in position 7)
decreases, and methylation of two OH groups (in positions 7 and 9) causes the
disappearance of the activity of oliveroline (Quevauviller and Hannoniere, 1977).
Annona muricata L. ANNONACEAE

Sour sop
Annona reticulata L.
Custard apple, bullocks heart
Introduced and naturalized in many places, these species are natives of tropical
America and the West Indies. A decoction of the leaves of A. muricata is used as a
soothing and sudorific remedy for fever, whilst the pounded fresh leaves are applied
to cicatrize wounds. In general, the leaves are considered a useful treatment for fever
and dysentery (Dalziel, 1937). In India, the rootbark is given in ptomaine poisoning
(Nadkarni, 1954). The leaves of A. reticulata are considered in popular medicine to
be an insecticide and anthelmintic and the fruit an antidiarrhoeic. In Ghana,
A. arenaria is used as a remedy for epilepsy (Watt and Breyer-Brandwijk, 1962).
From the leaves and stems of A. reticulata, anonaine, roemerine, corydine,
isocorydine and many other aporphine alkaloids have been isolated (Guinaudeau et
al., 1975). In addition L-dopamine, salsinol(l-methyl-6,7-dihydroxy-l,2,3,4-tetra-
hydroquinoline) and coclaurine have been identified by thin-layer and gas chromato-
graphy (Forgaes et al., 1981). y-Aminobutyric acid has been found in the fruit and
stems of A. muricata (Durand et al., 1962) and in the leaves also two phytosterol
glycosides, ipuranol and anonol, have been reported to be present (Merck, 1976).
From the roots, two alkaloids, muricine and muricinine, have been isolated (Meyer,
1941; Manske and Holmes, 1950-71, Vol. IV, p. 142). The main alkaloids which
have been obtained from the roots of A. muricata from Guyana are (H-)-reticuline and
(+)-coclaurine. Three minor alkaloids of the isoquinoline type, coreximine,
anomurine and anomuricine, have also been reported (Leboeuf et al., 1980).
Hydrocyanic acid has been found in variable amounts in the roots, leaves and mainly
in the bark (Merck, 1976). From the leaves and stems of A. squamosa, a benzyl-tetra-
hydro-isoquinoline alkaloid, higemanine, has been isolated (Leboeuf et al., 1981); it
had been found earlier in Nelumbo nucifera seeds and is an effective adrenergic
agonist.
The constituents of A. reticulata. explain the cardio tonic activity of the plant which
is inotropic and chronotropic and also spasmolytic (Forgaes etal., 1981). An extract
of the leaves and stems of A. muricata has a passing depressive effect on the blood
pressure, which has been attributed to y-aminobutyric acid (Durand et al., 1962).
Intraperitoneal administration of this acid (3 g/kg) has been shown to protect animals
against the convulsive acid of brucine if it is given three days beforehand (Sorer and
113
Pylko, 1965). Intracerebroventricular administration of 25 /z-g (+)-coclaurine in

mice suppresses or prevents the locomotor activity induced by dopaminergic
stimulating agents (Watanabe et al., 1981). An insecticidal principle, resistant to
heat but not to saponification, has been detected in the seeds of A. muricata; it was
effective against a great number of insects (Heal and Rogers, 1950). The screening
of different extracts of the plant as to its anticancer action gave no significant results
(Abbot et al., 1966), although in related species, such as A. squamosa, aporphine
alkaloids isolated from the bark (Bhakuni et al., 1972) and constituents of the bark
of A. senegalensis were found to have significant antineoplastic activity (Durodola,
1975; Adesogan and Durodola, 1976).
Pachypodanthium staudtii Engl. & Diels ANNONACEAE

The bark was formerly used as an arrow poison and, in Liberia, medicinally. In the
Congo, the bark is also considered to be analgesic and odontalgic, and a decoction is
used in coughs and dyspnoea by certain tribes (Bevalot et al., 1976).
Seven isoquinoline alkaloids have been isolated from the bark: two tetrahydroproto-
berberines, corypalmine and discretine; and oxo-aporphine, liriodenine; three
aporphines, pachypodanthine (7-methoxy aporphine), pachystaudine and nor-
pachystaudine (4-hydroxy-7-methoxy aporphine), and a new alkaloid, staudine,
which proved to be the result of the combination of jateorrhizine (a protoberberine
alkaloid) and 2,4,5-trimethoxysterine (Bevalot et al., 1976, 1977; Cave et al., 1980).
Earlier, a flavonic genin, dihydroxy-5,4'-trimethoxy 3,7,3'-flavone had been iso-
lated from the stem- and rootbark by Cave et al. (1973). An unusual neutral
constituent, trimethoxy-2,4,5-styrene, which might be identical with the
trimethoxystyrene obtained from Piperomia lucida, was found to be present in
Pachypodanthium confine and in P. staudtii (Bevalot et al., 1976).
P. staudtii is said to have an excitant action on the nervous system; it produces
peripheral vasodilatation and has a weak spasmolytic action of the papaverine type
(Bevalot et al, 1976).
(b) Antispasmodics acting mainly on sympathetic terminals
Euphorbia hirta L. syn. (E. pilulifera Chev.) (Fig. 3.7) EUPHORBIACEAE

Australian or Queensland asthma herb
In the native medicine of Nigeria, the plant is used in an enema for constipation and
in the treatment of dysentery. The latex is squeezed into the eye to cure eye troubles.
Extracts of the dried entire plant are mentioned in the British Extra Pharmacopoeia
(27th edn) for asthma and the treatment of coughs. In Konakry hospital, good
results were achieved with a decoction of the fresh plants in cases of acute enteritis
and dysentery (Dalziel, 1937).
Analysis of the latex has revealed (-)-inositol, pyrogallic and catechuic tannins and
the alkaloids xanthorhamnine (Oliver, 1960). Gupta and Garg (1966) found taxerol,
friedelin, /3-sitosterol, myricyl alcohol, ellagic acid and hentriacontane in extracts of
the stem whilst Blanc et al. (1972) reported ellagic, gallic, chlorogenic and caffeic
114
acids, kaempferol, quercitol, quercitrin (as genin of a heteroside), and a number of

amino acids.
Early pharmacological trials seemed to indicate the presence of two active principles,
one with an antispasmodic action on smooth muscles and one with a spasmodic or
histamine potentiating action (Hallet and Parkes, 1953). In 1978, these two pharma-
cologically active constituents were isolated and identified. The relaxing principle
was identified as shikimic acid and the contracting principle as choline. iso-Inositol,
glucose and sucrose were also reported (El Nagger et aL,1978). An ethanolic extract
of the above-ground portion of the plant produced relaxation of the guinea pig ileum.
This extract, containing shikimic acid, was used in the treatment of asthma,
hay fever, bronchitis and other respiratory conditions. It was shown to have an
antispasmodic effect on the smooth muscles of mice and guinea pigs (Hellerman and
Hasleton, 1950). A clinical trial on 53 patients with amoebic dysentery and later on
150 cases of dysentery in Upper Volta, the Ivory Coast and Madagascar showed 83%
cure. There was no relapse for 5-12 months following the oral course. The substance
was perfectly tolerated and was put on the market in France and the USA
(Socambine) (Martin et al., 1964; Ridet and Chartol, 1964) but its use has since been
abandoned (Kerharo and Adam, 1974). The alcoholic extract of the whole plant had
an anticancer action against Friend leukaemia virus in mice. It also showed
hypoglycaemic action in albino rats and an antiprotozoal effect (Dhar et al., 1968).
Fig. 3,7. Euphorbia hirta L.

115
The maximum dose of the total extract, given perorally, that was tolerated in mice
was 1 g/kg. Purification of the total extract led to a new extract with a twenty times
higher activity against Entamoeba histolytica. Further purification is in progress
(Ndir and Pousset, 1981). Irritant and carcinogenic phorbol esters have been
reported to be present in the stem latex (Ayensu, 1979).
Uncaria africana G. Don. var. africana; Uncaria africana var. angolensis Havil.
syn. (U. talbotti Wernh., U. angolensis (Havil) Welw. ex Hutch. & Dalz.)
RUBIACEAE
The bark of these spp. is chewed as a remedy for coughs (Lane Pool, in Dalziel, 1937)
and has been used for the treatment of stomach pains and syphilis (Staner and
Boutique, 1937).
Some forty alkaloids have been identified in Uncaria spp. They are mainly of the
hetero-yohimbine and corresponding oxindole types although pyridino-
indoloquinolizidines (e.g. angustine) and harmane are also present. Rhynchophyl-
line, rotundifoline and isorhynchophylline, etc. have been reported as well as
gambirine and roxburghines (the latter in extremely limited quantities) as could be
expected in view of the close relation with the genus Mitragyna (Merlini et al., 1972;
Phillipson^tf/., 1973; Phillipson and Hemingway, 1973, 1975).
Antispasmodic and sedative action is attributed to the 'hooked thorns' of the plant
(Kariyone, 1971). The related U. rhynchophylla (not found in West Africa) is,
according to the dose administered, reported to have either muscle-relaxant or
muscle-stimulant activity (Harada and Ozaki, 1978,1979).
Alchornea cordifolia (Schum. & Thonn.) Mull. Arg. syn. (Schousboea cordifolia
Schum. & Thonn., A. cordata Benth.) EUPHORBIACEAE
Alchornea floribunda Mull. Arg.
The root of A. floribunda, called niando in the Congo region (Zaire) is used by the
Africans as a stimulating intoxicant and aphrodisiac. After reducing it to a powder,
it is either mixed with food or macerated for several days in palm wine and consumed
to provide energy for tribal festivities or warfare. It is said to provide a state of intense
excitement followed by a deep, sometimes fatal, depression. It is further considered
an excellent remedy for urinary, respiratory and intestinal disorders (Dalziel, 1937;
Oliver, 1960).
According to their origin (Ivory Coast, Guinea) and the time of conservation, the
root and bark of A. cordifolia have been found to contain 0.03-0.26% of total
alkaloids: the highest amounts were found in the most recent samples (Bennet,
1950). Thin-layer chromatography revealed two principal alkaloids, closely related
to but not identical with yohimbine (Paris and Goutarel, 1958). Ferreira et al.
(1963b) found in the roots of the plant in Portuguese Guinea 0.07% of alkaloids
together with gentisic and anthranilic acids and suggest that gentisic acid could be a
possible precursor in the biosynthesis of yohimbine. In addition, in the leaves and
bark of this species, 10% and 11% of tannins, respectively, have been found (Bennet,
1950).
116
The extract of the roots of A. floribunda has sympatholytic activity (Raymond-

Hamet, 1933). It considerably increases the sensitivity of the nervous system
towards adrenaline. In the dog, doses of 0.5 g/kg produce a slight hypotension,
followed by a slight hypertension. Higher doses produce a gradual decrease of the
carotid pressure, which returns only very slowly to its original value (Raymond-
Hamet, 1954). A patent has been obtained for the use of the leaf alkaloid as a
spasmolytic (Goutarel R. Brevet francos 2087982 of 5.5.1970). Guedel (1955)
obtained positive results in clinical experiments with root and leafy stem extracts in
the treatment of icterus in Abidjan.
Grewia bicolor Juss. syn. (G. salvifolia Heyne ex Roth.) TILIACEAE

Grewia carpinifolia Juss. syn. (Vinticena carpinifolia (Juss.) Burret)
Grewia lasiodiscus K. Schum. syn. (G. kerstingii Burret, Vinticena lasiodiscus
(Schum.) Burret, V. kerstingii (Burret) Burret)
The Grewias have edible fruits (sometimes made into a fermented drink). The shoots
of G. carpinifolia are given to sheep at lambing to help delivery (Irvine, 1930) and
women put the roots in soup when approaching childbirth (Dalziel, 1937).
The roots of all three species contain mucilage and catechuic tannins. In G.
carpinifolia gallic tannins are also reported. The barks of all spp. were found to
contain amines (aspartic acid and probably proline) but no alkaloids, quinones,
saponosides or histamine-like substances were reported. The flowers, like those of
other Tiliaceae, contain farnesol (Paris and Theallet, 1961).
The bark extract of the Grewia spp. has a more or less distinct depressive action on
the guinea pig ileum. This is contradictory to the effect observed on rat or rabbit
duodenum (Paris and Theallet, 1961). The action appears to be directly muscular,
and the authors suppose that the active principle belongs to the aminophenols. Binet
et al. (1972) observed that farnesol has spasmolytic action on the smooth muscle
fibres of the intestine as well as on those of the Oddi sphincter, while oxytocic action
has been reported in a non-West African species, G. elyseoi (Paris, 1956). Further,
farnesol has been found to have psychosedative action in cases of psychic over-excite-
ment; in higher doses it influences psychomotor defence reactions. Farnesol has
proved to be antagonistic to the excitant effect of caffeine and to potentiate the
hypnotic effect of barbiturates without being hypnotic itself (Paris, 1956).
Pentaclethra macrophylla Benth. MIMOSACEAE

Oil bean tree, Congo acacia
A decoction of the bark is used in Nigeria in a lotion for healing sores. In Sierra
Leone, the bark has been reported to be an anthelmintic. The Ibos hold a baby
suffering from adekuku (epileptic fits) in the smoke of the burning leaves (Irvine,
1961).
The beans yield 30-36% of a non-drying oil, the seed kernels 44—45%. This oil is
suitable for soap and candles and for lubrication (Oliver, 1958). In the shell of the
nut the presence of the alkaloid paucine, as well as a fixed oil and resinous
constituents, have been reported (Henry, 1949, p. 776). In the Ivory Coast, the nut
117
has been found to contain 55.4% lipids, 28.5% of protides and 12.2% of glucides.
The oil contains mainly glycerides of linoleic, oleic and lignoceric acids (Busson,
1965).
Correia da Silva and co-workers reported that 0.5-1 ml of a 1:10 aqueous decoction
of the bark causes violent and long-lasting contractions of the isolated guinea pig
uterus (Correia da Silva et al., 1960). Later they found that the same extract
decreases smooth muscle tone in the guinea pig trachea and in rat, rabbit and pig
blood vessels and that it antagonizes the effect of acetylcholine and histamine on the
intestine of the guinea pig (Correia da Silva and Quiteria Paiva, 1970). The
anticholinergic effect was confirmed by Sandberg and Cronlund (1982).
Newbouldia laevis (Beauv.) Seem, ex Bureau syn. (Spathodea laevis Beauv.)

(Fig. 3.8) BIGNONIACEAE
In Ghana in 1891 Easmon found N. laevis bark effective in the treatment of malaria
and dysentery and attributed the action to a tonic effect on involuntary muscles and
mucous membranes. In Lagos, an infusion of the bark and rootbark is used against
convulsions in children and the flowers and leaves are used in a liniment for skin
Fig. 3.8. Newbouldia laevis (Beauv.) Seem, ex Bureau.

118
diseases. The juice of the fresh leaves is applied to wounds (Dalziel, 1937; Watt and
Breyer-Brandwijk, 1962).
C From the roots of trees growing in Portugese Guinea, four different alkaloids have
been isolated. One of the bases was identified as harmane (Ferreira et al., 1963a).
Alkaloids have also been found in the bark but not the leaves of Congolese
specimens. In the leaves and bark, no flavonoids, saponins, quinones, terpenes or
steroids could be detected (Bouquet, 1972).
P The alkaloids obtained from the specimens from Guinea show an inhibiting action
upon the isolated rabbit duodenum and guinea pig ileum. They antagonize the
action of acetylcholine and histamine on the guinea pig ileum but do not act on the
isolated uterus (Correia da Silva et al., 1966).
Lantana camara L. syn. (L. antidotalis Thonn.) VERBENACEAE

Wild Sage, Bahama tea
L In Nigeria and Senegal, an infusion of the leaves is used as a treatment against coughs
and colds. In Senegal, it is also given to asthma patients as it is said to relieve
dyspnoea and suffocation. A mixed infusion with Ocimum is considered to have
diaphoretic and antipyretic action.
C The leaves, stems and flowers were found to contain the triterpenes a-amyrine,
/3-sitosterol, lantaden B and a triterpenoid acid. In addition, a lactone was obtained
from the hydro-alcoholic extract. The triterpenoid acid, later named lantaden A, has
been identified as rehmannic acid (Louw, 1948,1949). The essential oil found in the
leaves is rich in caryophyllene, eugenol, a-phellandrene, dipentene, terpineol,
geraniol, linalol, cineol, citral, furfural and phellandrone (Ahmed et al., 1972).
Sugars and lipids have also been reported to be present.
P The plant, if ingested, causes photosensitization in sheep (Seawright, 1963; Sea-
wright and Allen, 1972). In an extensive bibliographical research, Watt and
Breyer-Brandwijk (1962) showed that the icterogenous action of the plant is the basis
of the intoxication. Intoxications in children accidentally eating the berries showed
an icterogenous effect (Wolfson and Solomons, 1964) and rehmannic acid has been
shown to be an icterogenous triterpenoid acting on the permeability of the liver cells,
mainly by blocking the excretion of bile pigments (especially bilirubin and phyllo-
erythrine), thus causing icterus and abnormal sensitization (Heckel et aL, 1960;
Dhillon and Paul, 1971; DwivedietaL, 1971; Seawright and Allen, 1972). Lantanin,
later identified as the isomeric triterpenes lantaden A and B, was mentioned in The
US National Dispensary, 1926, as an antispasmodic, but has proved to be too toxic.
Some of the constituents of the essential oil account for the antiseptic effect.
(c) Stimulants of the cholinergic and adrenergic systems
Cissus quadrangularis L. syn. (Vitis quadrangularis (L.) Wall, ex Wight & Arn.)
(Fig. 3.9) VITACEAE
Edible stemmed vine, Vigne de Bakel (Senegal)
L The fresh leaves and pounded stems are applied to burns, wounds and also to saddle
119
sores of horses, camels, etc. The stem is also used for gastrointestinal complaints or
as a stomachic sometimes taken in the form of the succulent stem boiled and sugared.
In Guinea the stems and leaves are given to cattle to induce milk and in Senegal a
decoction of the stems and leaves is used as a friction and wash in pains with fever
and in malaria (Dalziel, 1937).
The plant was found to contain a steroid which can be separated into two fractions
(Sen, 1966). Further, a water-soluble glycoside has been obtained from the plant,
which on oral administration had no toxic effect in mice, rats or guinea pigs (2 mg/kg
for 10 days). On intravenous administration, however, the animals showed convul-
sions and died with 5 min.
Das and Sanyal (1964) noticed that an alcoholic extract of the plant (containing resins
and sterols) acted upon the isolated intestine and the uterus of rabbits and albino rats
in a manner comparable to that of acetylcholine. The effect was also observed in situ
on the tracheal and intestinal muscles of the dog. The LD 50 was 15.5 mg/kg in guinea
pigs. The extract has a favourable effect on gastrointestinal evacuation and is
recommended in cases of indigestion, dyspepsia and gastritis (Das and Sanyal,
1964). In dogs the glycoside fraction produced dose-dependent hypotension. The
negative chronotropic effects on the myocardium can be overcome by 7.5 M calcium
(Subbu, 1970). It is believed to act on the cell membrane by inhibiting the movement
of Ca2+ into the cell substance (Subbu, 1971). Intramuscular administration of an
extract of C. quadrangularis to rats and local use as an ointment in dogs was shown to
reduce the convalescence time of experimental cortisone-treated fractures by 33%
(cortisone has an anti-anabolic action and delays consolidation) (Udupa and Prasad,
Fig. 3.9. Cissus quadrangularis L.
Ct A
120
1964; Prasad and Udupa, 1963). A potent anabolic steroid isolated from the plant has
been shown to have a marked influence on the rate of fracture healing; it induces an
early regeneration process of all connective tissues involved in the healing and a
quicker mineralization of the callus (Udupa et al., 1965). Indeed, after 6 weeks the
bones recovered 90% of their original strength. Calcium-45 uptake studies indicated
early completion of recalcification and earlier remodelling. This steroid fraction
appears to have androgenic properties and produces an increase in body weight and
the total weight of the testes in animals (Prasad and Udupa, 1963; Udupa and Singh,
1964; Udupa et al., 1965; Prasad et al., 1970).
The pathway to the site of action of the phytogenic steroid can be studied by
tagging it with radioactive 14C. The site of action is located in the rat by microauto-
radiography. The probable pathway seems to be through the anterior pituitary
gland, then by the adrenals and testes. After some metabolism in the liver, the
steroid reaches the osteogenic cells at the fracture site, where it seems to exert a
stimulating effect on the healing of the fracture (Prasad and Udupa, 1972).
Sida cordifolia L. MALVACEAE

The plant provides fibre and is a troublesome weed. In India the rootbark,
pulverized and mixed with oil of sesame and milk, has been said to be effective in
cases of facial paralysis and sciatica (Chopra et al., 1956). Ephedrine has been found
in this plant and has been listed in the Indian Pharmaceutical Codex (1953) for the
relief of hay fever and asthma (Oliver, 1960).
Recent analyses have revealed that ephedrine and i/^-ephedrine constitute the major
alkaloids in the aerial parts (minor bases in the roots). From the aerial parts and the
roots the following were also obtained: /3-phenylethylamine, car boxy lated trypt-
amines, quinazoline alkaloids, S(9)Nb-tryptophan methylester, hypaphorine, vas-
icinone, vasicine and vasicinol in varying amounts (Ghosal et al., 1975). In S. acuta
and S. rhombifolia, also found in West Africa, the main alkaloid in Sri Lanka proved
to be cryptolepine, which was first found in Cryptolepis (Gunatilaka et al., 1980). In
5. acuta growing in India, the alkaloids cryptolepine and ephedrine were found in
the roots as well as a-amyrin (Krishna Rao et al., 1984).
The favourable combination of three sympathomimetic amines and a potent
bronchodilator principle (vasicinone) would, according to Ghosal et al. (1975),
account for the major therapeutic uses in asthma, hay fever, etc. Vasicine is said to
be a promising uterotonic abortifacient (it is mainly obtained from Adhatoda vasica
(Gupta etal., 1978).
Anticonvulsant and antipyretic activities of the plant (collected in India) have
been observed by Dhar et al. (1968). In addition these authors note extensive
antibacterial, antifungal and antiviral effects as well as antiprotozoal action on
Entarnoeba histolytica and anthelmintic action towards Hymenolepis nana and
Ascarides galli. A hypoglycaemic effect and action on the smooth muscles and heart
were also reported. Anticancer activity against human nasopharynx carcinoma (in
tissue culture) and lymphoid leukaemia and sarcoma 180 in mice were revealed in
CCNSC tests in the USA (Dhar et al., 1968).
121
Crateva religiosa Forst. syn. (C. adansonii Oliv.) CAPPARIDACEAE

The root is used in Nigeria as a febrifuge and the Yorubas apply the leaf as a mild
counter-irritant for headache (Dalziel, 1937). In India, the stembark has been used
as an antipyretic, stomachic, laxative and diuretic (Chopra et al., 1956). In the
Philippines, the juice of the bark is used to treat convulsions (Quisumbing, 1951).
In India, the bark was found to contain a gum, a saponoside and tannins. From the
air-dried powdered bark, the triterpenes lupeol, /3-sitosterol and lupeol acetate have
been isolated. The water-soluble portion contained traces of quaternary and tertiary
bases and sugars. The tertiary bases were found to contain both sulphur and nitrogen
(Bhandari and Bose, 1954; Chakravarti et al., 1959; Kjaer and Thomsen, 1963;
Smolenski et al., 1972; Kondagbo and Delaveau, 1974). In the leaves and twigs nine
flavonoids, mainly rutin, quercetin and isoquercetin have been reported (Hegnauer,
Vol. 3, p. 362).
The water-soluble fraction of the air-dried bark had spasmodic action, which was not
blocked by atropine, on the uterus of the rat, guinea pig, rabbit, dog and humans. It
was also observed to have cholinergic action on the isolated ileum of the guinea pig
and on dog tracheal muscle preparations. Nicotinic action of the extract on the
ganglia has also been noted by Deshpande (1973). Clinically, ingestion of a powder
of the whole plant has been observed to improve the tone of the urinary bladder in
12 cases of post-operative prostatic enlargement and it could even remove smaller
stones from the ureter and bladder and control various urinary tract infections. This
action has been attributed to the cholinergic action of the drug on smooth muscles
(Deshpande, 1973).
A petroleum ether extract and sterols isolated from the stembark significantly
inhibited the acute inflammation induced by carrageenan and histamine in albino
rats and inhibited the early and delayed phases of inflammatory changes in formal-
dehyde-induced arthritis (Ramjelal et al., 1972). Total extracts had an inhibiting
effect towards Shigella dysenterica and the leaves and stembark had (considerable)
anticancer action on sarcoma 180 (Kerharo and Adam, 1974) and on lung cancer
(leaves) (Abbots al., 1966),
Borreria verticillata (L.) Mey. syn. (Spermacoce verticillata L.,S. globosa Schum. &
Thonn.) RUBIACEAE
A lotion of the plants is used in Senegambie for febrile children and in the treatment
of leprosy, furuncles and paralysis (together with Datura metel). It is also said to be
diuretic and abortive (Dalziel, 1937; Kerharo, 1968).
Plants collected in the Ivory Coast and Senegal have been found to contain 0.20% of
total alkaloids. Emetine or cephaline, reported in older publications (Moreira, 1963)
could not be detected, but two other alkaloids have been reported to be present in
the aerial parts. They are borreverine, with a tetrahydro-/3-carboline nucleus, and
borrerine (Pousset et al., 1973). An essential oil is found in the aerial parts; from it,
a sesquiterpenic lactone was isolated (Benjamin, 1979). Iridoids, daphyloside,
asperuloside and feutoside have been obtained from the rootbark (Sanity et al.,
1981).
122
Pharmacological screening in Brazil showed that this plant has a stimulating action
on the uterus of the rat and on the duodenum of the rabbit. No actions on the blood
pressure and respiration of the cat could be detected nor were any effects observed
on the striated frog muscle and guinea pig intestine. Toxicity to mice and fish was nil
(Barros et al., 1970) and no insecticidal activity was found (Heal and Rogers, 1950).
The antimicrobial activity of the essential oil was tested by Benjamin (1979) and
revealed inhibition of Escherichia coli and Staphylococcus aureus.
Cardiospermum halicacabum L. syn. (C. microcarpum Kunth) SAPINDACEAE

In Nigeria the leaves are sometimes rubbed on the skin for the treatment of skin
eruptions, itch, etc. or applied as a poultice to swellings. The juice of the stem is
dropped in the eye to treat ophthalmia. The leaf and root are used as a remedy for
nervous diseases in many countries (e.g. Australia and South Africa) (Watt, 1967).
After eating the seeds in quantity children may develop epileptiform convulsions.
Stigmasterol, probably in the form of a glycoside, and quebrachitol have been
isolated from the air-dried plant in India and proanthocyanidin and apigenin have
been isolated from an alcoholic extract of the roots (Dass, 1966).
The water-soluble fraction of a dried alcoholic extract of the seeds produced an initial
depression followed by marked stimulation in the isolated frog heart preparation
(Moti and Deshmanhar, 1972).
Anti-infective activity of higher plants
Ideally, the plants used for anti-infective therapy should be toxic to infectious
organisms and devoid of toxicity for human beings. The aim is to obtain the highest
possible favourable ratio between the dose toxic to man and that active against the
agent of infection. Biochemical differences between the infective agent and the host
should allow the finding of plant constituents that are selectively toxic to the
infecting organism.
The plants used for anti-infective therapy can be divided into two groups:
I Anti-infective higher plants
These include:
(a) antibacterial plants;
(b) antifungal plants;
(c) antiviral plants;
(d) antiprotozoalplants;
(e) antimetazoal plants (anthelmintics).
II Plants with insecticidal and molluscicidal activity (parasitic hosts)
(a) insecticidal plants;
(b) molluscicidal plants.
The term antibiotics, which was first given to substances produced by fungi and
bacteria that inhibit the vital processes of certain microorganisms other than the
species producing them, has been extended by many authors to those constituents of
higher plants which have similar effects in very low concentrations (e.g. Paris and
Moyse, 1965). Those constituents which act on pathogenic fungi, viruses and
protozoa are also included (Patel et al., 1967) and the term has been used in this sense
throughout the book.
The antibacterials inhibit the multiplication of bacteria and can be either bacteri-
cidal or bacteriostatic. The lowest concentration that completely inhibits the
microorganisms after exposure in vitro for a specified period is referred to as the min-
imum inhibiting concentration (MIC). Conventional antibacterial drugs are known
to inhibit cell division in the microorganisms by interfering with p-aminobenzoic
acid, which is a co-factor in the synthesis of folic acid, others interfere with protein
124
synthesis in the bacteria, others again attack the cytoplasmic membrane by dissociat-
ing its lipoproteic structure and another group of antibacterial drugs inhibit the
building up of new cell walls during cell division by blocking the enzyme transpep-
tidase, which controls their synthesis.
The main endemic bacterial diseases in West Africa include leprosy, tuberculosis,
occasionally cholera, bacillary dysentery, enteric fevers and undulant fever.
The demand for antifungal drugs is considerable in a warm, damp climate in
which fungal diseases are rife. The diseases are mainly ringworm (Tinea imbricata,
T. cruris, T. pedis, T. unguium), caused by e.g. Epidermophytonfloccosum, E. concen-
tricum, Trichophyton mentagrophytes, T. rubrum and Nocardia minutissima; pityriasis
versicolor (Tinea versicolor), caused by e.g. Cladiosporum mansoni and Malessesia
furfur; and aspergillosis (in lungs), caused by Aspergillus fumigatus. Many of the
antimycotic drugs are used in topical application.
Virus diseases in West Africa include yellow fever, rabies, poliomyelitis and
trachoma, but of course dengue, influenza and measles also occur. As opposed to
the bacteria, which have their own reproductive system, viruses use certain syn-
theses of the cell itself for their reproduction. This explains why they can change the
function of normal cells. No relevant information about the action of antiviral drugs
has emerged from the pharmacological tests described in this section.
The main protozoal diseases in West Africa are malaria (parasite genus Plas-
modium); African trypanosomiasis; leishmaniasis, including kala-azar (visceral
form) and that caused by Leishmania tropica (oriental sore); and, rarely, amoebiasis
(amoebic dysentery, parasite Entamoeba histolytica) and giardiasis (parasite Giardia
intestinalis (Lamblia)).
Metazoal diseases in West Africa are caused by nematodes, trematodes and
cestodes. The main infectious agents include (Manson-Bahr, 1952):
Nematodes acting on the intestine; hookworm (Ancylostoma duodenale),
whip worm (Trichuris trichiura), pinworm (Oxyuris vermicularis), round-
worm (Ascaris lumbricoides), trichinose (Trichinella spiralis)
Nematodes acting on tissues: guinea worm (Wucheria bancrofti) (filariasis),
guinea worm (Dracunculus medinensis) (dracontiasis)
Nematodes acting on eyes: blinding worm (Onchocerca volvulus) (on-
chocerciasis), eye worm (Loa Loafilaria) (loa loa filariasis).
Trematodes: flukes (Schistosoma mansoni) (bilharzia)
Cestodes: adult and larval tapeworms (Taenia solium, T. saginata,
Echinococcus granulosis, Hymenolepis nana)
Plants with anti-infective activity which have already been described in Chapter 2
for their action on the cardiovascular system are indicated hereunder by CV.
Similarly, the plants already described in Chapter 3 for their effects on the nervous
system are indicated by N.
The plants marked by an asterisk (*) in the enumeration of the constituents at the
beginning of each action group are described in this text, the others can be found in
the corresponding tables. Often several uses are indicated after each plant name, in
125
which case a dagger (f) is placed after the use under which the description of the
plant can be found.
So far, anti-infective experimentation with plants has been very superficial.
Often, the testing amounts to little more than in vitro exposure of material to
organisms which may or may not be pathogenic to man. Nevertheless, the tests
carried out by many authors on non-pathogenic organisms are indicated here: some
organisms formerly believed to be non-pathogenic have lately been found to be
possibly pathogenic or may be pathogenic to cattle or domestic pets.
The organisms discussed below that are considered non-pathogenic are Aspergillus
flavus, Bacillus cereus, B. subtilis, B. mycoides, B. megaterium, Giardia muris (ro-
dents), Micrococcus leirodeicticus, Mycobacterium smegmatis, Mycob. phlei. Penicillin
chrysogenum, Saccharomyces cerevisiae, Sarcina lutea and probably Penicillin
echyogenum. Paramecia, a formerly much-used genus for testing, has been aban-
doned.
I Plants with antibiotic activity

A great variety of components belonging to different chemical groups were
found to have antibiotic activities. Similar observations had been made by Lechat et
al. (1978) and Brannon and Fuller (1973) concerning the antibiotics isolated from
Streptomycetaceae and Thallophytae and were explained by them by the fact that
the different antibiotics attack different sites in the pathogenic organisms
Comparison of the MIC of essential oils from plants in vitro tests with their tissue
concentrations active in vivo showed that the mechanism of their anti-infectious
action is different from that of the antibiotic type of action. Antibiotics require an in
vivo concentration in the tissues that is equal to, or greater than, their minimum
active concentration in vitro. In the case of essential oils, however, concentrations in
the blood of about one-hundredth of their active concentration in vitro have been
shown to heal patients with acute or chronic infections. Thus patients have been
cured with essential oil arriving in the organism in doses quite insufficient to deal
with the infectious agent in the laboratory, the in vitro activity of the essential oils
being 100 times higher than that of antibiotics, whilst in vivo the actions are
comparable. The results of tests on 268 clinical cases (Valnet et al., 1978) suggest that
essential oils have a general action on the organism of the patients. Valnet and
co-workers call the microbiocidal use of the oils 'aromatotherapy' and their test-
records 'aromatograms'. They believe that the action of the essential oils is based on
a global action which modifies the general condition of the patient (action on
neuro-endocrine functions?)
(a) Antibacterial plants

Active constituents
The plant constituents with antibacterial action are tentatively grouped
according to their main chemical groups.
126
Phenols. In Anacardium occidental the aromatic phenols cardol and anacardol

(decarboxylated derivatives of anacardic acid) are not only bactericidal! and antifun-
gal but also vermicidal and protozoicidal. The phenol chloropherin in Chlorophora
excelsa is antibacterial and antifungal and in Ocimum viride, thymol (also vermicidal)
and eugenol are antimicrobial.
Quinones. The napthoquinone plumbagin, found in Plumbagozeylanica* and also
in Diospyros mespiliformis and Drosera indica*, is antibacterial,! antifungal, antipro-
tozoal and anthelmintic, and the benzoquinone from Embelia schimperi* is slightly
antibacterial but mainly anthelmintic.f
Acids. Citric acid in Bryophyllum pinnatum*, is antibacterial and the fatty acids
with a cyclopentene nucleus (chaulmoogric and gorlic acids) in Caloncoba echinata*
act on the lepra bacillus. The acidic phenols gallic acid (and ethylgallate) are reported
to be antibacterial in Bomb ax spp. and antibacterial and anthelmintic in Acacia
farnesiana and Mangifera indica.
Alkaloids. Berberine in Argemone mexicana (also found in Chasmanthera dependent)
is said to be antimicrobial and antiprotozoal; sanguinarine acts as a lipolytic pro-drug
and is antifungal. Cryptolepine in Cryptolepis sanguinolenta * andSida spp., canthine-
6-one, chelerythrine and berberine in Zanthoxylum zanthoxyloides* and solanine in
Solanum nodiflorum are all antibacterial;! and this also applies to the indole alkaloids
of Strychnos afzeli and funiferine from Tiliacora funifera.
Flavonoids. Ageratum conyzoides* contains an antibacterial! flavone (the plant
extract is also anthelmintic in vitro). Combretum micranthum* and C. racemosum* are
antibacterial;! they contain flavonoids, alkaloids (combretines) and catechuic tan-
nins. Canscora decussta* (xanthones) inhibits Mycob acterium tuberculosis* and is also
antiviral, whilst Psidium guaijava* has three flavonoids with a strong antibacterial!
effect on Mycob. tuberculosis. The flavonoids of Uvaria chamae* act on Mycob.
smegmatis*; they are also reported to be larvicidal.
Sulphur heterosides. Allicin in Allium * spp. is antibacterial! and antifungal and this
is also the case for the isothiocyanate glucosides in Capparis decidua * (glucocappa-
rin), Lepidium sativum (glucotropeolin), Moringa oleifera* (rhamnosyl-oxyben-
zylisothiocyanate); and Carica papaya* seeds (tropaeolin). Cleomin from Ritchiea
longipedicillata* is antibacterial and anthelmintic! (mainly). Hydrogen cyanide
(HCN) found in Acalypha wilkesiana * may account for the antibacterial action of this
plant.
Terpenoids. Antibacterial activity is reported for Borreria verticillata* (sesquiter-
penic lactone), Xylopia aethiopica* (diterpene, xylopic acid), Azadirachta indica*
(seeds, triterpenoids, also antiviral) and Ekebergia senegalensis* (stembark,
meliacins). The leaves of Azadirachta are insecticidal and those of Ekebergia are
ichthyotoxic.
Proteolytic enzymes. Papain from Carica papaya, calotropine from Calotropa
procera and bromelain from Ananas comosus are able to digest bacterial and parasitic
cells and bromelain even digests worms.
Polyacetylenes and phenylheptatriene from Eclipta prostrata and Bidens pilosa
127
(leaves) respectively, have a strong UV-mediated toxicity to bacteria and Candida

and are also toxic to insects and larvae (Wat et aL, 1978,1979,1980).
Anacardium occidentale L. (Fig. 4.1) ANACARDIACEAE

Cashew nut tree
This tree has been described earlier (CV).
Anacardic acid, which constitutes 39% of the 'cashew balsam' from the fleshy parts
of the fruit (Gellerman and Schlenk, 1968) and is found also in crude extracts of
cashew nut shells (Rahman et aL, 1978), is a mixture of 6-(n-C15-alkyl) salicylic acids
with side chains varying in degrees of unsaturation. Anacardic acid has been found
to have moderate bactericidal activity against Staphylococcus aureus (Ogunlana and
Ramstad, 1975). Investigation of certain decarboxylated derivatives of anacardic
acid, cardol and anacardol, showed that these were not only bactericidal but also
fungicidal, vermicidal, protozoicidal, parasiticidal and even anti-enzymatic
(Eichbaum et aL, 1950; Jacquemain, 1959; Gulati et aL, 1964; Laurens and Paris,
1977). More recently anacardic acid, its acetate and the fully saturated analogues
have been found to be very active against Mycobacterium smegmatis and moderately
active against Bacillus subtilis. Good antifungal action against Trichophyton menta-
grophytes and moderate action against Saccharomyces cerevisiae have also been
reported (Adawadkar and El-Sohly, 1981). The antimicrobial activity of anacardic
Fig. 4.1. Anacardium occidentale L.

128
acids (which are also the main constituents oiGinko biloba) had been reported earlier
by Gellerman et al. (1969). The anthelmintic action of the Anacardium nut-shell
liquid had been tested before in ancylostomiasis, ascaridiasis and trichuriasis and
had given satisfactory results (Eichbaum et al., 1950). It has further been shown that
the molluscicidal activity of crude extracts of nut shells requires both the unsaturated
side chain and the carboxyl group of anacardic acid (Sullivan et al., 1982).
The antibacterial activity of metallic complexes of anarcardic acid with mercury,
zinc, copper, manganese and cobalt was the subject of tests by Chattopadhyaya and
Khare (1970) against 17 test organisms. The strongest antimicrobial activity of
anacardic acid proved to be against Staphylococcus aureus. The mercury complex was
particularly active against Staph. aureus, Streptococcus pyogenes, Escherichia coli and
Bacillus pumilis.
Another Anarcadiaceae, Heeria insignis (Del.) O. Ktze. has also been found to
have antimicrobial activity; it gives positive reactions for tannins and saponins. In
West Africa it is much employed as an anthelmintic and antidysenteric (Delaveau et
al., 1979).
Plumbago zeylanica L. PLUMB AGIN ACE AE

Ceylon leadwort
The root is a vesicant and counter-irritant. Dried and pulverized it is added to a
maize pap as a remedy for parasitic skin diseases and in Southern Nigeria the leaves
are put in soup as a remedy for worms and for fever. In Ghana the root is
administered as an enema to treat piles (Dalziel, 1937). In the Ivory Coast and Upper
Volta it is used in the treatment of leprosy (Kerharo and Bouquet, 1950).
The roots contain plumbagin or plumbagol, a 2-methyl-5-hydroxy-l,4-
naphthoquinone, in amounts of 1.26% in the Ivory Coast (Paris and Moyse-Mignon,
1949; van der Vijver and Lotter, 1971). (Plumbagin is also found in Diospyros and
Drosera spp.) The leaves and stems of P . zeylanica contain only very small amounts
in addition to a fixed and a volatile oil (Watt and Breyer-Brandwijk, 1962).
Plumbagin has vitamin K action and antibacterial properties. In India it is also said
to stimulate the secretion of sweat, urine and bile and to have a stimulating action on
the nervous system and on the muscular tissue (Bhatia and Lai, 1933). In a
concentration of 1:50000, plumbagin has a marked antibiotic action on
staphylococci and certain pathogenic fungi (Coccidoides imminentis, Histoplasma
capsulatum, Trichophyton ferrugineum) and on parasitic protozoa (Carrara and
Lorenzi, 1946; Van der Vijver and Lotter, 1971). Intravenous injections in patients
with boils, anthrax or cystitis have been well tolerated and brought about a rapid
recovery (Saint Rat et al., 1946,1948; Saint Rat and Luteraan, 1947; Blanchon etal.,
1948; Vichkanova et al., 1973a). Experimental Microsporum infections in mice have
been healed by local applications of 0.25-0.5% solutions in 40% alcohol or 1%
emulsions of plumbagin (Vichkanova et al., 1973a). In vitro, the growth of
Staphylococcus aureus, Streptococcus pyogenes and Pneumococcus has been completely
inhibited by solutions of plumbagin at concentrations of 1:100000; that of My cobac-
terium tuberculosis at concentrations of 1:50000 and the growth of Escherichia coli
129
and Salmonella at concentrations of 1:10000 (Skinner, 1955; Oliver, 1960; Vic-

hkanova et aL, 1973b). Antispasmodic activity of plumbagin was also reported, by
Bezanger-Beauquesne and Vanlerenberghe (1955), but it proved inactive in the
treatment of infection by Haemophilus pertussis, Plumbagin (isolated from P.
capensis) showed a potent antifeedant activity against larvae of the army worms
(Spondoptera exempta) at 10 p.p.m. and of S. littoralis at 20 p.p.m., and caused their
complete inhibition at a concentration of 12.5 /xg/ml; it has proved to be antimicro-
bial in Candida utilis and Saccharomyces cerevisiae (Kubo et aL, 1980).
Drosera indica L. DROSERACEAE

The plant is used in India as a powerful rubefacient and a maceration is applied
topically to corns in Vietnam (Chopra et aL, 1956).
The plant contains naphthoquinones, mainly plumbagin (see Plumbago zeylanica)
(Bezanger-Beauquesne and Vanlerenberghe, 1955).
Drosera rotundifolia, D. coryifolia and D. intermedia have been reported to prevent
bronchospasms produced by acetylcholine or histamine and to decontract in vitro
spasms of the intestine caused by acetylcholine or barium chloride. They are said to
be antitussive and to prevent coughing induced by excitation of the larynx nerve in
the rabbit (Paris and Moyse, 1967, pp. 227-9). The napthoquinones also have an
antimicrobial action; a plumbagin solution inhibits the growth of Staphylococci,
Streptococci and Pneumococci in concentrations of 1:50 000 and has been used against
whooping cough although practically no action against Haemophilus pertussis was
noted (Bezanger and Vanlerenberghe, 1955) and is used in the treatment of other
severe, persistent coughs. France was said to use about ten tons yearly in 1969 as an
antitussive (Paris and Moyse, 1967, Vol. II, p. 229). Denoel (1958) reported that
plumbagin is an isomer of phthiocol, a constituent of the tubercle bacillus, and some
authors suppose that substitution of phthiocol explains the activity of Drosera on the
respiratory tract. In fact certain plumbagol-sulphamide compounds showed an
antituberculostatic activity in vitro. According to Vichkanova et al. (1973a) the
antimicrobial spectrum of plumbagin includes Gram-positive and Gram-negative
bacteria, influenza virus, pathogenic fungi and parasitic protozoa. However, they
report it to be ineffective against Giardia muris (a protozoan parasite to rodents) and
tuberculosis in mice when administered orally for 5 days. They successfully treated
experimental Microsporum infections in guinea pigs by local application of 0.25-0.5%
solutions in 40% alcohol or 1% emulsions of plumbagin.
Bryophyllum pinnatum (Lam.) Oken syn. (B. calycinum Salisb., Cotelydon pinnata
Lam., Kalanchoepinnata (Lam.) Pers.) CRASSULACEAE
Never die or Resurrection plant (from viviparous properties)
The crushed leaves (or the juice squeezed out after heating) are mixed with
sheabutter and oil and the mixture is applied to abscesses, swellings, ulcers and
burns or used to rub the bodies of young children suffering from fever. The juice is
also applied for earache and ophthalmia (Dalziel, 1937). In India, where the leaves
are also used as an application on bruises, wounds, boils and insect bites, the leaves
130
of an Indian species (Kalanchoe laciniata) are similarly used and are said to allay
irritation and promote healing; the juice is considered styptic and is also adminis-
tered in the treatment of bilious diarrhoea and lithiasis (Chopra et al., 1956).
The leaves contain bryophyllin, potassium malate and ascorbic, malic, isocitric and
citric acids (Mehta and Bhat, 1952; Chopra et al., 1956; Gaind and Gupta, 1969).
Studies of the antimicrobial activity of the juice obtained from the heated leaves,
using the agar diffusion method, showed an inhibition zone of more than 20 mm
when used on test organisms of Staphylococcus aureus, Bacillus subtilis, Escherichia
coli and Pseudomonas aeruginosa. It has also been noted that the heated leaf, when
applied to inflamed areas, produces a soothing effect, keeping wounds clean and
preventing them from going septic (Boakaiji Yiadom, 1977).
Caloncoba echinata (Oliv.) Gilg syn. (Oncoba echinata Oliv.) FLACOURTIACEAE

Caloncoba glauca (P. Beauv). Gilg syn. (Ventenatia glauca P. Beauv., Oncobaglauca
(P. Beauv.) Hook, f., C. dusennii)
Caloncoba Welwitschii (Oliv.) Gilg
Gorli
A lotion made from the plant is used by several native tribes in Guinea, Sierra Leone
and Ghana for pustular eruptions of the skin. The seeds contained in the fruit
capsule have long been known to contain chaulmoogric acid but the toxic ingredients
of the acid cause nausea and vomiting and irritation of the mucous membrane of the
stomach, and hydnocarpic acid is therefore preferred (Dalziel, 1937). The Caloncoba
spp. are not used much in modern leprosy treatment.
The three Caloncoba spp. have nearly the same constituents as chaulmoogra oil,
which is obtained by squeezing out the fresh ripe seeds of Taraktogenus kurzii from
Burma. However, the oil of the Caloncoba spp. is less appreciated than chaulmoogra
or mainly hydnocarpus oil (from Hydnocarpus spp.) as the seeds are very small,
extraction is laborious and the fat is less suitable for injection. The Caloncoba spp.
contain in general 30-50% lipids of which 1-3% is non-saponifiable. The fat consists
in West Africa of 60-80% chaulmoogric acid (against 50-70% hydnocarpic acid in
Hydnocarpus spp. which have been acclimatized in Nigeria, the Cameroons, Guinea
and the Ivory Coast); the remaining lipids consist in both cases of 8-15% gorlic acid
and 10-12% of ordinary fats (oleic and palmitic acids) (Chevalier, 1928; Pelt, 1959;
Paris and Moyse, 1963). Both chaulmoogric and hydnocarpic acids have saturated
side chains.
In 1967 there were some 10-12 million lepers in the world (Paris and Moyse, 1967).
Chaulmoogra remains a classic medicine although often associated with sulphones,
which are more effective in the malignant forms of the disease, and might be used as
a suspension of diaminodiphenylsulphone in acetylchaulmoograte. The treatment is
lengthy (250 ml/year is required) and should be combined with an adequate diet.
Chaulmoogra oil is also used for certain skin complaints (lupus) and as a parasiticide
in veterinary medicine (Pelt, 1959; Zenan and Podkorny, 1963).
131
Cryptolepis sanguinolenta (Lindl.) Schltr. ASCLEPIADACEAE

The hypotensive and antipyretic properties of this plant have already been briefly
described (CV). In local medicine it is also reputed to be active in the treatment of
urogenital infections and malaria. Hence Dwuma Badu et al. (1978) and Boakaiji
Yiadom (1979) have carried out antibacterial tests. In those against urogenital
pathogens the aqueous extracts of the roots showed antimicrobial activity against
Neisseria gonorrhoeae, Escherichia coli and Candida albicans but not against
Pseudomonas aeruginosa. With 20.0 and 10.0 g/1 solutions the inhibition zones were
approximately equivalent to those produced by a solution of 25 ^tg/ml of trihydrate
of ampicillin used as a control, only the effect on Candida albicans was slightly
weaker, especially with the smaller dose. The effect of 5.0 g/1 was inferior to that of
the control for all the test organisms. Cryptolepine has no plasmocidal effect
(Boakaiji Yiadom, 1979).
Similar effects were reported with the hydrochloride of cryptolepine (an
indoloquinoline alkaloid isolated from the roots) (Gellert et al., 1951; Dwuma Badu
et al., 1978; Boakaiji Yiadom and Heman Ackah, 1979). Recently, Bamgbose and
Noamesi (1981) have reported an inhibition by cryptolepine of carrageenan-induced
oedema.

F. senegalensis (DC.) Chev., Z. senegalense (DC.) Chev., Z. polyganum Schum.)
RUTACEAE
Prickly ash, toothache bark, candlewood (see also CV)
The root of this plant is much used as a chewing stick in Nigeria. Other common
chewing sticks in the country are: Vernonia amygdalina root and stem, Terminalia
glaucescens root, Massularia acuminata stem, Garcinia kola root. Chewing sticks are
believed to have antimicrobial properties (Fadulu, 1975).
Chromatographic and chemical purification of an ethanolic extract of the powdered
root of Zanthoxylum zanthoxyloides yielded four compounds which showed anti-
microbial activity: canthin-6-one, a tertiary phenolic alkaloid, two quaternary
alkaloids with antimicrobial action (chelerythrine and berberine) and a compound
whose structure is still to be determined (Odebiji and Sofowora, 1979).
The antimicrobial effect of the buffered extracts of all these chewing sticks on the
oral flora has been tested by the streak-plate method and it has been shown that all
are to some extent active, whilst the controls showed a heavy increase in micro-
organisms although to differing degrees. The action against more than 20 organisms,
including Gram-positive and Gram-negative bacteria as well as Candida spp. and
protozoa (Entamoebia gingivalis) was examined. Canthine-6-one (also isolated from
Zanthoxylum elephantiasis) has been shown to be consistently active against
Staphylococcus aureus, Klebsiella pneumoniae, Mycobacterium smegmatis and Candida
albicans (Mitscher et al., 1972a, b). The rootbark also contains fagarol, which has
been found to be identical with sesamine from Sesamum indicum (Karrer, 1958). The
root of Z. zanthoxyloides, in addition to giving the biggest zone of inhibition of all the
132
chewing sticks tested, in the seeded blood agar plate also preserved the colour of the
blood in that zone (El Said et al., 1971), but this effect was absent in the blood agar
plates for the other plant extracts. Further investigation of this curious phenomenon
showed that the extract was able to reverse sickling and crenation in erythrocytes in
vitro (see CV) (Isaac-Sodeye, 1971; Sofowora et al., 1975).
Ageratum conyzoides L. COMPOSITAE

The common medicinal use of the plant in West Africa is for healing wounds,
especially burns. For this treatment the juice of the bruised leaves is squeezed into
the wound, which is then covered by a bruised but intact leaf. In Nigeria the patient's
chest is also rubbed with the leaves of the plant as a treatment for pneumonia
(Durodola, 1977).
The whole plant contains an essential oil (0.16% of the dried plants composed of
phenols (traces of free eugenol), phenolic esters, coumarin and ageratochromone.
From the Indian plant 6-dimethoxy-ageratochromene and ageratochromene have
been isolated (Kasturi and Manithomas, 1967) and Rudloff (1969) has found
ageratochromone to be the principal constituent (75%) of the essential oil of the
leaves in the Indian plant. In the West African plant a new flavone, 5,6,7,8,3',4',5'-
heptamethoxyflavone, has been identified in the stems and leaves as well as
stigmasterol dotriaconthene, 7-methoxy-22-dimethylchromene and a new flavone,
conyzorigun (Adesogan and Okunade, 1979).
The untreated leaves of the plant have proved significantly superior to vaseline gauze
as a wound dressing, and the juice has displayed antibacterial activity in vitro against
Staphylococcus aureus. Different fractions of the plant extract have been tested
against Staph. aureus and the greatest activity was observed with the petroleum ether
fraction containing more than 90% of a new flavone, assumed to be 5-methoxynobili-
tin (Durodola, 1977). A. conyzoides has also shown an in vitro anthelmintic activity
(Alberts al., 1972).
Combretum micranthum G. Don syn. (C. ahum Perr., C. floribundum Engl. &
Diels, C. raimbaultii Heck.) COMBRETACEAE
Kinkeliba
In Nigeria and Guinea a decoction of the root is considered an anthelmintic and is
also used as a wash for sores. Diuretic and cholagogic properties are attributed to the
leaves, which are given as an infusion for the treatment of bilious haematuric fevers
accompanied by vomiting, and also for ordinary colic and nausea, to prevent
vomiting. Hot decoctions of the leaf and root are applied as a vapour bath, as a wash
for febrile patients and for lumbago. The pulverized dry fruits are mixed with oil to
form an ointment for application to suppurating swellings, abcesses, etc.
Flavonoids, heterosides of vitexine (8-C-D-glucopyranosyl apigenine-12) and its
isomer saponaretine have been reported to be present in the leaves as well as
quaternary amino bases comprising two major alkaloids (combretines A and B,
stereoisomers of betonicine) and traces of a third base (Jentzch et al., 1962; Ogan,
1972). In addition, choline has been found (also in the flower buds) as well as betaine
133
and gallic acid, both free and esterified as catechols and catechuic tannins, together
with organic acids and mineral salts (potassium nitrate) (Paris, 1942; Paris and
Moyse-Mignon, 1956). Alkaloids have been reported in the bark (Popp etal., 1968).
The antidiuretic and anticholagogic action of the drug has long been known (Paris,
1942). Amongst the constituents, combretum-catechine has proved to be strongly
diuretic and slightly hypotensive (Paris, 1942), whilst the choleretic action is
believed to be related to combretoside (saponaretin heteroside) (Gregoire, 1953).
The leaves and extracts of C. micranthum are reported to have an antibiotic action
against Staphylococci, Streptococci and Escherichia colt (Mela, 1950). The bark of the
tree growing in Nigeria has shown an antibiotic action against Gram-positive and
Gram-negative organisms (Malcolm and Sofowora, 1969).
The young leaves of C. racemosum Beauv. (Fig. 4.2) are considered to be
anthelmintic in Nigeria and are used by certain tribes in Senegal (Balant) against
internal parasites (Dalziel, 1937; Kerharo and Adam, 1974).
Two other Combretaceae are known for their anthelmintic action: Anogeissus
leiocarpus (DC.) Guill. and Perr. syn. (A. schimperi Hochst ex Hutch. & Dalz.), the
root- and stembark or seeds of which are used mainly for tapeworm in horses and
donkeys (see Table 4.5) and Quisqualis indica L. (rangoon creeper), commonly
grown in the area, the seeds of which are used in India, its country of origin, as an
anthelmintic (ascarides) (Chopra et al., 1956), and the active principle of which is
believed to be an alkaloid.
Fig. 4.2. Combretum racemosum Beauv.
1*
4& 'U
134
The roots of C. rhodanthum Engl. and Diels (C. comosum of F.T.A.) act on
Gram-positive and Gram-negative organisms, in particular on Sarcina lutea,
Staphylococcus aureus and Mycobacterium phlei (Malcolm and Sofowora, 1969).
Canscora decussata (Roxb.) Roem. & Schult. syn. (Pladera decussata Roxb.)
GENTIANACEAE
L In India the fresh juice of the plant is prescribed for insanity, epilepsy and nervous
debility (Chopra et al., 1956).
C Triterpenes, alkaloids, mangiferin (flavonic heteroside) and a number of xanthones
have been isolated from the roots (Chaudhury and Ghosal, 1971; Ghosal etal., 1971).
P The alcoholic extract of the plant has been found to have CNS depressant action in
mice, producing a fall in blood pressure, and to stimulate the isolated smooth
muscles of the rabbit intestine and of the uteri of rats and guinea pigs. It enhances
the effect of acetylcholine on skeletal muscles. The extract also possesses antiviral
activity (Bhakuni et al., 1969). Spermicidal action of the plant has also been reported
(Madran, 1960). Rat sperm had been killed in 5 min by a concentration of 1:50000
of the alcoholic extract of the plant and a concentration of 1:20 000 of the aqueous
extract. Human sperm required higher concentrations (Madran, 1960).
A number of xanthone derivatives isolated from C. decussata have shown an
inhibitory activity in vitro against Mycobacterium tuberculosis, equivalent to that of
streptomycin. Toxicity to mice was low. Mangiferin, also isolated from the plant,
has proved to have weak antitubercular properties (Ghosal and Chaudhury, 1975),
and also to have CNS depressant and significant anti-inflammatory activity in rats
(Shankaranarayan et aL, 1979).
Psidium guajava L. MYRTACEAE

Guava
L The fruits are used locally for an antidiarrhoeial.
C The leaves contain an essential oil rich in cineol, tannins, four triterpenic acids and
ursolic and oleanolic acids (Arthur and Hui, 1954). In addition Khadem and
Mohammed (1958) have isolated three flavonoids from the leaves: quercetin, its
3-L-4-arabinofuranoside (avicularin) and its 3-L-4-pyranoside with strong anti-
bacterial action.
P Nickel (1959) had reported the antibacterial action of guava leaves on Gram-positive
and Gram-negative organisms. In 1969, Malcolm and Sofowora confirmed the
antibacterial action on Gram-positive organisms (Sarcina lutea and Staphylococcus
aureus) and also noted action on Mycobacterium phlei by Nigerian plants. The flavone
derivatives isolated by Khadem and Mohammed (1958) were reported to inhibit the
growth ofStaph. aureus in a dilution of 1:10000.
Uvaria chamae Beauv. syn. (U. cylindrica Schum. & Thonn., U. cristata R. Br. ex
Oliv., U. nigrescens Engl. & Diels, U. echinata Chev.) ANNONACEAE
L The root is regarded in Nigeria and Ghana as a purgative and antipyretic. The
rootbark is used in the treatment of dysentery and respiratory catarrhs. The juice of
135
the leaves is sometimes applied to wounds and sores or an infusion is used as a lotion
for injuries, swellings, ophthalmia, etc. (Dalziel, 1937).
Tannins and alkaloids were reported to be present in the roots and stembark by
Persinos and Quimby (1967). C-benzylated flavonoids have also been isolated,
including a C-benzylated monoterpene, chamaenen, dihydrochalcones and
flavanones (chamanetin 5-methyl ether and dichamanetin methyl ether) (Lasswell,
1977; Hufford and El Sohly, 1978; Hufford and Lasswell, 1978; El Sohly et al.,
1979; Leboeuf and Cave, 1980).
The MIC values of these flavonoids and certain of their derivatives against
Staphylococcus aureus, Bacillus subtilis mdMycobacterium smegmatis compare favour-
ably with those of streptomycin sulphate. No activity was observed against
Escherichia coli and the fungi Aspergillus niger and Saccharomyces cerevisiae. The
dihydrochalcones were slightly more active than the flavanones. A number of the
C-benzylated flavonoids are also cyto toxic. A larvicidal compound in this
Annonaceae was also found to be a benzylflavanone (Towers and Wat, 1979).
Allium sativum L. LILIACEAE

Garlic
Allium cepa L.
Onion
These plants have already been mentioned as possessing hypotensive and anti-
diabetic properties (see CV). As they also have major antibiotic properties, they
deserve mention here. In fact they are very potent fungicidal and antibacterial
agents, useful in the treatment of fungal and staphylococcal skin and alimentary tract
diseases (Vohora et al., 1973). The unusually strong action of the Allium spp. in
Candida infections is of great importance as there are few active antibiotics which can
be used in dermatology cases (Tynecka and Gos, 1973).
The antibiotic effects have been attributed to the action of allicin (diallyl-
disulphide oxide) (which is contained in the juice of garlic and onion) on the growth
and respiration of microorganisms such as Candida albicans, Staphylococcus aureus
and Escherichia coli. Candida was the most sensitive of these organisms to allicin,
whilst E. coli seemed to be more resistant than Staph. aureus (Kabelik, 1970) The
- S O - S - grouping is essential for the bacterial action of allicin as it inhibits the - S H -
enzymes whereas - S - S - , - S - and - S O - groupings were not effective (Willis, 1956).
It has been observed that the permeability of bacterial cells to allicin is greatly
influenced by the lipid content of the microorganisms (Small et al., 1949). E. coli
contains about 20% lipids in the cell wall as compared to only about 2% in Staph.
aureus, which may account for the fact that allicin more easily penetrates Staph.
aureus cells as low lipid content facilitates penetration. The optimum conditions for
the action are obtained in combination with oxidizing agents, which improve the
antibiotic effect. The therapeutic effect of allicin is weakened through reduction and
in the presence of blood; it is inactivated by cysteine but can be reactivated by H 2 O 2
and reduced by thiosulphates (Kabelik, 1970). The allicin content of the bulbs varies
with origin, moment of vegetation and soil conditions. In storage the amount
136
decreases, depending on the storage conditions and species. Besides allinin, from
which allicin is formed, Allium spp. contain several other sulphoxides which are
converted by allinase to allicin analogues.
Capparis decidua (Forsk.) Edgew. syn. (C. aphylla Hayne ex Roth, Sodada decidua
Forsk.) CAPPARIDACEAE
The root and rootbark are pungent and bitter and are given in Persia and India for
intermittent fevers and rheumatism. They are also used for boils and swellings of the
joints and for their anthelmintic action (Dalziel, 1937; Chopra et al., 1956).
In the non-saponifiable petroleum ether fraction of the rootbark of the Indian plant,
Gaind and Juneja (1969) identified w-pentacosane, triacontanol and /3-sitosterol, and
in the alcoholic extract two alkaloids, one of them being (-)-stachydrine, were
found. From the flowers and fruits, w-pentacosane, /3-sitosterol, (—)-stachydrine,
choline and phthalic acid could be isolated. Flowers and seeds yielded 0.4% and
0.6%, respectively, of a volatile material composed of an organic sulphur compound.
Later, Juneja et al. (1970a, b) identified glucocapparin (an isothiocyanate glucoside)
in the seeds.
An aqueous extract of the flowers, fruit pulp and rootbark has been found to have
anthelmintic properties on earthworms (Gaind et al., 1969a). Whereas the alcoholic
extracts of flowers, fruit-husks and seeds were highly active against Staphylococcus
aureus, Escherichia coli, Bacillus subtilis, Proteus vulgaris, B. megaterium and Vibrio
cholerae iinaba), none had antifungal properties. A steam-volatile organic sulphur
containing compound from the seeds showed both high antibacterial and antifungal
action particularly at dilutions of 50 /xg/ml against Aspergillus flavus, Penicillium
echyogenum and Candida albicans (Gaind et al., 1969b, 1972) and of 25 /mg/ml against
V. cholerae. In the case of V. cholerae ogawa complete inhibition was obtained with
25 fJLg/ml within 5 h, in that of V. cholerae inaba within 13 h and in the case of
V. cholerae el tor in 5 h when the dose was 60 /ng/ml (Gaind et al., 1972).
Moringa oleifera Lam. syn. (M. pterygosperma Gaertn.) (Fig. 4.3) MORINGACEAE
Horseradish tree
Some properties of this plant and of the sulphurated amino bases of the rootbark of
moringa have been described earlier (see CV). As mentioned the roots contain three
antibiotic constituents, pterygospermine, athomine and spirochine.
Pterygospermine is a condensation product of two benzylisothiocyanate molecules
with one benzoquinone molecule. This substance has powerful antibiotic and
antimycotic effects. The toxicity of pterygospermine in the mouse (LD 50 ), given
perorally, is 350-400 mg/kg, whilst at higher doses all animals die from respiratory
arrest. The purified or crystallized pterygospermine has a broad antibacterial
spectrum, acting on Gram-positive and Gram-negative organisms including Micro-
coccus pyogenes var. aureus, Bacillus subtilis, Escherichia coli, Aerobacter aerogenes,
Salmonella typhi, Salm. enterides, Shigella dysentariae andMycobacterium tuberculosis.
Pterygospermine further inhibits filamentous fungi, including plant parasites.
Thiamine and glutamic acid antagonize its antibiotic action, whilst pyridoxine
137
enhances it (Kurup and Narasimha-Rao, 1954; Watt and Breyer-Brandwijk, 1962;

Kerharo, 1969). The antibacterial action of pterygospermine on M. pyogenes appears
to be based on its interference with the glutamic acid metabolism of the micro-
organism (Eilert et al., 1981).
Athomine, the second antibiotic substance, is particularly active against the
cholera vibrion, showing a degree of activity which is intermediate between that of
chloramphenicol and streptomycin (Chatterjee in Watt and Breyer-Brandwijk,
1962). This substance is entirely non-toxic to the rabbit (Kurup and Narasimha-Rao,
1954; G u p t a s a/., 1956; Das etal., 1957a, b; Kurup et al., 1957).
The third antibiotic in the roots is spirochine, a sulphurated amino base which also
acts on the myocardium. When administered intramuscularly or in local application
spirochine is prophylactic and antiseptic against wound infections even in patients
with a marked existing infection. Its action against Staphylococcus aureus is observed
at a dilution of 1:70000 in vitro (Chatterjee, 1951 in Watt and Breyer-Brandwijk,
1962, p. 782). It has been observed to promote epithelization and some analgesic and
antipyretic activities have been attributed to spirochine as well.
In the seeds of Moringa oleifera another derivative of benzylisothiocyanate (a
glycosidic mustard oil) has been reported (Das et al., 1958). This is 4(4'-acetyl-
Fig. 4.3. Moringa oleifera Lam.
•'< i
138
a-L-rhamnosyloxy)-benzylisothiocyanate, a compound which has proved to have

bactericidal action in a concentration of 56 /xmol/1 against B. subtilis and of 40 /u,mol/l
against My cob. phlei. It has proved more effective than the currently used
isothiocyanate and could be a welcome substitute (its pure crystals being non-
volatile, water-soluble and easy to handle) (Das et al. ,1958; Kjaer et al., 1979; Eilert
etal, 1980, 1981).
The seed oil is used for lubrication and in cosmetics and the seed itself finds use in
the Sudan and elsewhere as a natural coagulant for water purification (Eilert et al.,
1980,981).
Ekebergia senegalensis A. Juss. syn. (Charia chevalieri D C , E. chevalieri (DC.)

Harms, C. indeniensis Chev., E. indeniensis (Chev.) Harms, E. dahomensis Chev.)
MELIACEAE
Mainly a timber tree, according to Sebire, the bark is used locally in Senegal for
epilepsy (Dalziel, 1937).
From the roots a bitter principle related to calicedrin has been extracted by Paris and
Moyse-Mignon (1939). This has been identified by Bevan et al. (1965) as a mixture
of two meliacins, which were named ekebergalactones B and C.
Paris and Moyse-Mignon (1939) noticed that the water extract of the leaves stupefied
goldfish and concentrations of 3 g/1 killed them. Gaudin and Vacherat (1938) also
noticed the ichthyotoxic effect of the macerated leaves. The stembark gave positive
results for Staphylococcus aureus and Sarcina lutea in short antimicrobial tests on a
series of Nigerian plants on Gram-positive organisms (Malcolm and Sofowora,
1969).
Carica papaya L. (see also CV) (Fig. 4.4) CARICACEAE

The aglycone of tropaeolin, a benzylisothiocyanate found in the seeds of C. papaya,
has been studied for its antibiotic and pharmacological activity and for its toxicity.
Maximum antibiotic action has been achieved with freshly crushed seeds and the
average concentration of 6 mg/g of seeds has proved sufficient for therapeutic
purposes. An antifungal effect has been found useful in the treatment of fungal skin
diseases and benzylisothiocyanate may be a useful bactericidal agent for intestinal
and urinary infections, being active against a wide range of microorganisms and
eliminated in the urine 3-6 h after administration (Georges and Pandelai, 1949).
Further the toxicity of the seeds is low; the therapeutically effective single dose of
4-5 g of seeds (25-30 mg of benzylisothiocyanate) is believed to be innocuous (El
Tayeb et al., 1974). The seeds also have anthelmintic activity (Krishnakumari and
Majumdar, 1960; Dar et al., 1965) and are carminative. Ripe and unripe fruits
(epicarp, endocarp and seeds) showed very significant antibacterial activity on
Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa and
Shigella flexneri (Georges and Pandelai, 1949). The MIC was 0.2-0.3 mg/ml for
Gram-positive organisms and higher (1.5-4 mg/ml) for Gram-negative organisms.
The purified bactericidal agent showed protein-like properties (Emeruwa, 1982).
Papain, an enzyme present in the fruit, has proteolytic properties. It is reported to
139
be an anticoagulant (Pillai et al., 1957) and may contribute to the antibiotic action.
The leaves contain the alkaloid carpaine, which has amoebicidal action (Burdick,
1971).
Borreria verticillata (L.) Mey. syn. (Spermacoce verticillata L., S. globosa Schum. &
Thonn.) RUBIACEAE
L The plant is mainly found in the wet season and is used as an anti-eczematic in parts
of Nigeria. The juice obtained from the aerial parts is applied topically (Benjamin,
1979). In East Africa the plant is also used in the treatment of skin diseases
(Kokwaro, 1976).
C Two major indole alkaloids, borrerine, which appears to be a condensation product
of tryptamine with isoprene, and borreverine, which may be formed by the union of
two borrerine molecules, have been isolated by Pousset et al. (1973) from the aerial
parts of the plant. These authors have not, however, been able to confirm the
presence of emetine in the roots as had been reported by Orazi (1946). Seven iridoids
have been isolated from B. verticillata rootbark (Sainty et al., 1981).
Fig. 4.4. Carica papaya L.
t» *r
140
P An antibacterial action of borreverine towards Staphylococcus aureus and Sarcina

lutea has been reported by Maynart et al. (1980). The air-dried aerial parts provide a
brown oil after several extractions. This oil inhibits the growth of Gram-positive and
Gram-negative bacteria, and has been separated by chromatography into a hydrocar-
bon and an oxygenated terpene fraction. Purification of the hydrocarbon fraction
produces a sesquiterpene fraction containing gaiene, caryophyllene and cadinene.
This fraction inhibits the growth of Escherichia coli but not of Staph. aureus. The
oxygenated terpene fraction, violet with a pungent smell, inhibits both E. coli and
Staph. aureus. Evidence for antibacterial action of a sesquiterpenic lactone has been
provided (Benjamin, 1979). Research designed to reveal insecticidal action has given
no significant results (Heal and Rogers, 1950).
Xylopiaaethiopica(Dunal) A. Rich. syn. (Annonaaethiopica Dun.,X. eminiiChev.)

ANNONACEAE
Guinea of Ethiopian pepper, spice tree
L In Nigeria the fruits are used as a cough cure, a carminative and a stimulating
additive to other remedies. A fluid extraction or a decoction of the fruit or bark is
recommended in the treatment of bronchitis, dysentery and biliousness. An extract
of the seeds is also used to eliminate roundworm. The fruit is used as a condiment
(Dalziel, 1937).
C From the fruit of the Nigerian species xylopic acid, a new diterpenic acid (15
/3-acetoxy(-)kaur-16ene-19-oic acid), three diterpenic alcohols, one of them iden-
tified as kauran-16-a-ol, 4 diterpenic acids, including kaurenoic and 15-oxo-
kaurenoic acid, two acyclic compounds, fats, oils and an essential oil have been
obtained and cuminal (isopropylbenzaldehyde) has been obtained from the seeds
(Ekong and Ogan, 1968; Ekong et al., 1969a; Ogan, 1971).
P An extract of the fruit has been found to have some antibiotic effect on Sarcina lutea
and Mycobacterium phlei (Malcolm and Sofowora, 1969) and on Staphylococcus
aureus, Bacillus subtilis, Pseudomonas aeruginosa and Candida albicans. It is, however,
inactive against Escherichia coli (Boakiji Yiadom et al., 1977). This action seems due
mainly to xylopic acid and to a lesser extent to two other diterpene isolates. The effect
of xylopic acid is comparable to that of chloramphenicol.
Azadirachta indica A. Juss syn. (Melia azadirachta L., M. indica (Juss.) Brandis)
(Fig. 4.5) MELIACEAE
Neem, margosa tree
(Considerable confusion between this tree and Melia azedarach is found in the
literature and must be watched!)
L Introduced and now naturalized in West Africa and Nigeria, this tree is mainly
ornamental. The seed oil (margosa oil or neem oil) is used in India for the treatment
of skin diseases and as a hair tonic (Indian Pharmacopoeia). The dried flowers find
use as a tonic and stomachic and an infusion or tincture of the dried bark as a tonic
and antipyretic.
141
In India the seed oil has been found to contain bitter constituents. Those reported
have been mainly 1.1% nimbidin (containing sulphur) and 0.1% nimbin and 0.01%
nimbinin (both free from sulphur), which also occur in the stembark (Chatterjee et
al., 1948). Meliacins found in the seeds include gedunin, 7-desacetylgedunin,
desacetylnimbin and azedarachtin (Manske and Holmes, 1950-71, Vol. 5, p. 423).
From the flowers a flavonoid, nimbicetin, later found to be identical with
kaempferol, has been isolated, together with a bitter substance and a pungent bitter
essential oil. In the dried bark the same bitter components as in the seed oil have been
found, and in the pericarp of the fruit a bitter principle, bakayanin, has been found
(Narayanan and Iyer, 1967). From the Nigeria species El Said et al. (1968) isolated
nimbin, nimbidol and other bitter tetra-nor-triterpenoids as well as a resin and a
tannin. Ekong et al. (1969b) obtained two new meliacin cinnamates, nimbolin A and
B, from the wood of the trunk besides a small quantity of nimbin, fraxinellose and
gedunin. In the fresh leaves they found deacetylnimbine and a lactone, nimbolid.
Fig. 4.5. Azadirachta indica A. Juss.

142
In India, a marked antibacterial action of the seed oil on Gram-positive and

Gram-negative organisms and even against resistant strains of tuberculosis has been
reported. The growth of all strains of Mycobacterium tuberculosis and Micrococcus
pyogenes var. aureus was inhibited by a concentration of 1:800000 and the growth of
Shigella typhosa, Salmonella paratyphi and Vibrio cholerae inaba was notably inhibited
by a concentration of 2 mg/1; that of Klebsiella pneumonia by concentrations of 5 mg/1
(Murthy and Sirsi, 1957; 1958). Nimbin and nimbidin also inhibited potato virus X
(Verma, 1974). The leaves appear to be insecticidal and are used in India to protect
woollen fabrics and books against insects (Chopra et al., 1956). The triterpenoids of
the seeds have been reported to repel certain parasites of cultivated plants and to
have antiviral as well as antibacterial properties (Rai and Sethi, 1973; Anisimov et
al., 1974; Kraus etal., 1978).
Azedarachtin, together with warburganal from East African Warburgia cyanensis,
is considered one of the strongest antifeedants of African army worms hitherto
discovered (Kubo et al., 1977).
An aqueous extract of the root has been reported to reduce sarcoma 180 (Abbot et
al., 1966). An aqueous extract (1:1000) of the leaves of the Nigerian tree was found
to act on the isolated guinea pig intestine, to contain a histamine-like substance
(Oladele Arigbabu and Don Pedro, 1971) and to cause, on intravenous injection in
the dog, an initial increase in blood pressure followed by a prolonged decrease with
accelerated breathing (Luscombe and Taha, 1974; Thompson and Anderson, 1978).
The fresh leaf extract has also been shown to have hypoglycaemic and anti-
hyperglycaemic effects in dogs. When injected intravenously it prevented
adrenaline-induced, as well as glucose-induced, hyperglycaemia. This action lasted
from 30 min to 4 h after administration (Satyanarayan Murty et al., 1978).
Anti-inflammatory and antipyretic properties of Azadirachta leaf extract have been
reported in Nigeria by Okpanyi and Ezeukwu (1981).
Acalypha wilkesiana Mull. Arg. EUPHORBIACEAE

Cultivated (from tropical Asia)
In Nigerian local medicine the plant is administered in the form of a tincture, a
decoction or an infusion. The leaf juice, obtained by rubbing the leaves between the
palms of the hands, is smeared on parts affected by Pityriasis versicolor or similar
types of fungal skin infections. Alternatively, the decoction of the leaves may also be
drunk by itself or in combination with other remedies.
The active principle responsible for the antimycotic and antimicrobial action is
being investigated by the agar diffusion method (Adesina et al., 1980b).
Five different extracts have been tested (the preparation of each extract including a
number of chemical operations) against seven test organisms and marked anti-
microbial properties (inhibition zone over 15 mm) have been displayed against
Bacillus subtilis, Staphylococcus aureus and B. cereus by extract B and to a certain
extent against Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris and Serrata
marcescens. (Adesina et al., 1980b).
143
Eclipta prostrata (L.) L. syn. (E. alba (L.) Hassk., Verbesina prostrata L.)
COMPOSITAE
In Nigeria the plant is used as a pot-herb and in Ghana it is used to combat
constipation (Dalziel, 1937). In India and in Senegal (Wolof) the root is considered
emetic and purgative and is applied externally as an antiseptic to ulcers and wounds
(Chopra etal., 1956; Kerharo, 1968). The leaves can also be used but are less active.
The plant has been reported to contain the alkaloid nicotine (0.08%) (Pal and
Narasimhan, 1943). The leaves have been found to contain wedelolactone and
desmethylwedelolactone and its glucoside besides polyacetylenes and their
thiophene derivatives (Govindachari et al.., 1956; Dhar et al., 1968) and the presence
of free triterpenoids in the leaves has also been observed (Kerharo and Adam, 1974).
The alcoholic extract of the plant has been reported to have antiviral activity against
Newcastle disease virus. The leaves and the polyacetylenes of E. prostrata were
highly active when exposed to UV light (phototoxicity) to microorganisms in
antibiotic tests against Escherichia coli, Saccharomyces cerevisiae and Candida albicans
(Dhar et al., 1968; Towers and Wat, 1979; Wat et al, 1980).
For a more comprehensive list of plants with antibacterial action see Table 4.1.
(b) Antifungal plants

The fungicidal substances present in some plants appear to play an
important role in the defence against invasion by cryptogamic parasites. Thus a high
concentration of sanguinarine just beneath the epiderm of the roots of Berberidaceae
and Sanguinaria has suggested defence against root-rot fungi (Phymatotricum
omnivorum). Similarly, solanine accumulation, observed around wounds in potatoes,
has been considered a defence against Fusarium avenaceum (dry rot disease) (McKee,
1955).
Active constituents
The plant constituents with antifungal properties are often the same
constituents or similar to those that are active against other microorganisms. They
include flavonoids like tetra- and trihydroflavones, glycoflavones and kaempferol as
in Cassia occidentalism, C. alata*, C. tora*, Euphorbia prostrata*, E. thymifolia* and
Phyllanthus niruri*; polyphenols, like those of Anacardium occidentale (anacardic
acid), Chlorophora excelsa (chloropherin) and Cocos nucifera; naphthoquinones like
plumbagin in Plumbago zeylanica* and senevols as in Allium sativum*, Lepidium
sativum and Carica papaya. Triterpene glycosides are also reported to inhibit fungal
growth (Olsen, 1975). All of these have already been mentioned under the chemical
groups of the antibacterial plants. These plants are mainly used for fungal skin
diseases and are applied locally. Simeray etal. (1981) noted that in Europe antifungal
plants are mostly found amongst Liliaceae, Scrophulariaceae (containing
saponosides), Leguminosae, Compositae and Rhamnaceae.
Table 4.1. Antibacterial plants
The names are given here without the authorities; these are mentioned in the Botanical Index. The names of the infectious organisms are "
abbreviated as follows: B., Bacillus; Cor., Cory neb acterium; Ent., Entamoeba; Ep., Epidermophyton; Esch., Escherichia; M., Microsporum; My cob.,
Mycobacterium; Ps., Pseudomonas; Rh., Rhinosporidium; Sacch., Saccharomyces; Salm., Salmonella; Sh., Shigella; Staph., Staphylococcus; Strep.,
Streptococcus; Tr., Trichophyton.
Plant Part used Active constituent(s) Action/acts on References

Acantospermum hispidum Leaves Essential oil B.pumilis, B. subtilis, Cor. B. Jain and Kar(1971)
diphtheriae, Salm. typhi, Sh.
dysenteriae
Achyranthes aspera Seeds Oleanolic glycoside Leprosy Gopalchari and Dhar (1958)
Ojha era/. (1966)
Alafia multiflora Latex Alcohol-phenol, vanillic acid Staph. aureus, Strep, faecalis, Balansardera/. (1980)
Esch. coli, Ps. aeruginosa
Ananas comosus Juice Bromelain (enzyme) Antibacterial, anthelmintic Shukla and Krishnamurti
(1961a, b)
Sakkawala era/. (1962)
Argemone mexicana Leaves, stems Berberine, sanguinarine (acts as My cob. tuberculosis, Staph. aureus, CV
lipolytic prodrug allowing Salm. typhi, Esch. coli, Sh. Lambin and Bernard (1953)
greater intracellular penetration) dysenteriae Mitscher era/. (1978)
Bombax malabaricum, B. Seeds Gallic acid, ethylgallate Staph. aureus, Esch. coli Dhar and Munjal (1976)
buonopozense?
Butyrospermum paradoxum Nut (fat) Triterpenic alcohols Sarcina lutea, Staph. aureus, Malcolm and Sofowora (1969)
subsp. parkii 'in butter' Mycob.phlei Mital and Dove (1971)
Calotropis procera Latex Calotropain (enzyme) Micrococcus leirodeikticus Shukla and Krishnamurti
(1961b)
Sakkawala etal. (1962)
Cannabissativa Resin, leaves Phenols (2.15% in leaves) Gram-positive organisms, B. N
megaterium, Staph. aureus, Nickel (1959)
Esch. coli Veliky and Genest (1972)
Fournier etal. (1978)
Capsicum annuum Fruit Capsicidin (steroid saponin) 'Antibiotic', yeast {Saccharomyces Gal (1964,1967)
cerevisiae)
Cardiospermum halicacabum Seeds Essential oil Ophthalmias N
Modi and Deshmankar (1972)
Shukla^fl/.(1973)
Carica papaya Fruit, seeds Protein Staph. aureus, B. cereus, Esch. Emeruwa(1982)
coli, Ps. aeruginosa, Sh.flexneri;
0.2-0.3 mg/ml for Gram-
positive organisms and 4 mg/ml
for Gram-negative organisms,
of purified extract
Cassia absus Seeds Chaksine, isochaksine B. haemolyticus, Staph. aureus InayatKhanâ/.(1963)
Cheema and Priddle (1965)
Centella asiatica Leaves, stem Asiaticoside My cob. tuberculosis, B. leprae, N
Ent. histolytica Bhattacharya and Lythgoe
(1949)
/. (1949)
Cnestis ferruginea Roots, leaves Squalene, myricyl alcohol, Sarcina lutea, Staph. aureus Malcolm and Sofowora (1969)
/3-sitosterol, methyl-linolenate Boakaiji Yiadom and Konnig
homologues (1975)
Olugbadeera/.(1982)
Crateva religiosa Stembark Total extract Sh. dysenterica N
Cyperus rotundus Plant Obturastyrene (cinnamylphenol) Staph. aureus Towers and Wat (1979)
Khan era/. (1980b)
Diospyros mespiliformis Rootbark Plumbagin Staph. aureus, Cor. diphtheriae, CV
also antifungal Paris and Moyse-Mignon (1949)
Goutam and Purohit (1973)
Steffen and Peschel (1975)
Dracaena manni Rootbark Sarcina lutea, Staph. aureus, N
Mycob.phlei Malcolm and Sofowora (1969)
Sofowora and Olaniji (1975)
Ekebergia senegalensis Stembark Saponin? meliacin? Staph. aureus, Sarcina lutea, N
also ichthyotoxic (leaves) Malcolm and Sofowora (1969)
Eucalyptus globulus Leaves Phenol acids, essential oil Antitubercular (Mycob. Low etal. (1974)
tuberculosum) Boukef<?ra/.(1976) ^
(Table continued) KJ\
Table 4.1 (Continued)
Plant Part used Active constituent(s) Action/acts on References

Guierasenegalensis Leaves Gallic and catechuic tannins Choleriform diarrhoea Kerharo era/. (1948)
Khaya senegalensis Bark Meliacins Sarcina lutea, Staph. aureus, N
Paramecium coli
Lasiosiphon kraussianus Roots Heteroside Bacillus leprae Tubery(1968)
Lawsonia inermis Leaves Lawsone, gallic acid Bactericidal CV
Carrara and Lorenzini (1946)
Bendz(1956)
AbdElMalikera/.(1973)
Khorrami(1979)
Mangifera indica Kernel Mangiferin, ethylgallate, Antibiotic and anthelmintic CV
phenylpropanoids Singh and Bose (1961)
Malcolm and Sofowora (1969)
Momordica charantia Leaves Aqueous extract Esch. coli, Staph. aureus Georges and Pandelai (1949)
Moringa oleifera Roots Athomine Vibrio cholera Sen Guptaetal. (1956)
Pterygospermine B. subtilis, Staph. aureus, My cob. CV
phlei, Salm. typhosa Kurup and Narasimha-Rao
(1954)
Kurup etal. (1957)
Ocimum basilicum Plant Thymol, eugenol Antimicrobial (Gram-positive N
bacteria and mycobacteria), Jain and Jain (1972)
antiparasitic Jainet at. (1974)
Valnet etal. (1978)
Ocimum canum Plant Camphor Gram-positive bacteria and N
mycobacteria Balansard(1936)
Jain and Jain(1972)
Jain*ra/.(1974)
Piper guineense Fruit, leaves Piperine, amide-alkaloids Mycob. smegmatis in concentration N
(terpenes), dihydropiperine of 100 /xg/ml, also Candida DwumaBaduera/. (1976)
albicansfMycob. smegmatis AddeaMensahe?a/. (1977)
and Klebsiella pneumoniae
(100/ig/ml)
Polygonum salicilifolium, Leaves, roots, Flavonoids Saint, typhi, Sh. dysenteriaey Abd El-Gawad and El Zait
P. senegalense stems B. subtilis, Esch. Coli (1981)
Salvadora persica Leaves, twigs Organic sulphur compounds (Tooth brush and chewing stick) Faroqui and Srivasta (1968)
Bactericidal Ray era/. (1975)
Lewis and Elvin-Lewis (1977)
Etkin(1981)
Ezmirlyera/. (1979)
Oil Trimethylamine derivatives Githens(1949)
Sida acuta, S. cordifolia Aerial parts Cryptolepine and vasicine Antibacterial, Proteus vulgaris Gunatilaka etal. (1980)
(600/xg/ml) Prakash era/. (1981)
Solarium nigrum {S. Leaf Solanine Staph. aureus, Candida albicans N
nodiflorum)
Strychnos afzelii Stembark (Chewing stick) dimeric indole Strep, mitis, S. mutans, S. sanguis Verpoorte era/. (1978,1983)
alkaloids
Tabernaemontana glandulosa Bark Hydroxycoronaridine and Antibiotic Patella/. (1967)
hydroxyibogamine Aschenbach era/. (1980)
Terminalia glaucescens, Bark Gallic tannins Gram-positive organisms; Sarcina Delaveau etal. (1979)
T. avicennoides lutea, Staph. aureus, My cob. phlei Malcolm and Sofowora (1969)
Thalictrum rugosum Leaves Thaliadanine (alkaloid) Mycob. smegmatis CV
Mitscheretal. (1972c)
Wuera/.(1976)
Liaoetal. (1978)
Thevetia neriifolia Leaves, fruits Aucubigenol Antibiotic CV
Paris and Etchepare (1966)
Sticher and Meier (1978)
Tiliacorafunifera Funiferine Mycob. smegmatis Ayimetal. (1977)
Withania somnifera Leaves Withaferine (steroidal lactone) Gram-positive and Gram- N
negative organisms, also Sethi etal. (1974)
antifungal Merck's Index (1976 (9716))
Ikram and Inamul-Haq (1980)
148
Cassia occidentalis L. CAESALPINIACEAE

Coffee senna, stinkweed
Cassia tora L.
Foetid cassia
The seeds of C. occidentalis have been used as a coffee substitute. In local medicine
the leaves are used as a purgative, febrifuge and diuretic and also as an eye lotion.
The dried or fresh leaves of C. tora are used in Northern Nigeria in the treatment of
ulcers, ringworm (Tinea cruris) and other parasitic skin conditions. The treatment
may consist of application of the powdered dried leaves or of a lotion made from a
decoction of fresh leaves.
The seeds of C. tora and C. occidentalis have been found to contain rhein,
aloe-emodin and chrysophanol as indicated by thin-layer chromatography studies
(Tewari et al., 1965; Shah and Shinde, 1969; Tewari and Rajbehari, 1972) and
extracts of C. occidentalis furnished in addition two pigments, physcion and
of-3-sitosterol and a xanthone (Ginde et al., 1970). In the leaves kaempferol and
probably a flavanone have been found by Anton and Duquenois (1968) and a major
fungicidal principle, chrysophanic acid anthrone, was isolated by Acharya and
Chatterjee (1974, 1975). The fresh seeds of C. occidentalis contain a phytotoxin
which loses its toxicity on roasting so that the seeds can be used as a coffee substitute.
Plant cell cultures in vitro of both species were antibacterial against Gram-negative
organisms (Quadry and Zafar, 1978). Antibiotic activity of C. occidentalis seeds
against Staphylococcus aureus, Bacillus subtilis, B. proteus and Vibrio cholerae and
against the fungi Aspergillus niger, A. flavus and Penicillium chrysogenum has been
reported by Gaind et al. (1966), who believe that this activity is due to the presence
of a volatile oil contained in the seeds.
Alcoholic extracts of C. tora leaves showed antibacterial action against Gram-
positive organisms and were also antifungal (Osborne and Harper, 1957; Shah et al.,
1968). The seeds were strongly antibiotic especially in patients with skin diseases
and Anton and Duquenois (1968) attribute this effect to chrysophanol derivatives of
kaempferol. C. tora was also found to have antiviral action against Newcastle disease
virus and Vaccinia virus (Dhar et al., 1968).
Cassia alata L. c. and naturalized CAESALPINIACEAE

Ringwormbush
The juice of the fresh leaves is universally recognized by the local healers as a remedy
for parasitic skin diseases, and is used in the treatment of many eruptive and pustular
skin conditions by simply rubbing the crushed leaves either alone or mixed with lime
juice or an oil, on the skin. In Ghana the juice of the fresh leaves is squeezed into the
eye to cure eye troubles (Irvine, 1930; Dalziel, 1937).
Anton and Duquenois (1968) reported that the leaves contain rhein and its glucoside,
aloe-emodol, small quantities of free chrysophanol, free kaempferol and probably a
flavanone. Chrysophanic acid is found in all parts of the plant, particularly in the
149
fruit. The residue after extraction of the leaves with a chloroform-ethyl alcohol
mixture produces by distillation an 'oil' containing sesquiterpenic and phenolic
compounds (Benjamin and Lamiranka, 1981).
The biological activity of C. alata leaf extracts is comparable to that of the medicinal
Senna species, the extracts being rich in anthrones and anthraquinone. They are
used as a purgative. The leaves were also used in the first half of this century by
'orthodox doctors' in West Africa in the form of an ointment made from a watery
extract in combination with lanolin, etc. in the treatment of crural ringworm (dhobie
itch), i.e. Tinea cruris (fungal skin disease caused by Trichophyton mentagrophytes,
Epidermophyton gloccosum, etc.) (Dalziel, 1937), An alcoholic extract of flowers and
leaves also had a certain antibiotic effect against Gram-positive organisms (Nickel,
1959). Antibacterial properties towards Bacillus mycoides, B. subtilis, Staphylococcus
aureus, etc. had already been reported in 1949 by Anchel. The activity of the 'oil'
prepared by Benjamin and Lamiranka (1981) on Gram-positive and Gram-negative
organisms including Pseudomonas has also been reported by these authors. Cassia
seeds are often discarded after the medicinal constituents have been extracted.
However, they may be valuable as sources of amino acids and proteins which
could be used to supplement diets, as suggested by Dale and Court (1981).
Arginine and aspartic and glutamic acids seem to be the main constituents in most
species.
Euphorbia prostrata Ait. EUPHORBI ACE AE

Euphorbia thymifolia L. syn. (E. burmannia Gay partly, E. aegyptiaca Soiss. andE.
scordifolia Jacq. of F.T.A. partly)
E. prostrata is considered in Northern Nigeria to be a good anthelmintic for
tapeworm and is used as a purge (Dalziel, 1937). The juice of E. thymifolia is used
locally in India in the treatment of skin diseases including ringworm {Tinea cruris)
and for snake bite.
The leaves and stems of E. thymifolia contain 5,7,4-trihydroxyflavone-7-glycoside
(Chopra et al., 1956; Sankara Subramanian et al., 1971) and Caiment-Leblond
(1957) isolated three flavone-derivatives by paper chromatography, including one
closely related to rutoside. E. thymifolia also proved to have insecticidal action (Heal
and Rogers, 1950).
The ether extracts of E. thymifolia and E. prostrata have been found to be highly
effective against sarcoptic mange in sheep (Lai and Gupta, 1970), and to have
powerful antifungal activity in vitro against Trichophyton mentagrophytes (Rao and
Gupta, 1970). This antifungal activity was repeatedly found by Pal and Gupta
(1971), who used petroleum ether and linseed oil extracts of the two plants and
observed activity against Tr. simii and Mycobacterium gypseum as well.
For a more comprehensive list of plants with antifungal action see Table 4.2.
150 151
Table 4.2. Antifungal plants
See also Chaumont and Bourgeois (1978) and Chaumont and Senet (1978).
Plant Part used Active constituent(s) Acts on/action References

Alpinia speciosa c. Rhizome Flavonoids Trichopkyton rubrum, Tr. Chopra etal. (1956)
A. officinarum and allied menlagrophytes, Epidermophyton Ray and Majumdar(1976)
species floccosum and antibacterial
A rgemone mexicana Leaves, stems, Berberine, chelerythrine Antibacterial (Table 4.1), anti- Adgina(1972)
root protozoal (Leishmania,
Trypanosoma lewis)
Seeds Sanguinarine (toxic) Phymatotrichum microsporum Greathouse(1939)
Bidenspilosa Leaves Phenylheptatriyene (phototoxic Anti-Candida albicans, wounds, Morton (1962)
polyacetylene, external use) ulcers, also toxic to certain Degener(1975)
insects and larvae, reacts with Wat«a/. (1978,1979)
DNA and kills human fibro- Tomassini and Mathos (1979)
blast cells (concentration
lOppm)
Carica papaya Seeds Benzylisothiocyanate Antifungal in skin diseases, El-Tayeb«a/.(1974)
antibacterial Emeruwa(1982)
Chlorophora excelsa Wood (leaves) Chlorophorin (phenol) Fungicidal (Rhinosporidium Amdt(1968)
(iroko) flavipes and R h. lucifungus) and Lewis and Elvin-Lewis (1977)
antibiotic, acts also against
termites
Cocosnucifera Nutshell Phenols Antifungal against 3 Microsporum GaindandSingla(1966)
and 4 Trichophyton spp. Malathi«a/.(1959)
(100/u.g/ml),and lEpider-
mophyton sp. (200 /^g/ml),
antitubercular
Desmodium gangeticum Roots Tannins in related species, Antifungal, antibacterial N
indole alkaloids Ghosaland Bannerjee (1968)
Haematoxylon campechianum Wood Ethylgallate Mycobacterium Little«a/.(1953)
Hygrophylaauriculata syn. Plant Steroid and triterpene Trichophyton rubrum Tr. Venkataraman and
(Asteracantha longifolia) glycosides mentagrophytes, Mycobacterium Radnakrishnan(1972)
gypseum, Candida albicans, also
acts on N. gonorrhoea
Hymenocallis littoralis Plant Lycorine Antifungal, antitubercular Verpoorteeta/. (1983)
Chaumont and Bourgeois (1978)
Chaumont and Senet (1978)
Chaumont etal. (1978)
Ieven«a/.(1978)
Lepidiumsativum c. & nat. Plant Glucotropeolin essential oil Fungicidal and bactericidal Githens(1949)
withsenevols Watt and Breyer-Brandwijk
(1962)
Phyllanthus niruri Roots Glycoflavones(kaempferol4'-and Ringworm (tinea cruris), N
eryodictyol 7-rhamnopyrosid ulcers, scabies, jaundice Chauhan eta/. (1977)
Pipernigrum Seeds Essential oil Fungicidal Chaurasia and Kher (1978)
Raina«a/.(1976)
Ricinuscommunis Oil Undecylenic acid prepared Fungistatic and antibacterial Oliver (1960)
from oil Tinea spp., moniliases Martindale(1958,p. 1331)
Paulose«a/.(1964)
152
(c) Antiviral plants

Viruses possess an outer coat, or capsid, of protein or lipoprotein and an inner core
of nucleic acid, either DNA or RNA, but not both. The viruses have an exclusively
intracellular mode of reproduction and like all living entities share a common
mechanism of replication at the molecular level. Hereditary traits of the virus can be
transferred from one type of cell to another by purified fragments of DNA. All
viruses exist in two basic forms, the metabolically inert transmissible virion and the
vegetative virus, an active constituent of the host cell. In situ fragmentation of the
RNA in polio virus has been reported by van den Berghe and Boeije (1973). Cohen et
al. (1964) had observed that extracts of Melissa officinalis (lemon balm plant) had
antiviral activity against several viruses (Newcastle disease, Vaccinia, Herpes
simplex and Semliki forest viruses) in eggs and in chick embryo fibroblast
monolayers. They considered the active principle to be a tannin, which attaches
itself to the virus and thus prevents its adsorption to the host cell receptors. The
antiviral activity was prevented by injection of gelatin into the eggs following
injection of the Melissa extracts. The authors explain this by dissociation of the weak
complex formed by the virus and the active principle (Kucera et al., 1965). Lysogeny
is attributed to the presence of bacteriophages in the bacterial genome.
The immunological character of some viruses, e.g. the influenza viruses, varies a
great deal, so it is difficult to prepare the appropriate vaccine in advance of an
outbreak of the diseases caused by these viruses, and a vast amount of research has
been done on the development of drugs which will prevent or cure new outbreaks
(Beveridge, 1977).
Certain viruses (arbo or toga viruses) are transmitted to Man and animals by
arthropods (mosquitos, flies, ticks) and they multiply in the arthropod as well as in
the vertebrate host. Their virion (RNA) is able to act as a mRNA in the host cell
(Beveridge, 1981).
Antiviral constituents of higher plants

Poliomyelitis virus. Antagonistic action on this virus is claimed for two
Apocynaceae, Plumeria rubra * and Allamanda cathartica, and is attributed to a bitter
glycoside, plumeried and a lactoflavone, fulvoplumierin. Antipoliomyelitis virus
action has also been reported for Anagallis arvensis cultivated in the area (A. pumila
widespread in West Africa, might be examined). Saponosides are believed to be
responsible for this action.
Vaccinia virus is antagonized by three members of the Caesalpiniaceae, Caesalpinia
bonduc*; Cassia fistula* and Caesalpinia pulcherrima. The latter also has an antiviral
action on the Influenza virus.
Influenza virus is antagonized by Canavallia ensiformis (through xanthones),
Drosera indica (through plumbagin) and by Gossypium* spp. (through gossypol).
Measles virus and coxsackie virus. Lycorine from Hymenocallis littoralis has an
antiviral effect on these viruses. For further details and references see the text and
Table 4.3.
153
Arbo-viruses, with a lipoidal envelope, are destroyed by salts of mono- and

poly-unsaturated acids from the roots of Olax latifolia (e.g. Aedes aegypti, which
transmits dengue fever).
Herpes simplex. Action on Herpes simplex has been obtained with gossypol from
Gossypium spp., with eugeniin from Syzygium guineense and with saponosides from
Anagallis arvensis.
Newcastle disease (fowl pest) provides a convenient test-condition for antiviral
activity and positive anti-Newcastle virus action has been noted in Anagallis arvensis,
Cassia fistula, Cocculus pendulus and Milletia congolensis.
Plumeria rubra L. (Fig. 4.6) APOCYNACEAE

P. alba L.
Frangipani
Use as a medicine is avoided in West Africa as the latex is a drastic purgative (Dalziel,
1937). In tropical America and East Asia it is sometimes used as a purgative and
abortifacient and to treat venereal diseases (Hager's Handbuch, 1977).
In the roots, plumericin, isoplumericin, their dihydro-derivatives and fulvo-
plumierin have been found (Hager's Handbuch, 1977). Rao and Anjaneyulu (1967)
and Rao et al. (1967) reported the presence in P. rubra bark of fulvoplumierin,
lupeol, /3-sitosterol and the bitter glucoside, plumeried (up to 2% in the bark), which
is also present in the leaves (these constituents had already been isolated from Indian
P. acutifolia by Rangaswani et al. in 1961). In the flowers kaempferol and quercetin
Fig. 4.6. Plumeria rubra L.

154
glycoside have been found, and the latex also contains lupeol and its acetate and
esters with fatty acids (Rangaswani et al., 1961; Rao and Anjaneyulu, 1967).
Fulvoplumierin is a lactoflavone; plumeried, also called agoniadin, is a pseudo-
indican glucoside (Malvan et al., 1974).
The bark of P . acutifolia is very toxic, producing vomiting and mydriasis and
slowing down the heart (Hagefs Handbuch, 1977, p. 783). Extracts of the stem have
been found to produce significant surface anaesthesia on the cornea of the rabbit
(Chak and Patnaik, 1972). In the guinea pig all extracts produced, by infiltration, an
anaesthesia lasting over 1 h. In mice all extracts prevented pain induced by
phenylquinone, but none of the extracts showed analgesic action in mice if pain was
induced by a hot plate or pinching of the tails. Spasmolytic activity was not specific
(Chak and Patnaik, 1972). Plumeried was found to be mainly purgative (in doses of
0.2-0.3 g in man) (Watt and Breyer-Brandwijk, 1962; Harrison et aL, 1973).
Antibiotic activity was reported for plumericin (Hager's Handbuch, 1977) and
fulvoplumierin has been shown to be bacteriostatic (tuberculostatic) in doses of 1-5
fxg. Extracts of P . rubra have also been shown to be highly active against the polio
virus (van den Berghe et al., 1978). P . rubra var. alba contains a lower percentage of
antibiotic constituents than P . rubra L. (Cochran and Lucas, 1958-59).
Cassia fistula L. (Fig. 4.7) CAESALPINIACEAE

Indian laburnum (cultivated in West Africa)
In India, the rootbark, seeds and leaves are considered laxative, the fruit is
cathartic and is applied in the treatment of rheumatism and for snake bite. The roots
are used as an astringent, tonic and febrifuge and the juice of the leaves in the
treatment of skin diseases.
The leaves of C. fistula have been found to contain free rhein, rhein glucoside and
sennoside A and B (Kaji et al., 1968). A butanol extract of the powdered stembark
contained tannins whilst the benzene extract yielded lupeol, /3-sitosterin and
hexacosanol (Sen and Shukla, 1968). From the alcoholic extract of the pods a new
anthraquinone (fistulic acid) was obtained and identified as l,4-dihydroxy-6,7-
dimethoxy-2-methylanthraquinone-3-carboxylic acid (Agrawal et al., 1972). In an
acetone extract of the flowers kaempferol and a proanthocyanidin (leucopelargonidin
tetramer) have been found and in one of the bark a leucopelargonidin trimer has been
found (Narayanan and Seshadri, 1972).
Lillykutty and Santhakumari (1969) studied the antibacterial action of the leaves,
stembark and fruit pulp of C. fistula and found the fruit pulp to be the most potent.
The ether-soluble fraction of the fruit pods had the most potent activity against
Staphylococcus aureus, Staph. albus, Bacillus megaterum, Shigella flexneri, Sh. Shiga
and Salmonella paratyphi A and B, and in vitro 1 g of this extract was more potent
than 1 /xg of chloramphenicol. This activity was attributed to the presence of rhein.
The acetone extract of root- and stembark was found to have antifungal action
against Trichophyton tonsurans, Tr. rubrum and T. megnini (rosaceum). In vitro 100 /x,g
155
of the rootbark proved more potent than 16 /xg of griseofulvin (Lillykutty and
Santhakumari, 1969). The activities might be due to the presence of flavonoids. The
pods and stembark of C. fistula have also been found to have antiviral activity against
Newcastle disease virus and Vaccinia virus (Cutting et al., 1965) and in addition
extracts of C. fistula also have a hypoglycaemic action in rats (Dhar et al., 1968). On
screening various extracts of 620 Indian plants for their antiviral activity (Balbar et
al., 1970) found that C. fistula extracts were amongst those which were most effective
against Vaccinia and Newcastle disease viruses. They inhibited the cytopathy of the
host viruses and also their replication in the cells of the host and were more effective
when given before or along with the virus. The virus-inhibitory activity of the plant
extracts is believed to be associated with some interferon-like factor.
Caesalpinia bonduc (L.) Roxb. syn. (C. crista L., C. bonducella (L.) Fleming,
Guilandina bonduc L.) CAESALPINIACEAE
Bonduc or nicker nut
L A decoction of the root is used in Guinea as an antipyretic, and a gargle for sore
throats is prepared from the boiled leaves. In India, the dried seeds are reputed to be
Fig. 4.7. Cassia fistula L.

156
antipyretic, styptic, tonic and anthelmintic {Hager's Handbuch, 1967-80, Vol. HI,
p. 561). In Nigeria, a decoction of the rootbark is used as a rubefacient and in cases
of dyspepsia, and the seed oil is considered to be a remedy for convulsions in Nigeria
and in South Africa (Watt, 1967).
The seed kernel was known to contain, besides 20-28% of albuminoids, 35% of
starch and 5-6% of sugars, a bitter glucoside, bonducin or guilandinin, a saponin,
a phytosterin (sitosterol) and an oil (20%). Neogi et al. (1958) separated the bitter
constituent into four fractions, A, B, C and D. Further analysis of the seeds
revealed three bitter principles, a-, /3- and y-caesalpin. These are diterpenic
derivatives with three aromatic rings and one lactone ring. Later, fourth and fifth
principles, 8- and e-caesalpin were reported and their formulas established
(Canonica et al., 1963, 1964, 1966; Qudrat-I-Khuda and Efran, 1964; Balmain et
al., 1967). The wood contains two dyes, brasilin and brasilein, which are related
to haematoxylin.
The alcoholic extract of four fractions produced slight hypotension in the dog and
depressed the heart of the frog. Fractions A and B were antibiotic, fraction B also
antipyretic and diuretic, and fraction D anthelmintic (Watt and Breyer-
Brandwijk, 1962). Alcoholic extracts of the roots and stems were found to have
an antiviral action against Vaccinia virus (Dhar et al., 1968). An antimalarial
action could not be detected (Spencer et al., 1947a). In India, the powdered seeds
were found to have an anti-oestrogenic activity in rabbits and mice, and an anti-
fertility action was noted in mice and rats (Bhide et al., 1976). Aqueous extracts
of the roots, stems and leaves showed a distinct action on sarcoma 180 (Abbot et
al., 1966).
Gossypium spp., Gossypium hirsutum, G. barbadense, etc. MALVACEAE

Cotton plant
A number of Gossypium spp. and hybrids are widespread in tropical and subtropical
West Africa. Many species have been cultivated and are naturalized and some are
now subspontaneous. Kano (Nigeria) has been a cotton market since the ninth
century. The seed floss provides the cotton and the seed oil is used locally as a source
of oil for cooking and cattle food. The husks are sometimes used as a fuel.
Medicinally, a cold infusion of the leaves with lime juice is said to give relief in
dysentery; the root is believed to be emmenagogic and oxytocic, the active part being
the rootbark. The leaves and crushed seed-kernels are applied to sores or as a
poultice to bruises and swellings and the lint is used as a dressing for wounds
(Dalziel, 1937).
Absorbent cotton wool is obtained directly from the seed floss as well as from card
strips and comber waste in cotton mills. The kernel oil is composed of 47.8% linoleic
acid, 23.4% palmitic acid and 22.9% oleic acid plus small amounts of myristic and
myristoleic acids and other fatty acids. The residual cake is rich in proteins (97%)
157
and contains most of the essential amino acids, together with flavonoid pigments
(glucosides of quercetol, kaempferol, isoquercetrin, etc.) while the pigment glands
of the seeds contain a toxic poly phenol, gossypol, which is destroyed by heating
(thus rendering the oil suitable for consumption) (Aizikov and Kurmukov, 1973).
The root bark contains a yellow oil which consists of furfur aldehyde, a phenolic acid
(probably 2,3-dihydroxy-benzoic acid), betaine, a phytosterol and a resin (with
1-2% gossypol).
Gossypol has been demonstrated to have antiviral activity and apogossypol formed
by deformylation of gossypol retains the potent antiviral activity but is at least 10
times less toxic for human Ep cell cultures (Abbot et al., 1966). Influenza virus is
inactivated by treatment with gossypol resulting in a 96-100% protection rate.
Both gossypol and apogossypol inactivate the enveloped virus para influenza 3 and
herpes simplex in vitro (Dorsett et al., 1975). The non-enveloped polio virus is not
affected by either agent. Incubation of infected cells with gossypol or apogossypol
does not alter subsequent plaque formation, indicating that the antiviral effect does
not occur within the cell (Vichkanova and Shipulina, 1972). From the roots of G.
hirsutum and G. barbadense, 6-methoxygossypol and 6,6'-dimethoxygossypol (di-
meric sesquiterpenes) have been isolated, respectively. They have proved to be
active in vitro against Penicillium and Cladisporum spp. and frequently inhibit
Aspergillus fumigatus (lung aspergillosis) (Stipanovic et al., 1975). When instilled
three times daily into the conjunctival sac of rabbits suffering from experimental
herpetic keratitis, a solution of 0.005-0.1% of gossypol could eradicate the infec-
tion (Maichuk et al., 1972; Dorsett et al., 1975). Gossypol had antiherpetic action
in infected mice on both oral and subcutaneous administration. It was, however,
more effective against dermotropic than against keratogenic strains of the herpes
virus. Further, a strong viricidal action against Influenza A2 virus (Frunze strain)
in vitro and in vivo (mice) has been reported for gossypol (Vichkanova and
Gorunyunova, 1972).
Gossypol is a nerve and cellular poison and hence before feeding cattle with
oil-cakes the pigment pockets should be eliminated in a pre-press process. Fed to
pigs in amounts of 0.02-0.03% of the total ration, gossypol causes liver congestion
and oedema especially in the lungs and body cavities, while the grazing of sows in
harvested cotton fields leads to abortion. A horse weighing 450 kg cannot tolerate
more than 450 g of oil-cake per day and dies when the dose is as much as 1.4 kg. Small
amounts over a long period cause a bad general condition and anaemia in calves and
sheep; larger amounts cause haemorrhage, inflammation, haematuria, muscular
weakness, respiration difficulties and paralysis. Abortion and blindness are also
reported (Steyn in Watt and Breyer-Brandwijk, 1962). The LD 100 for gossypol given
intraperitoneally to rats is 20 mg/kg, death occurring between the thirteenth and
twentieth day after the injection.
For a more comprehensive list of plants with antiviral action see Table 4.3.
158 159
Table 4.3. Antiviral plants

Allamanda cathartica Bark Plumericin, isoplumericin Antiviral to polio virus CV
Pai«a/.(1970)
WackerandEilmes(1975)
Anagallis arvensis Plant Oleanane triterpenes, curcubitacins Polio virus, Newcastle disease and Bhakuniefa/. (1969)
herpes viruses Amoros«a/. (1977,1979)
Yamada«a/.(1978)
Bezanger-Beauquesne et al.
(1980)
Caesalpinia bonduc Root, stem a- and /S-caesalpins, 5-caesalpin Anti-vaccinia virus, anthelmintic Dhar«a/.(1968)
Watt and Breyer-Brandwijk
(1962)
Caesalpinia pulcherrima Plant Alcoholic extract Influenza and vaccinia virus, also Watt and Breyer-Brandwijk
anti Gram-negative bacteria (1962)
and Candida spp. Cochranetal. (1966)
Dhar etal. (1968)
Ieven«a/.(1979)
Canavalia ensiformis Seeds Xanthones, canavanin (2-amino- Influenza virus and bactericidal, Kitagawa and Tomiy ana (1930)
44-guanidinooxybutyric acid), alsoinsecticidal Farley (1944)
canavalin HealandRogers(1950)
Burger (1960, p. 1103)
Thomson etal. (1964)
Muelenaere(1965)
Olson and Liener (1967)
Calharanthus roseus Roots, leaves a-Acylindolic acid = perivine A2 influenza virus Farnsworth«a/. (1968)
Citrus spp. Rind Hesperidin Vesicular stomatitus virus Kaleyra(1975)
WackerandEilmes(1975)
Hoizey«a/.(1978)
Cocculus pendulus and related Aerial parts Cocculidine, l%picrotoxin Newcastle disease virus Bhakuni«a/. (1969)
C. indicum
Desmodium gangeticum Roots Aqueous extract, flavonoids Antiviral, antibacterial N
Ghosal and Banerjee (1968)
Prema(1968)
Hymenocallis Kttoralis c. Plant Lycorine Antiprotozoal, moderate plaque Berghe, van den era/. (1978)
inhibition of measles and Ieven«a/.(1978)
coxsackie viruses
Maesopsis eminii Stems Saponoside Antiviral Soulimov«a/. (1975)
Chaumontâ/. (1978)
Milletia barteri Extract of Saponin Strongly viricidal to Newcastle Balbartfa/. (1970)
stems disease Soulimov«a/. (1975)
Olax latifolia Roots Mono- and poly-unsaturated Acts on arboviruses with lipoidal Jenkin(1973)
acids (salts) envelopes Soulimovtfa/. (1975)
Porterandia cladantha Root, stem Saponosides Viricidal, abscess, furunculosis, Balbaaetal. (1970)
bronchitis Soulimoveta/. (1975)
Syzygium spp. and related Buds Eugeniin Acts on herpes simplex virus in Takechi and Tanaka (1981)
S. guineense? (S. aromatica, concentration of 10 /u.g/ml
not in West Africa)
160
(d) Antiprotozoal plants

General tests for antiprotozoals were formerly carried out on paramecia,
which are non-pathogenic to man, but these proved to be of no value. The malaria
parasites, of which the most malignant is Plasmodium falciparum, have two main
phases: intracorporal, in Man, and extracorporal or exogenous in the mosquito
(Anopheles). The intracorporal phase has three distinct cycles: asexual (schizogony),
sexual (sporogony) and an extra-erythrocytic cycle in the liver. Thus Man is an
intermediary; the mosquito is the final host in which the sexual cycle is completed.
Trypanosomiasis is also conveyed by an animal vector, the tsetse fly (Glossina
morsitans). Similarly, in leishmania tropica the intermediate host is Phlebotomus
papatassi and visceral leishmaniasis is transmitted through the sandfly Phlebotomus
argentipes. In bilharzia the vector is the freshwater snail. In all these cases,
prophylactic action against insects and molluscs is an essential part of any campaign
against the disease.
Active constituents
The activity of chemical constituents (e.g. alkaloids) against protozoa such
as Trypanosoma lewisi is determined by the method of Hopp et al. (1976) in terms of
the immobility produced on the organism and is expressed as the average percentage
of non-motile organisms from four microscopic fields. Phenol and pentamidine are
comparatively tested as controls. In looking at the effects registered in this chapter,
it appears that in their activity against protozoa, the constituents seem to be
chemically less varied than in the preceding groups. Many are alkaloids.
Plasmodium spp. Apart from the antimalarial action of the alkaloid quinine from
Cinchona spp., which has been known for many years, brucine (or bruceolides?)
from Brucea antidysenterica, funiferine from Tiliacorafunifera, rhynchophylline from
Crossopteryx febrifuga and meliacins from Trichilia roka are said to act against
Plasmodium berghi.
Activity against Leishmania tropica has been observed with the alkaloids
echitamine from Alstonia boonei and berberine (also anti-amoebic) from Argemone
mexicana. The latter species also contains sanguinarine, which is trypanocidal.
Berberine is also found in Chasmanthera dependens, which has both anti-leishmania
and trypanocidal action. At one time berberine was also believed to be antimalarial
but Chopra et al. (1938) could show that berberine acts on the spleen, increasing its
volume and rhythmic contractions, and that the parasites thus liberated in the
peripheral circulation are then able to respond to quinine action. The diagnosis of
latent malaria as carried out by certain specialists is based on this property. Harmane
derivatives in certain plants like Acacia nilotica, Newbouldia laevis and Pauridiantha
lyalli are also antiprotozoal.
The motility of Trypanosoma lewisi can be inhibited by harmine, harmol, harmane
chloride, palmatine iodide and, most of all, sanguinarine derivatives (nitrate and
sulphate). These compounds caused 70-100% immobility of the test organisms after
1-24 h. The most active is sanguinarine from Argemone mexicana; it causes 100%
non-motility even at dilutions of 1:40000 and in vitro had eighty times the activity
of pentamidine on Trypanosoma lewisi. Palmatine from Zanthoxylum zanthoxyloides,
161
Chasmanthera dependens and Cocculus and Tinospora spp., at dilutions of 1:8000 led
to 95% non-motility after 1 h, but at dilutions of 1:16 000 only 70% non-motility was
achieved after 24 h (Hopp et al., 1976; Al-Shamma and Mitscher, 1979; Al-Shamma
et al., 1981). (The antiprotozoal action of Zanthoxylum zanthoxyloides and of
Anacardium, Plumbago, Drosera etc. have been mentioned under Antibacterial
plants.)
Conessine from Holarrhenafloribunda* bark has proved to be very active against
Entamoeba histolytica in intestinal and hepatic amoebiasis, preventing multiplication
of the amoeba. It was found to produce neurological side-effects and therefore its
clinical use was suspended. (Conessine is also active against Trichomonas vaginalis
and is now mostly used in the topical treatment of trichomoniasis.) Other antipro-
tozoal alkaloids have been found in Alchornea cordifolia (alchornine) and Mitragyna
inermis (rhynchophylline). Anti-amoebic effects have been observed with carpaine
from Carica papaya leaves, an ethanolic extract of Phyllanthus niruri* and borrerine
(closely related to emetine) from Borreria verticillata. Antiprotozoal activity is also
associated with some terpenoid and meliacin constituents. Thus Curcuma domestica *
rhizomes and the aerial parts of Euphorbia tirucalli* have also been reported as active
anti-amoebics, owing to the presence of sesquiterpenic ketones (turmerones) and
terpenoids, respectively, and the anti-amoebic effect of Euphorbia hirta* has been
attributed to euphosterol.
Paramecia are mentioned as responding to the meliacins from Khaya senegalensis,
Crossopteryx febrifuga* and Trichilia roka* and to pseudocedrelin fromPseudocedrela
kotschyi*, whilst Melia azedarach does not seem to be active against paramecia
(Spencer et al., 1947a). On the other hand, the triterpenic saponins in Paullinia
pinnata* are said to be active paramecidals. It is interesting to observe from this list
that the majority of the plants with antiprotozoal action are plants which show a
depressive action on the central nervous system.
Chasmanthera dependens Hochst. MENISPERMACEAE

L The leaves and juice are used locally as a dressing for fractures and mixed with shea
butter as an embrocation for pain, sprains, etc. An extract of the bark is given in the
treatment of venereal disease and as a tonic for physical and nervous debility
(Dalziel, 1937).
C The alkaloid berberine has been found in the roots. The related species C. palmata
from Mozambique contains bitter principles without nitrogen such as colombin,
chasmanthin, palmarin and 2-3% of alkaloids of the berberine group, namely,
colombamine, jateorhizine and palmatine (Oliver-Bever, 1968).
P C. dependens is used as a bitter tonic. Berberine sulphate is used in India in the
treatment of oriental sores; it inhibits Leishmania tropica in concentrations of
1:80000. The alkaloid is also a uterine stimulant (Oliver-Bever, 1968).
Curcuma domestica Valeton syn. (C. longa L.) ZINGIBERACEAE

Turmeric
L The plant is cultivated in West Africa in the forest areas and often grown in native
162
compounds as a dye plant for leather, palm fibre, etc. It is used amongst Moslems as
an anthelmintic, an eye wash and an ointment for skin diseases (Dalziel, 1937). In
India turmeric is the main constituent of curry powder and is used in local medicine
(fresh juice) as an anthelmintic and antiparasitic in the treatment of many skin
diseases. It is also said to be an ant repellent (Chopra et al.9 1956). In Vietnam
turmeric is taken as an anthelmintic and diaphoretic.
A colouring matter has been isolated from the rhizomes. It contains the curcumines
belonging to the dicinnamoyl-methane group and an aromatic oil, turmeric oil
(0.24% in the fresh rhizomes), composed of 25% terpene-carbon derivatives and
65% of sesquiterpenic ketones (turmerones) (Paris and Moyse, 1967, p. 78).
Sodium curcuminate administered intravenously to dogs in a dose of 24 mg/kg
doubles the rate of bile flow without any appreciable disturbance of the blood
pressure and respiration. It has in addition a powerful antibacterial action against
Micrococcus pyogenes var. aureus (Ramprasad and Sirsi, 1956). Basu (1971) compared
the antibacterial action of C. domestica to that of penicillin on Gram-positive
organisms and that of streptomycin on Gram-negative organisms, and showed that
C. domestica was less active than these antibiotics. Antiprotozoal activity against
Entamoeba histolytica has been reported for the alcoholic extracts of the rhizomes
(Dharer<z/.,1968).
Euphorbia tirucalli L. EUPHORBIACEAE

In India E. tirucalli latex is used as a fish poison. It is applied medicinally to warts
and used in the treatment of rheumatism and neuralgia (Chopra et aL9 1956). In
contact with the eye it is a dangerous poison, producing inflammation of the cornea
and iris (Crowder and Sexton, 1964). Ingestion of 'remedies' containing the latex can
produce ulceration of the gastrointestinal mucous membrane (Crowder, 1964 in
Kerharo, 1968).
The latex contains 75-82% of a resin and 14-15% of a rubber. From the latex three
terpenic alcohols have been isolated: taraxasterol, tirucallol and euphol (Haines and
Warren, 1949,1950; McDonald et ah, 1949). From the fresh latex, isoeuphorol has
been obtained, which, when the latex is dried out, is replaced in a few months by
euphorone, a ketone. The stem of E. tirucalli has been found to contain hentriacon-
tane, hentriacontanol, /3-sitosterol, taraxerol, 3,3'-di-0-methylellagic acid, ellagic
acid and also a glucoside which on hydrolysis produces kaempferol and glucose
(Gupta and Mahadevan, 1967).
Alcoholic extracts of the aerial parts of E. tirucalli were shown to possess antipro-
tozoal activity against Entamoeba histolytica (Dhar et al.9 1968; Rao and Gupta,
1970). The protozoal effect of Euphorbia hirta might be due to euphosterol, also
reported to be present in this plant (Watt and Breyer-Brandwijk, 1962). A fraction
of lyophilized extract, at a dilution of 1:200, had after 48 h the same anti-amoebic
effect as emetine hydrochloride at a dilution of 1:80000 after 24 h (Ndir and
Pousset, 1981).
The alcoholic and aqueous extracts of the stems were observed to reduce
adenocarcinoma and sarcoma to a considerable extent (Abbot et al,9 1966).
163
Holarrhenafloribunda(Don.) Dur. & Schinz var. floribunda syn. (H. africana D C ,

H. wulfsbergii Stapf, RondeletiafloribundaDon.) APOCYNACEAE
Conessi or kurchi bark
For local uses and chemical constituents see CV.
Holarrhena alkaloids and berberine hydrochloride were studied on intestinal
amoebiasis in rats and on hepatic amoebiasis in hamsters and their activity was
compared to that of emetine hydrochloride. All the alkaloidal fractions ofHolarrhena
effectively reduced the infection in rats and hamsters. Kurchamine appeared to be
one of the most promising active compounds. Berberine showed marked effective-
ness in both types of infection (Bertho, 1944). Berberine is also remarkably toxic
against Leishmania tropica, inhibiting the growth of Leishmania in vitro at a 1:80000
dilution. A 2% solution injected at the base of the lesion caused healing after 2-3
administrations (Chopra et al., 1932).
Clinical tests with conessine on patients with intestinal and hepatic amoebiasis
have been found to give results comparable to those obtained with emetine. Use of
conessine must, however, be closely supervised, as in some cases it can produce
neurological troubles (vertigo, sleeplessness, agitation, anxiety and delirium) (Cros-
nier et al.,1948; Tanguy et al.,1948; Alain et al., 1949; Siguier et al., 1949). For this
reason the administration of conessine in cases of dysentery has been discontinued
and the substance is now limited to the external treatment of Trichomonas vaginalis
and urethritis (Godet, 1950).
Phyllanthus niruri L. EUPHORBIACEAE

Used locally for dysentery and intestinal spasms in Ghana. Sometimes used as
a bitter stomachic and for constipation, the leaves of the plant are also chewed
to cure hiccups. An infusion is sometimes used for genito-urinary disorders (Dalziel,
1937).
In the aerial parts, three crystalline lignans including phyllanthine, hypophyllan-
thine and quercitin have been found (Krishnamurti and Seshadri, 1946). Five
flavonoids have been identified: quercitin, astralgin, quercitrin, isoquercitrin and
rutin (Nara et al., 1977). Four leucodelphinidine alkaloids were separated from the
leaves and stems, one of them being an enanthiomorph of securinine (Stanislas et al.,
1967; Rouffiac and Parello, 1969).
Extracts of P. niruri (by 50% ethanol) have extensive antibacterial, antifungal and
antiviral action. They also act on Entamoeba histolytica (protozoa) but not on the
malaria parasite Plasmodium berghei, and they are anthelmintic to Hymenolepsis
nana. The extracts have depressive action on the isolated guinea pig ileum and have
an anticancer action on Friend leukaemia virus (Dhar et al., 1968). Aqueous extracts
of the leaves have been found to have an oral hypoglycaemic effect comparable to
that of tolbutamide (Ramakrishnan, 1969).
The maximum dose of an extract of the whole plant tolerated by the mouse is
1 g/kg, given orally (Dhar et al., 1968).
164
Pseudocedrela kotschyi (Schweinf.) Harms syn. {Cedrela kotschyi Schweinf.,

P. chevalieri DC.) MELIACEAE
Dry zone cedar
The rootbark is used in Nigeria and Togo as a febrifuge and also in the treatment of
dysentery and rheumatism (Dalziel, 1937).
The bark contains 1% of a bitter non-nitrogenous principle, pseudocedrelin, which
is related to calicedrin. Pseudocedrelin is an unsaturated phenolic lactone with OH
and OCH 3 groups. In the wood oil, Ekong and Olagbeni (1967), Ekong et al. (1968,
1969b) and Taylor (1979) found meliacins (limonoids), including 7-desacetoxy-7-
oxogedunin and the pseudrelones A, B and C. Each of these consists of a single
limonoid alcohol which is esterified with various acids. In the bark 8.5% of mineral
substances, 14.6% of tannins, a saponin and 1% of lipids were also reported.
Pseudocedrelin in a dilution of 1/10000 kills paramecia in 20 min and the bark (3 g/1)
is toxic to goldfish inducing death after 1 h, whilst greater dilutions have a stupefying
action. In guinea pigs with experimentally induced hyperthermia, 0.05 g/kg
pseudocedrelin given subcutaneously or intraperitoneally produces a lowering of the
temperature of 2-3°C compared with control animals.
Carapa procera DC. syn. ( C guineensis Sweet ex Juss., C. touloucouna Guill. et

Perr., C. gummiflua D C , C. velutina D C , C. microcarpa Chev.) MELIACEAE
Crab wood, Monkey cola
The bark exudes a gum resin, is bitter, and is said to have antipyretic and tonic
properties. It is used in Nigeria in the treatment of fevers and as a general tonic. It is
also given to women during pregnancy. In addition, it is a component of native
cough mixtures and anthelmintic remedies, and is applied externally as a dressing
for sores. In the Congo area, the bark, cut up and mixed with palm wine, is used as
a quinine substitute.
From the plant collected in the Casamance, a bitter principle named tulukinin,
which is closely related to calicedrin, was isolated together with 19.5% mineral
compounds and 12% tannins. This bitter principle was also found in the seed oil
(Moyse-Mignon, 1942). Later, Bevan et al. (1963) obtained from the Nigerian plants
a crystalline substance analogous to the triterpenoid of the limonin group obtained
from Cedrela odorata. It was called carapin and its structure was identified as a
bicyclononalid (Bevan *tftf/., 1963, 1965).
The toxicity of the rootbark extract in mice was found to be 1.28 g/kg. It appeared
to be inactive as an antimalarial agent (Popp et al., 1968).
Trichilia roka (Forsk.) Chiov. syn. (T. emetica Vahl, Eleaja roka Forsk.)
MELIACEAE
Roka tree
An extract or decoction of the root is used in West African local medicine as a purge
and emetic, and the pounded bark and seeds are applied in the form of an ointment
in parasitic skin diseases (ringworm, etc.). In Senegal, T. roka has also been reported
to be used in skin diseases and to act as a tonic, to stimulate bronchial secretion and
165
to have an antiepileptic effect, whilst the related T. prieuriana A. Juss. is considered

in Senegal to have antipyretic, purgative and anti-arthritic actions (Kerharo and
Adam, 1974). Also in India Trichilia spp. are used for skin diseases (Chopra et al.,
1956).
In the rootbark of T. roka, a bitter principle related to calicedrin has been found
(Paris and Moyse-Mignon, 1939) as well as resin and a tannin. In the Nigerian
species of T. prieuriana, a meliacine called prieurianine was isolated by Bevan et al.
(1965). The seeds of Trichilia spp. yield 49-60% of fat which is used in candle-
making. It consists of palmitic, linoleic and oleic acids (Watt and Breyer-
Brandwijk, 1962). The analysis of the bark of T. heudelotti has revealed
an orange bitter principle, sterols and 10.2% of pyrocatechuic acid (Planche,
1949).
The seeds are purgative and emetic and the toxicity of the seed-cake for cattle has
been repeatedly reported (Watt and Breyer-Brandwijk, 1962).
Crossopteryx febrifuga (Afzel. ex Don) Benth. syn. (Rondeletia febrifuga Afzel. ex

Don, C. kotchyana Fenzl, R. africans Winterb.) RUBIACEAE
In local medicine the roots and bark are used in the treatment of fever, and a
decoction of the roots is used in the treatment of coughs and gastrointestinal
complaints (Dalziel, 1937). In Zambia the extracts have been used in trials by ordeal
(Marwick, 1963).
A glycoside and an alkaloid have been isolated from the bark. The glycoside has been
identified as /3-quinovin and the alkaloid has been called crossoptine (Blaise, 1932).
Raymond-Hamet (1940) considered that the characteristics of the alkaloid described
by Blaise are those of mitrinermine, later identified with rhynchophylline. The
presence of an alkaloid in the Nigerian species has been confirmed by Persinos et al.
(1964). A phytosterol and a phlobaphene have also been found in the bark
(Caiment-Leblond, 1957).
The alkaloid isolated by Blaise shows no toxicity upon ingestion in the dog at doses
up to 14 mg/kg; it has a slight hypotensive effect and produces vasoconstriction in
the kidneys. It does not appear to modify the hypertensive action of adrenaline and
seems pharmacodynamically different from quinine and yohimbine (Blaise, 1932).
A survey for supposed antimalarial activity gave negative results (Spencer et al.,
1947b).
Paullinia pinnata L. (Fig. 4.8) SAPINDACEAE

A flavotannin extracted from the leaves of this plant also has a cardiotonic effect (see
Chapter 2, CV).
The rootbark of P . pinnata collected in Brazil is said to contain a bitter principle,
timboin, and an oily substance, timbol, which act as a violent nerve poison
producing paralysis preceded by convulsions (Watt and Breyer-Brandwijk,
1962). An alkaloid, ichthyonine, a resin and a pigment have also been reported,
but the botanical identity of the plant appears uncertain (Kerharo et al., 1960,
1961, 1962).
166
P A saponoside with a triterpenic aglycone, present in the leaves and twigs of the plant
in West Africa, could account for its toxicity (Boiteau et al., 1964) (the plant had
caused a number of deaths when it had been used as an abortifacient). Kerharo et al.
(1960,1961,1962) think that the saponin is probably also the responsible constituent
for the toxicity of Paullinia towards protozoa (Paramecia were killed in 1 h by a
concentration of 1:500).
For a more comprehensive list of plants with antiprotozoal action, see Table 4.4.
Fig. 4.8. Paullinia pinnata L.

Table 4.4. Antiprotozoal plants
Plant Part used Active constituents) Acts on/action References

Acacia nilotica Leaves Tryptamine, tetrahydroharmane Entamoeba hystolytica Bhakuni«a/.(1969)
Albizialebbeck Pods Saponins (genins are triterpenoids, Antiprotozoal Dhar«a/.(1968)
echinocystic acid, etc.) Kaleyra(1975)
TripathiandDasgupta(1974)
Bouquet(1972)
A Ichomea cordifolia Root Alchornine (alkaloid) Antiprotozoal N
Ferreiraeta/. (1963a)
Hartetal. (1970)
Ogunlana and Ramstad (1975)
Alstonia boonei Bark Echitamine, plumeried? Filariasis (Calabar swellings) N
Argemone mexicana Leaves, stems Berberine Leishmania tropica, Trypanosoma CV
lezvisi and antibacterial Lambin and Bernard (1953)
Bixaorellana Seed-coat Wax-like substance Paralyses intestinal parasites Freise(1935)
Brucea anlidysenterica, Bruceolides (bruceantin, Plasmodium berghi, also NgoVanThueta/. (1979)
B.guineensis bruceantinol, dehydrobruceins) antifungal Phillipson and Darwish (1981)
Carica papaya Leaves Carpaine (alkaloid) Strongly amoebicidal, also CV
inhibits Mycob. tuberculosis Webb (1948b)
Burdick(1971)
Chasmanthera dependens Root Berberine Leishmania tropica, trypanocidal Das Gupta and Dikshit (1929)
Chopra etal. (1932)
Henry (1949, p. 345)
Mitschereta/. (1972a)
Cinchona spp. Bark Quinine Plasmodium, anti-amoebic CV
Kaustiva(1958)
Euphorbia hirta Plant Euphorbon (triterpene) Anti-amoebic Kerharo and Bouquet (1950)
Debaille and Petard (1953)
Martin etal. (1964)
Ridet and Chartol (1964)
Khaya senegalensis Bark Meliacin Paramecia (Balanlidium coli) N
Malcolm and Sofowora (1969)
Mitragyna inermis, Rootbark Rhynchophylline Antiprotozoal CV
M. stipubsa
Newbouldia laevis Bark Harmane derivatives, harmine, Protozoicidal and anthelmintic N
harmol Ferreiraera/. (1963b)
Ross«a/.(1980)
AlShammaera/. (1981)
Nymphea lotus Rhizomes Nymphaeine Mycob. tuberculosis, Mycob. Su«a/. (1973,1975)
smegmatis
Paullinia pinnata Bark leaves Triterpenic saponins Paramecia (in vitro) N
Kerharo«a/. (1960,1962)
Delaveaueta/. (1979)
Pauridiantha lyalli (not in Bark Harmane derivatives, harmine, Antiprotozoal N
West Africa) harmol Pousset«<z/. (1974)
Leveque«ra/.(1975)
Ross et al. (1980)
Phyllanthus niruri L. Plant Flavonoids Entamoeba histolytica, also Dhar«a/.(1968)
anthelmintic and antibacterial Naraeia/. (1977)
Tiliacorafunifera Leaves Funiferine Antimalarial N
Trichilia roka Rootbark Meliacins, catechuic tannins Antimalarial N
Ogunlana and Ramstad (1975)
Delaveaueta/. (1979)
Urginea indica Bulb Scillarenin Antiprotozoal, inhibits rhinovirus CV
Dhar era/. (1968)
SatoandMuro(1974)
169
(e) Antimetazoal plants (anthelmintics)

Some anthelmintics act by paralysing worms (such as tapeworm), which
then may have to be expelled by a purge. However, some drugs are also purgative
themselves. Other anthelmintics can destroy the parasite through lysis, for example
those containing proteolytic enzymes like bromelain from Ananas comosus, calotro-
pain from Calotropis procera and papain from Carica papaya can digest worms. In
other cases drugs (like antimony in the case of trematodes) act through inhibition of
phospho-fructokinase, thus reducing the energy required by the worms to maintain
their attachment to the walls of the mesenteric vessels and forcing them to emigrate
into intra-hepatic portal veins, where they are destroyed by phagocytosis. Certain
filaricides also cause the filaria embryos to emigrate to the liver, where they are
subject to lysis by the cells of the reticulo-histiocytal system (Lechat et al., 1978).
Active constituents
Many constituents with antibacterial activity are also anthelmintic. Apart
from the vermicidal action already mentioned under antibacterial constituents,
plumbagin (naphthoquinone) also appears to be active against cestodes; thus,
Diospyros mollis also acts on Hymenolepis nana. Other plants containing gallic acid
and ethylgallate such as Acacia arabica, A. farnesiana and A. nilotica also act on
cestodes. This applies also to Combretum racemosum and another Combretaceae,
Anogeissus leiocarpus, which contain gallic acid and tannins.
Alkaloids are often the active agents. Echitamine from Alstonia boonei acts against
loa loa filariasis (Calabar swellings). The anthelmintic action of Spigelia anthelmia is
attributed to spigeline, that of Andira inermis to berberine and/or andirine, that of
Punica granatum to pelletierine tannate (acts on cestodes), that of Quisqualis indica to
an alkaloid contained in the seeds and that of Hunteria umbellata to hunteramine or
related alkaloids.
Flavonoids found in Citrus acida and Albizia lebbeck have antinematodal proper-
ties. In Bixa orellana the wax-like substances from the seed coat have been said to
paralyse intestinal parasites.
Terpenoids. Many plants contain glucosides with terpenoids or resins as a genin
and for many of these plants the action may be due to the genin. Amongst them we
find some well-known anthelmintic plants such as Chenopodium ambrosioides*
(ascaridole, monocyclic terpene) and Cucurbita maxima* and C. pepo* (fruits),
which have glucosides of tetracyclic triterpenes (cucurbitacines). These and
ascaridole also force cestodes to emigrate but do not destroy them and their
administration must therefore be followed up by a purge. Triterpenes are also found
in Melia azedarach roots (act on cestodes and ascarides) and Santalum album
(santalenes, tricyclic sesquiterpenes) both plants also being insecticides. Tetracyclic
sesquiterpenes are reported in Euphorbia resins (euphol and euphorbol). Pentacyclic
triterpenes derive from a- and /3-amyrine, and oleanolic acid has been found as a
constituent of the stembark oiOpilia celtidifolia*, which stimulates the activity of
Taenia pisiformis. Several anthelmintics owe their action to resins or glucoside
resin-compounds. Albizia lebbeck, Embelia schimperi*, Mallotus philippinensis and
Phytolacca dodecandra have been mentioned as such.
170
Mustard-oil heterosides. Plants with antibiotic properties that contain mustard-oil

heterosides, such as Allium spp., Cleome gynandra and Ritchiea longipedicilata,* are
also anthelmintic, and an active benzylisothiocyanate derivative (pterygospermine)
is present in Moringa oleifera as well as triterpenoids.
The plants containing proteolytic enzymes have been mentioned above and under
Antibacterial plants. In Harrisonia abyssinica*, warburganal is considered to be the
active agent.
Chenopodium ambrosioides L. CHENOPODIACEAE

American or Indian wormseed, sweet pigweed
Cultivated and naturalized as a domestic anthelmintic. The pounded leaves are also
applied to sores (Dalziel, 1937).
The fresh aerial parts, harvested when the plant is flowering, yield 0.2-0.5% of an
essential oil from the leaves, 0.5-1% of the oil from the flowering tops and over 1%
from the fruits. The oil contains 20-30% of terpenoids (p-cymene, limonene,
terpene) and 60-80% of ascaridol (peroxide of a terpenoid), which is mainly
abundant in the fruit (Paris and Moyse, 1967, p. 131).
Ascaridol is toxic to cold-blooded animals. It kills and paralyses Ascaris and
hookworms (Ankylostoma) and to a lesser extent oxyurides and cestodes. Its
administration must be followed by a saline or oily purge. In Man it may induce
vertigo, vomiting and headaches, and is more often used in veterinary medicine
(Paris and Moyse, 1967, p. 132; Kerharo and Adam, 1974).
Cucurbita maxima Duchesne Cucurbita pepo L. CUCURBITACEAE

Pumpkin, squash gourd
The fruit (pulp) and leafy shoots of these plants are eaten as a vegetable and in soup
whilst the gourds are used as domestic utensils. The seed kernels of both species are
used in India and in some parts of Europe as an anthelmintic for tapeworm and as a
diuretic, and the scraped pulp is applied as a poultice to burns, boils and swellings
or even as a cooling application for headache or neuralgia (Dalziel, 1937).
The pulp of the fruit of both species has been found to contain highly nutritive
proteins, carbohydrates and minerals and also contains an amino acid, cucurbitine
(amino-3-carboxy-3-pyrrolidine), believed to be responsible for the anthelmintic
effect (Schabort, 1978). The seed oil of C. maxima is composed of 20.5% palmitic,
28% oleic, 8.5% stearic and 43% linoleic acids (Tewari and Srivasta, 1968) and that
of C. pepo contains the same fatty acids but in slightly different proportions. In some
bitter varieties of C. pepo (var. ovifera) the cucurbitacines B, D, E and I (toxic
tetracyclic terpenes) have been found. Some of these which act as purgatives are also
present in other Cucurbitaceae, particularly cucurbitacine E.
The aqueous, ethereal and alcoholic extracts of the seeds of both plants have been
found to have anthelmintic properties in vitro and in vivo. In vitro they significantly
affect trematodes (Fasciolopsis buski) but they seem to be virtually inactive on
nematodes and on Ascaris lumbricoides (Srivasta and Singh, 1967) and they are also
inactive on cestodes (Rallietina casticillus in fowl) (Lahon et aL, 1978). The extracts
171
have some cardiotonic action. The active principle is believed to be cucurbitine,

which paralyses earthworms (Lumbricoides terrestris) within 117 min after application
of a 2.9 x 10~ 3 M solution. This is an effect comparable to that of piperazine, a
standard anthelmintic drug (Bailenger and Sequin, 1966). Gonzalez et al. (1974)
noted that cucurbitine had a contractile action on the isolated rabbit intestine, which
was counteracted by atropine but not by papaverine. Similarly cucurbitine paralyses
Taenia spp. but its administration must be followed after 4-5 h by a saline purge to
expel the parasite. Oral administration of a preparation of a stable, concentrated and
deproteinized extract of the fresh seeds of C. maxima was, according to Junod
(1964), not only well tolerated but in 80 patients with Taenia saginata produced
84.6% success. When the extract was given by duodenal or gastric tube, the
treatment was successful in all of 54 cases (Gonzalez et al., 1974; Bizyulyavichyus,
1969). The seeds of C. pepo are also reported to be an excellent anthelmintic
especially against Taenia and Botriocephalus; in adults, doses of 50-60 g of fresh
seeds are non-poisonous. Two fractions (not only cucurbitine) are thought by
Bailenger and Sequin (1966) to be responsible.
Furthermore, it has been noted that the crude aqueous extract of the ripe fruit of
C. pepo inhibited in vitro virulent strains of Mycobacterium tuberculosis in 1:10000
dilution and retarded over 50% at a 1:100000 dilution. This efficiency was
confirmed in vivo in mice. Peposin (obtained from the acetone extract) inhibited the
growth of Mycob. tuberculosis in a dilution of 1:50000 for a period of 3 weeks
(Gangadharan and Sirsi, 1955).
Opilia celtidifolia (Guill. ex Perr.) End. ex Walp. syn. (Groutia celtidifolia (Guill. &
Perr.) Endl. ex Walp., O. amentaceae of Chev.; of Aubrev.) OPILIACEAE
An extract of the bark of Opilia is used as an anthelmintic while its leaves are used in
the treatment of sleeping sickness and as a diuretic.
A methanol extract of the stembark yielded four saponins, the sugar moiety of all of
these being arabinose and mannose. The aglycones of two of them have been
identified as aleonalic acid whilst the aglycone of a third was found to be hederagin
(Haerdi, 1964; Bouquet, 1972; Shihata <?r a/., 1977).
Pharmacological studies by Shihata et al. (1977) revealed that intravenous injection
of the saponin fraction of the stembark into anaesthetized dogs in doses of 20 mg/kg
caused an increase in respiratory rate and a fall in blood pressure, which started to
increase slightly after 30 min but did not return to its normal level. There was no
effect on the renal circulation. The non-pregnant rat uterus was stimulated by doses
of 40-100 mg/50 ml bath whilst the pregnant uterus did not respond. Doses higher
than 10 mg inhibited intestinal motility but did not affect the intestinal response to
acetylcholine. On the isolated rabbit heart 5-25 mg produced severe reduction in
coronary outflow.
A study on the anthelmintic action of the saponins on intestinal worms isolated
from dogs has shown slight stimulation of motility in Toxocara leonani by high doses
(100-150 mg/50 ml bath). Taenia pisiformis was more easily affected: 50-150 mg/50
ml produced distinct stimulation of motility (Shihata et al., 1977).
172
Embelia schimperi Vatke syn. (E. abyssinica Bak.) MYRSINACEAE

In Uganda the leaf is used as a foodstuff; in different parts of Africa the berries are
used as an anthelmintic against Taenia (an overdose is said to be often fatal). Related
Indian species like E. ribes are also anthelmintic and mainly used against
ascarides.
The berries of the African species contain 6-7.5% embelin (2.5-dihydroxy-3-
undecylbenzoquinone) whilst those of the Indian species contain 2.5-3% of
embelin. In addition, quercitol, fatty ingredients and an alkaloid, christembine,
are reported to be present (Chopra et al., 1956; Kapoor et al., 1975). The African
Embelia is said to contain a toxalbumin (Watt and Breyer-Brandwijk, 1962,
p. 786).
In Africa embelin has been used in doses of 0.2-0.4 g as a taeniacide. In India
embelin is said to have no effect on Taenia and hookworm but to be very effective
in the treatment of ascarid infections. Clinical studies on 40 children infected by
ascarides have shown a positive effect in 80% of the cases using an alcoholic and
aqueous percolation of the berries whilst an aqueous extract cured 55% in both
cases, eliminating ova from patients' stools. The worms were also expelled from
the stools and no purging was required. No evidence of toxicity was noted during
or after the treatment (Guru and Mishra, 1966). Perhaps the same results might
be obtained in Africa if the toxalbumin could be eliminated. Aqueous extracts of
the berries have proved to be antibacterial against Staphylococcus aureus and
Escherichia coli in India (Chopra et al., 1956) and have also been found to reduce
fertility (Arora et al., 1971). Gupta et al. (1976) have reported that the anthelmin-
tic properties of embelin were greatly improved by using analogues obtained by
chemical substitution such as isobutyl-embelin or w-hexylaminoembelin whilst
di-imines were inactive. In concentrations of 1-3 x 10~3 the analogues were active
(contact period 30 min) on the parasites tested: Paramphistomum cervi, Trichuris
ovis, Oesophagostomum columbianum, Dipylidium caninum (flukes, roundworms and
tapeworms).
Ritchiea longipedicillata Gilg CAPPARIDACEAE

In Nigeria, an extract of R. reflexa is used to treat guinea worm infection, the roots
being used to treat earache (Dalziel, 1937). The leaves of the related R. cap-
paroides (Andr.) Britten are reputed in Senegal to be antivenomous and antifilarial,
and the roots plus leaves are used externally in the treatment of snake bites and of
guinea worms infection. Roots and twigs are used as a plaster on the cervical (en-
larged lymph nodes) 'ganglia' of patients suffering from Gambiense trypanosomiasis
(Kerharo and Adam, 1974, p. 323).
Cleomin has been isolated from the rootbark and identified as S(-)-ethyl-5-
methyl-2-oxazolidine-thione, which is obtained by enzymatic hydrolysis of glucoc-
leomin, a mustard-oil glycoside; it has also been found in Gynandropsis gynandra
173
(L.) Briq. (Misra and Sikhibhushan Dutt, 1937; Ahmed et al., 1972; Oguakwa et
al.9 1981).
Mustard oils, including the oils of Allium spp., and senevols are reputed to have
antiseptic, rubefacient and anthelmintic properties; this seems to justify the local
uses of the plant.
Harrisonia abyssinica Oliv. syn. (H. occidentalis Engl.) SIMAROUBACEAE

In Ghana the rootbark is boiled and drunk with palm wine as a laxative (Irvine,
1930). Watt and Breyer-Brandwijk (1962) report that the Teita and Jaluo tribes use
the root as a remedy for bubonic plague, and the Sukuma administer it as an
anthelmintic against oxyures and ascarides. The Nyamwezi swallow the smoke from
the burning rootbark for ancylostomiasis until 'the smoke passes through the
intestine'. The leaf is applied to abscesses and carbuncles.
From Harrisonia (root?) cantine-6-one, harrisonin, obacunin, obacunoic acid,
warburganal and muzigadial have been isolated (Mitscher etal., 1972b; Kubo etaL,
1976, 1977).
Githens (1949) has reported the action of Harrisonia roots against roundworm. In
experimental malaria the roots proved ineffective (Spencer et al., 1947a). Warbur-
ganal is a potent antifungal, antiyeast agent and a potent antifeeding agent against
army worms {Spodoptera littoralis and S. exempta) (Kubo et al., 1977; Vigneron,
1978), thus confirming local anthelmintic uses. Ether extracts of the root are
reported to have an antimicrobial effect against Neisseria gonorrhoea and Trichophyton
mentagrophytes (Uiso, 1979).
For a more comprehensive list of plants with antimetazoal action see Table 4.5.
174 175
Table 4.5. Antimetazoalplants

Acacia famesiana Aerial parts Ethylgallate, gallic acid Taenia, also antibacterial Littler al. (1953)
Hussain«a/.(1979)
Acacia nilotica Juice Ethylgallate, flavonoids Taenia Camp and Norrel (1966)
Attia«a/.(1972)
Albizia lebbeck Bark Saponin Ascaris lumbricoides in vitro Sannie«a/. (1963)
Kaleyra(1975)
Alpinia galanga and spp. Rhizome Flavonoid Ascaris lumbricoides in vitro Mitsuietal. (1976)
Ray and Majumdar (1976)
Andira inermis Rootbark n-Methyltyrosine, berberine Anthelmintic (also insecticide) N
Heal and Rogers (1950)
Anogeissus leiocarpus Root-and 17% tannins Taenia (veterinary) N
stembark Dalziel(1937)
Carica papaya Seeds, latex Carpasemin (benzylthiourea), Anthelmintic and amoebicidal CV
proteolytic enzyme, papain Krishnakumari and Majumdar
(ascaridol) digests worms (1960)
Shukla and Krishnamurti
(1961b)
Dar«a/.(1965)
Carissaedulis Twigs Quebrachytol, cardio-glycosides Taenifuge, anthelmintic and Hager's Handbuch (1967-80,
antiparasitic Vol.3,p.716)
Bhaduri«a/.(1968)
Citrus acida, C, medica Rind Hesperidin (flavonoid) A. lumbricoides in vitro CV
Kaleyra(1975)
Diospyros spp. Fruit Plumbagin Hymenolepis nana, also insecticidal CV
Sen«a/.(1974)
Farnsworth and Cordell (1976)
Khan el al. (1980a)
Gynandropsis gynandra Leaves Glucocapparine (methyl senevol Anthelmintic Ahmed etal. (1972)
(Cleome gynandra) glucoside) Misra and Sikhibushan Dutt
(1937)
K jaer and Thomson (1963)
Hunteria umbellata syn. Bark Alcoholic extract of bark Paralyses and kills Ascaris, also Onuaguluchi(1964,1966)
(Polyadoa umbellata) smooth muscle depressant
(Erin tree)
Mallotus oppositfolius var. Leaves Rottlerin Locally used to expel tapeworms Dalziel(1937)
pubescens Oliver (1960)
Mallotus philippinensis c. Hairs from Rottlerin, 'kamala' Taenifuge in Indian Pharma- Chopras al. (1956)
('Kamala'cultivated in fruit copoeia and British Veterinary
French-speaking West Codex
Africa)
Morinda geminata Rootbark Morindin = methylanthraquinone A. lumbricoides CV
glycoside Nguyen BaTuoc(1953)
Adesogan(1973)
Punica granatum c. Bark Pelletierin and isopelletierin, Taenia, Ascaris (toxic), British Pharmacopoeia (1948)
tannates, friedelin Ankylostoma
Quisqualis indica (Fig. 4.9) Fruit Sesquiterpene (santonin-like), Cestodes, trematodes, thread- and Guerreros al. (1924)
quisqualicacid hookworm Henry(1949,p.782)
Xaio(1983)
Secundaca longepedunculata Roots Saponosides MoUuscicidal, intestinal parasites, CV
Tinea cruris (fungus) Fraga de Azevedo and de
Medeiros(1963)
Gaudin and Vacherat (1938)
Qdebiji(1978)
Prista and Correia Alves (1958)
Spigelia anthelmia Roots, leaves Spigeline, spigeleine (alkaloids) Anthelmintic (toxic!), high doses British Pharmaceutical Codex
(fresh) cause spasms of eye and face (1923)
muscles and even convulsions US National Dispensary (1926)
176
II Plants with insecticidal or molluscicidal activity

In tropical climates especially, a number of infective diseases are conveyed
by insects or molluscs, and the need for prophylactic action has already been
mentioned in the discussion on protozoal and viral diseases. Some nematode
infections are also transmitted by animal vectors; thus river blindness (onchocer-
ciasis) is transmitted by the buffalo gnat, Simulium damnosum, and in filariasis caused
by Manzonella ozzardi transmission is done by the midge Culicoides furens (Manson-
Bahr, 1952). Insofar as the combating of these animal vectors can be based on the use
of plants, they will be dealt with here.
(a) Insecticidal plants

Plant-insect relationships are numerous and often contradictory. Plants
can provide a home and food for insects, and can live in partial symbiosis with some
insects, for instance ants. Thus in Nigeria the spindle-shaped swellings of the
branchlets ofBarteria nigritiana Hook. (Passifloraceae) are occupied by stinging ants
which defend the plant against larvae, caterpillars, beetles, and in fact, as I have
found out to my considerable discomfort, against any living creature approaching
the plant. Many plants attract insects, through bright colour and the smell of the
flowers, to ensure pollination (Fraenkel, 1959). On the other hand, plants can also
trap and 'digest' insects. An example is the insectivorous Drosera.
In insects, basic food requirements seem to be very similar and yet most insects
feed preferentially only on a few closely related plant species. Fraenkel (1959)
assumes that plant substances which are of secondary importance to the metabolism
of the plants, such as glycosides, saponins, tannins, alkaloids and essential oils, may
repel most insects or other animals but attract those few that feed on the particular
plant species, which may have its particular smell or taste. Tests have shown that
isolated active substances (glyco-alkaloids, mustard-oil glycosides, essential oils)
even induced feeding when incorporated into neutral media (filter paper or agar
jelly) or when applied to leaves commonly not accepted by the insects. Euw and
Reichstein (1968) isolated 0.1 mg of aristolochic acid from swallowtail butterflies
(the larvae of which feed exclusively on plants of the Aristolochia family). This acid
protects the butterflies against vertebrate predators (Oliver-Bever, 1970). Like most
insects, mites and microorganisms (bacteria and fungi) appear to be affected by the
secondary plant products, and a number of plants have constituents with insecticidal
action.
Most of the constituents of insecticidal plants are highly toxic for several
cold-blooded animals and often their toxic properties are tested in fish. They are
virtually non-poisonous to mammals (including Man) when given orally, but when
intravenously injected some can produce respiratory paralysis and death by asphyxia
(Heftmann, 1975).
A number of Fabaceae are insecticidal. The best known, which are widely used
commercially, belong to the genera Denis and Lonchocarpus, and contain 3-20% of
rotenone. Unfortunately, the West African species of Denis* and Lonchocarpus*
177
appear to have less active components than the American or Indian species, but some
other Fabaceae, such as Entada africana*, Mundulea sericea* and Tephrosia vogelii*,
which are found in West Africa, are very efficient.
All these insecticidal Fabaceae have roughly the same chemical constituents and
their efficiency is often measured in relation to the amount of rotenone present.
Rotenone has an isoflavone nucleus combined with a furan and pyran ring. It is said
to belong to the isoflavones (Paris and Moyse, 1967, p. 387), or to the phenyl-
propanoid flavonoids (Towers and Wat, 1979). Substances chemically related to
rotenone, also found in these Fabaceae, are called rotenoids. Thus, degueline is an
isomer with a 2-dehydrobenzopyran nucleus; tephrosine or toxicarol have phenolic
hydroxyl groups. Derric acid constitutes the common half of the molecule of
rotenone and these rotenoids. The oral lethal toxicity of rotenone is low for
mammals: 3 g for the rabbit, 0.6 g for the rat and 0.06 g for the guinea pig. In insects
and fish it acts on ingestion or contract and is a potent inhibitor of mitochondrial
oxidation (Towers and Wat, 1979); it is active in dilutions down to 1:20000000. At
this concentration it can kill goldfish in 2.5 h. As a stomach poison in silkworms,
rotenone is 30 times as toxic as lead arsenate. It is 15 times as toxic as nicotine when
used as a contact insecticide against bean aphis and is 25 times as toxic as potassium
cyanide to goldish (Watt and Breyer-Brandwijk, 1962).
Saponosides have been reported to be present in other Leguminosae with insectic-
idal properties, such as Dichrostachys glomerata (also molluscicidal against Bulinus
globulus), Pentaclethra macrophylla and Tetrapleura tetraptera.
Triterpenoids seem to be responsible for the insecticidal activity of Melia
azedarach*, Annona spp*. and Santalum album*. The insecticidal action of Sesamum
indicum has been attributed to a lignan (sesamin) and that of Duranta repens
cultivated in West Africa, to an alkaloid. Vernonia pauciflora, with sesquiterpenic
lactones (vernolide and hydroxyvernolide), is considered useful for killing termites.
Larvicidal properties have been found in Thevetia neriifolia (aucubine, flavonic
heteroside), Uvaria chamae (chamaenetin, benzylflavanone) and Spilanthus uliginosa
(spilanthol). The leaves of Melia azedarach are insect repelling through their
meliacins and a repellant action is found in many essential oils. The oils of Ocimum
basilicum and O. canum are reputed to repel ants and moths. (For details on
U. chamae, O. basilicum and O. canum see Antibacterial plants).
Derris microphylla Miq. Jacq. FABACEAE
Derris spp. have been introduced in certain parts of West Africa (Congo, the Ivory
Coast and Nigeria). They were originally used in China and India and were
introduced into the USA and Europe towards 1930 (Paris and Moyse, 1967, Vol. II,
p. 388). Commercial Derris is mainly obtained from Southern Asia (D. elliptica
Benth. and D. malaccensis Prain). The roots of these contain 4-20% of rotenone.
Seasonal variations of the rotenone content have been reported (Nandy and Gupta,
1968). Rotenone is colourless and odourless, and thousands of tons of rotenoids are
used against agricultural parasites and to relieve domestic animals of insects. In its
commercial formulation, rotenone is often associated with pyrethrins (from certain
178
plants of the genus Chrysanthemum, referred to as Pyrethrum, not present in West

Africa), which act more rapidly but are less stable and more expensive to produce
(Paris and Moyse, 1967, Vol. II, p. 389). Prenylated flavonoids (derricin, derridin,
lonchocarpin, etc.) are almost ubiquitous in Denis and Lonchocarpus spp, and may
be considered as biogenetic precursors of the rotenoids (Delia Monache etal., 1978).
Lonchocarpus sericeus Poir. H.B, & K. syn. (Robinia sericea Poir.) FAB ACE AE
The bark is employed as a stomachic and laxative and in Nigeria for convulsions and
backache. It is applied locally for parasitic skin conditions and eruptions. In America
this species has been listed, together with other Lonchocarpus spp. as an insecticide
(Dalziel, 1937).
From the roots, seeds and leaves of this tree, lonchocarpine has been isolated in the
Congo (Castagne, 1938). It was identified as a 5-hydroxy-2,2-dimethyl-3-chromen-
6-yl-strylycetone. From the leaves, sterols (including /3-sitosterol), prenylated
flavonoid precursors, p-coumaric acid, quercitin, rutin and hyperosid have been
isolated (Kerharo and Adam, 1974; Delia Monache et al., 1978). The main
commercial sources for rotenone are the American L. nicou DC. andL. urucu Phillips
& Smith, In the Nigerian L. laxiflorus Guill. & Perr., Pelter and Amenechi (1969)
reported an isoflavonoid and a pterocarpanoid.
Entada africana Guill. et Perr. syn. (E. ubaguiensis de Wild., E. sudanica Schweinf.,
Entadopsis sudanica (Schweinf.) Gilb. & Boutique) MIMOSACEAE
This tree has many local uses. It yields an inferior quality gum and the leaves are used
as cattle fodder. The bark of root and stem yields a long fibre used for cordage,
commonly for roof-binding, the tying of grass matting, etc. In Northern Nigeria and
Northern Ghana, an infusion of the leaves or of the bark is taken as a tonic and
stomachic. The leaves also constitute a good wound dressing, preventing suppur-
ation (Dalziel, 1937).
Rotenone has been reported to be present in the plant (Gaudin and Vacherat, 1938)
and saponosides have been found in the bark and leaves (Githens, 1949).
An infusion of the leaves at a concentration of 1:1000 kills Carassius auratus
(goldfish) in 12 h but was not toxic even in doses of 5 g/kg to the guinea pig (Gaudin
and Vacherat, 1938).
Mundulea sericea (Willd.) Chev. syn. (M. suberosa (DC.) Benth.) FABACEAE
The bark is known to be poisonous and both bark and seeds are used as a fish poison
in Nigeria, Ghana, India, Sri Lanka, Tanzania and Zimbabwe. It is said to kill and
not merely to stupefy. Both bark and roots have been suggested as an insecticide
(Dalziel, 1937).
Worsley (1936) has isolated rotenone, deguelin, tephrosin and some alkaloids and
glycosides from the bark. Chopra etal. (1941) confirmed the presence of rotenone.
Mundelone or mundulone of isoflavonoid structure has been isolated from the bark
as well as a rotenoid, munduserone, and a flavonoid, sericetin (Finch and Ollis,
179
1960). In addition, the flavanones lupinifolin, lupinofolin, mundulin, mundulinol

and a chalcone, sericone, have been reported by van Zyl et al. (1979). The plant is
also said to contain hydrocyanic acid (Watt and Breyer-Brandwijk, 1962).
In India the root, bark, leaves, stem and seeds are all said to be toxic and several
authors consider the plant to be an extremely efficient fish poison capable, even, of
killing small crocodiles (Chopra et al., 1941). According to Worsley (1937) it is
considerably more toxic to insects than Tephrosia vogelli Hook. The bark is said to
be equivalent in toxicity to the root of Denis elliptica, despite a lower percentage of
rotenone but the toxicity of plants grown under different conditions varies and the
smooth bark from the closed forest region is much more toxic than the rough corky
bark of the savannah areas. The leaves, root and bark have proved to be efficient
against Chrysanthemum aphids (Watt and Breyer-Brandwijk, 1962, p. 636).
Tephrosia vogelli Hook. FABACEAE

Fish poison bean
The shrub was formerly cultivated throughout West Africa, and used to stupefy fish
(this has been prohibited in Southern Nigeria). If the pounded leaf is thrown into a
creek the fish are temporarily paralysed and can be lifted out of the water. Most
commonly the leaves are used alone but in some districts people also use them with
the pods or use the pod only. A very dilute solution is sufficient to produce paralysis
and death in fish.
Two main constituents, deguelin and tephrosin (hydroxy deguelin) have been found
not only in the leaves but also in the roots, fruit capsules and seeds. The leaves also
contain a volatile oil, tephrosal, which is responsible for their pungent odour
(Hanriot, 1907; Castagne, 1938). Furthermore, rotenone, dehydroxydeguelin,
rutin and tetrahydroxy-3,6,7,4'-methoxy-5-flavone (which was called vogeletin)
have been reported to be present in T. vogelii (Vleggaar et al., 1978) and rotenoid
extraction from the leaves was carried out by Barnes and Freyre (1966a, b, 1967).
By simple contact, fish kept in a 2% dispersion of the leaves have died within 3 h and
those kept in a 1% dispersion in 12 h. On the other hand, guinea pigs ingested as
much as 5 g/kg without adverse effects. When injected intravenously, however, a
leaf extract corresponding to 0.01 g/kg of tephrosin has killed dogs in 5 min whilst
the injection of 0.01 g/kg of pure tephrosin produced death through respiratory
arrest only the day after, preceded by accelerated breathing and convulsive effects
alternating with paralysis (Hanriot, 1907). Concentrations of tephrosin as low as
1:50000000 paralyse fish and a delayed fatal effect may occur. The Tephrosia
rotenoids are also toxic to insects, batrachians, worms and snails. Although deguelin
is about half as efficient a piscicide as rotenone (it kills fish in a dilution of
1:20000000 at 27°C in 4.5 h whilst rotenone in the same circumstances kills fish in
2.5 h (Barnes and Freyre, 1966b, 1967)), in Tephrosia it is the leaves which contain
the active rotenoids rather than the roots as in Denis and Lonchocarpus spp. After 22
years of storage the dried leaves of Tephrosia were still able to kill goldfish and larvae
of worms (Watt and Breyer-Brandwijk, 1962).
180
Spilanthes uliginosa Sw. syn. (S. acmella Chev, S. oleraceae Jacq.) COMPOSITAE
Bresil cress, para cress
The flowerheads of S. uliginosa have a pungent taste and cause salivation. They are
chewed in Nigeria and the Cameroons to relieve toothache and are used in local
application as a haemostatic and analgesic (Dalziel, 1937). In India, they are also
used for sore throats and gums and in paralysis of the tongue (Chopra et al., 1956).
The flower tops of both species contain spilanthol, which is an unsaturated amide
and may be identical with affinine (from Erigeron affinis) (Af-isobutyldecatriene-
2,6,8-amide), a sterol and a non-reducing sugar (Paris and Moyse, 1971, p. 458).
Extracts of the plants have a depressant action on the guinea pig ileum and on the
blood pressure of cats and dogs. In mice the maximum dose tolerated intraperito-
neally is 100 mg/kg (Dhar et al., 1968). Spilanthol has been said to have local
anaesthetic action (Chopra etal., 1956). It also has a larvicidal action. Extracts of the
flowerheads in a soapy suspension and spilanthol kill Anopheles larvae in a dilution
of 1:100000 (Kerharo and Adam, 1974) and the whole plant has insecticidal
properties towards cockroaches and bedbugs (Heal and Rogers, 1950).
A 50% ethanol extract of the plant is reported to have antibacterial action against
Staphylococcus aureus, Salmonella typhi, Escherichia coli, Mycobacterium tuberculosis
and Agrobacterium tumefaciens. Antifungal activity was found against Candida
albicans, Trichophyton mentagrophytes and Aspergillus niger. Antiviral action was seen
in Raniket disease and against Vaccinia virus, and antiprotozoal action against
Entamoeba histolytica. Finally, the plant has an anthelmintic effect towards
Hymenolepis nana (Dhar et al., 1968).
Melia azedarach L. (Fig. 4.10) MELIACEAE

Persian lilac, bead tree
Cultivated in Nigeria, its bark has been used as an anthelmintic. In India, the
country of origin, the juice of the leaves is used internally as an anthelmintic,
antilithic, diuretic and emmenagogue (Chopra et al. ,1956). The seeds are prescribed
for rheumatism and the oil is considered to be similar in its properties to Neem oil.
Schulte et al. (1979) isolated triterpenoids, steroids and aromatic compounds
from the air-dried roots. These compounds are 24-methylene-cycloartanone,
cylco-eucalenone, 4-stigmastene-3-one-2,4-campestene-3-one, 4-methylene-cyclo-
artanol, triaconthanol, cycloeucanol, /3-sitosterol, /3-sitosterol-D-glucoside, vanillic
aldehyde, transcumanic aldehyde and vanillic acid (Kraus and Bokel, 1981).
In the fruit and heartwood they found the same cyclonastone derivatives as in the
roots, plus two additional substances: 21,23,24,25-diepoxy-tirucall-7-en-21-ol and
a protolimonoid (Nath, 1954; Schulte et al., 1979). An alkaloid paraisine
(ocaziridine) was found in the leaves. In the rootbark of the Nigerian species the
limonoids gedunin and 7-deacetoxy-7-oxogedunin, the nimbolins A and B (meliacin
cinnamates), melianins A and B, as well as the products of decomposition (fraxinel-
lose and azedainic acid) were reported, besides 24-methylene-cycloartanone, cyclo-
eucalenone and cycloeucalenol (El Said et al., 1968; Ekong et al., 1969b; Okogun et
181
al., 1975). In Israel, the protolimonoids melianon, melianol, melianodiol and

meliantiol as well as an apo-eupol derivative were found by La vie el al. (1967) and
Lavie and Levy (1969) in the roots and bark.
Aqueous extracts of the fruits have been found to produce dyspnoea, tremor,
convulsions and death in rabbits. In cats, dogs and sheep they produced paralysis
and narcosis (Murthy and Sirsi, 1957,1958). However, Ekong etal. (1968) found no
components toxic to mice from Indian M. azedarach. The LD 50 in mice was 1.04 g/kg
for ether and chloroform extracts and 1.5 g/kg for a triterpene mixture.
The insecticidal properties of the leaves, stems and bark have been clearly
demonstrated on crickets, cockroaches and Aedes aegypti (Heal and Rogers, 1950)
and make Melia a very superior insecticide. It has also been noted that plants sprayed
with triterpenoids of the fruit are not visited by insects (Henry, 1949, p. 781;
Bezanger-Beauquesne el al., 1981). The repellant substance found in Melia leaves
(3.5%) has been named meliatin. It is very similar in its properties to cail-cedrin
(Chauvin, 1946). Anthelmintic properties have also been reported for Melia by
Fig. 4.10. Melia azedarach L.
43^"^f
182
Chopra et al. (1938) and Cortex azedarach was included in the US Dispensary as an
anthelmintic against tapeworm and ascarides, and as an antiparasitic.
The bark is said to act as an antispasmodic and tonic. Some antimicrobial activity
of extracts of the leaves, bark and seeds has been reported by Nickel (1959), mainly
on Gram-negative bacteria. The extracts were inactive against Paramecia (Spencer et
al., 1947a). In anticancer tests the extracts were only slightly active against sarcoma
180 and adenosarcoma 755 (Abbot et al., 1966).
Annona muricata L. ANNONACEAE

Soursop
Annona reticulata L.
Custard apple
The leaves of these introduced spp. have been reported to have anthelmintic
activities in their country of origin (Nadkarni, 1954; Watt and Breyer-Brandwijk,
1962) and an aqueous solution of the seeds of A. reticulata kills most wood bugs
(Lecanium). Insecticidal activity has also been reported for the seeds, stems and roots
of A. muricata and A. reticulata (Steenis-Kruseman, 1953). A. muricata has a potent
insecticidal effect against Macrosiphonella sanbornia. Against Aphis ruminis the
toxicity of the roots of A. muricata is inferior to that of Dends elliptica (Heal and
Rogers, 1950; Kerharo and Adam, 1974). The insecticidal constituent of the leaves
and roots is resistant to heat, but not to saponification, and may be related to fatty
acids of high molecular weight (Hegnauer, 1962-68, Vol. Ill, p. 120). Both Annona
spp. contain hydrocyanic acid and A. reticulata contains 0.12% of anonaine.
Annona senegalensis Pers. ANNONACEAE

The people of Northern Nigeria use the leaves of this small tree, mixed with cereal
cakes, or in the form of a large bolus mixed with soda and bran, as an anthelmintic
for horses. The bark and root have been similarly used. The leaves are also applied
as a dressing mixed with the latex of Calotropis procera and of Euphorbia balasamifera
in the treatment of epizootic lymphaginitis in horses (Dalziel, 1937).
The leaves of A. senegalensis have been found to contain rutin, quercetin and
quercitrin (Mackie and Ghatge, 1958) and in the stembark, positive reactions for
alkaloids, saponins and tannins have been obtained (Persinos and Quimby, 1967).
The leaf contains a hard and a soft wax, both of which contain higher saturated fatty
acids. From the hard wax, primary alcohols and palmitone (hentriacontanone), and
from the soft wax a yellow sesquiterpenic oil has been obtained (Mackie and Misra,
1956).
The soft leaf wax has proved to be effective against Sclerostoma larvae from horse
faeces; this action has been attributed to the sesquiterpenes. The twigs of
A. senegalensis produced 100% mortality of Oncopeltus fasciatus in concentrations of
500 /ug/ml (Jacobson et al., 1975).
183
Annona squamosa L. ANNONACEAE

Sweet sop, sugar apple
In Northern America and in Gambia the leaves of the sweet sop are used as an
insecticide and to eliminate bed-bugs (Dalziel, 1937). In Indonesia the seeds are used
against head-lice (Steenis-Kruseman, 1953).
From the bark, roots, seeds and stems of A. squamosa aporphine alkaloids (anonaine,
roemerine, norcorydine, corydine, norisocorydine and glaucine) have been isolated
(Bhakuni etal., 1972).
Anonaine has been found to possess antimicrobial properties against Staphylococcus
aureus, Klebsiella pneumoniae, Mycobacterium smegmatis and Candida albicans at the
100 juig/ml level (Chen et al., 1974). Corydine is reported to have anticancer activity
(Bhakuni et al., 1972). An ether extract of the seeds of A. squamosa has been found
to act as a stomach poison in the larvae and eggs of Bombyx mori and to be moderately
toxic to Musa nebulo and Triboleum castanum adults. When petroleum ether is added
to the extract an insoluble resin is formed and this treatment has been found to
increase the toxicity against M. nebulo by a factor of six (Mukerjee and Govind,
1958).
Santalum album L. SANTALACEAE

Sandalwood
A native of India introduced in parts of West Africa (Nigeria and the Ivory Coast),
this tree is used in India for its scented heart wood, yielding the fragrant sandalwood
oil.
From the bark a triterpenoid has been identified as urs-12-en-3/3-yl-palmitate
(Shankaranarayana et al., 1980). The bark is a waste material after sandalwood oil
extraction.
The benzene extract of the bark has insect growth-inhibiting and antireproductive
(chemosterilant) properties. Local application of the triterpenoid in micro-doses to
freshly formed pupae of economically harmful forest insects (Atteva fabriciella,
Eligma narcissus, Eupterote geminata, etc.) produced morphologically defective
adults with crumpled wings and shorter abdomen, suggesting a growth inhibition.
It has been observed that feeding a glucose solution containing a minute quantity of
the compound to freshly emerged moths prevented them from mating and laying
eggs, indicating an antireproductive (chemosterilant) effect (Shankaranarayana et
al., 1980). These authors write: 'Such chemosterilant compounds of late, are
becoming popular as "third generation pesticides" in controlling forest pests
without the bad side effects (like toxicity, environmental pollution etc.) generally
possessed by common organic pesticides.'
For a more comprehensive list of plants with insecticidal and molluscicidal action see
Table 4.6.
184 185
Table 4.6. Insecticidal and molluscicidalplants

Acacia nilotica Fruit, Tannins Molluscicidal, Bulinus truncatus, HusseinAyoub(1983,1984)
stembark Biomphalaria pfeifferi
Afrormosia laxiflora Rootbark Af-Methylcytisine Insecticidal N
Balanites aegyptiaca Stembark Saponosides, the genins are dios- Molluscicidal CV
and yamogenins
Seeds Furocoumarin Insect-feeding deterrent Hardman and Sofowora (1972)
Abdullah«a/.(1978)
Seida etal. (1981)
Tomassini and Mathos (1979)
Bidenspilosa Leaves Phenylheptatriene Toxic to insects and larvae Degener(1975)
Dichrostachys glomerata Roots Saponosides Molluscicidal to Bulinus globulus Bouquet (1972)
Adewunmi and Sofowora (1980)
Duranta repensc. Fruit juice Isoquinoline (alkaloid analogue Insecticidal lethal to anopheline Manson(1939)
to narcotine) and culcicine larvae Chopra etal. (1941)
Yousef(1973)
Leaves Flavonoids Makboul and Abdel-Baki (1981)
Euphorbia hirta Plant Euphorbon (triterpene, quercetol) Insecticidal anti-amoebic Heal and Rogers(1950)
antibacterial Debaille and Petard (1953)
Ridet and Chartol (1964)
Gupta and Garg( 1966)
Dhaietal. (1968)
Ndir and Pousset (1981)
Pousset(1981)
Hymenocardia acida Roots Hymenocardine (alkaloid) Insecticidal Heal and Rogers (1950)
Paisetal. (1976)
Milletia ferruginea (Fig. 4.11) Seeds Rotenone, saponins Insecticidal Paris andMoyse(1967, Vol. II,
p. 390)
Momordica charantia Leaves Momordicin Insecticidal, bacteriostatic Heal and Rogers(1950)
Watt and Breyer-Brandwijk
(1962)
Nicotiana tabacum Juice Nicotine, nornicotine, anabasine Insecticide, guinea worm (toxic!) Henry(1949,p.49)
Kerharo and Bouquet (1950)
Ocimum basilicum Leaves Methylchavicol, eugenol Chases ants, anthelmintic Heal and Rogers (1950)
O. canum Leaves Camphor Chases moths Nickel (1959)
Jain and Jain(1972)
Pentaclethra macrophylla Root Saponosides Insecticidal N
Soulimoveta/. (1975)
Piper guineense Fruit Piperine, dihydropiperine, Insecticidal and antibacterial Paris and Moyse( 1967, Vol. II,
dihydropiperlonguminine, (seeTable4.1) p. 114)
etc., dihydrocubebin Addea-Mensah«a7. (1977a)
Pseudocedrela kotschyi Bark Pseudocedrelin (phenolic lactone) Kills goldfish Moyse-Mignon (1942)
Quassia africana Stem wood Quassin Insecticidal, expels threadworms Heal and Rogers (1950)
Oliver(1960)
Securidaca longepedunculata Roots Triterpenic saponosides Molluscicidal Fraga de Azeveda and de
Medeiros(1963)
Kerharo(1968)
Sesamum indicum Plant Sesamine (lignan) Insecticide synergic to pyrethrum Webb (1948)
Ramaswany and Sirsi (1957)
Paris andMoyse(1971, Vol. HI,
p.251)
Spilanthus uliginosa Flower-heads Spilanthol = affinine (N-isobutyl- Larvicidal (anopheles, kills Heal and Rogers (1950)
decatriene-2,6,8-amide) cockroaches and bedbugs) Dhar«a/. (1968)
Tetrapleura tetraptera Fruit Saponosides (oleanic acid Insecticidal Adesina etal. (1980a)
triglycoside?) Sofowora (1980)
Thevetia neriifolia Fruit, leaves Aucubine (iridoid heteroside) Larvicidal and antibacterial CV
Sticher and Meier (1978)
Vemonia pauciflora Twigs (leafy) Sesquiterpenic lactones (vernolide Termites Kerharo and Adam (1974)
and hydroxyvernolide)
"Piperine is more toxic than pyrethrin to the housefly and 0.05% of piperine + 0.01% of pyrethrin is more toxic than a 0.1% solution of pyrethrin (Harvill and
Hartzell in Kerharo and Adam, 1974, p. 637).
186
(b) Molluscicidal plants

As already mentioned, snails can play an important part in the transmission
of diseases, especially those caused by Schistosoma spp. in their various forms. At
present over 200 million people in about 70 tropical and subtropical countries are
affected by endemic schistosomiasis (Hostettmann etal., 1982). The developmental
cycle in the snail (mostly Bulinus spp.) takes about 6 weeks. In the infected snail the
parasites are very prolific, a single miracidium can produce in optimal conditions
100000-250000 cercaria, these emerging at the rate of 50-1000 daily (none emerging
on dark days).
Active constituents
A number of plant extracts lethal to schistosome-transmitting snails were
submitted by Mozley (1939, 1952) to comparative tests. The fruits of Balanites
aegyptiaca Del., Swartzia madagascariensis* Desv. and Sapindus saponaria L. (grown
Fig. 4.11. Milletia aboensis (Hook.) Bak.

187
in West Africa, introduced from tropical America) were found to be amongst the
most promising molluscicides. Later, Lemma (1970) reported from Ethiopia the
strong molluscicidal properties of the dried berries of Phytolacca dodecandra
L'Herit. *, which also occurs in West Africa and which is widely used in Ethiopia as
a soap substitute. The active constituents in all these plants were found to be
haemolytic saponosides. Another plant, Croton macrostachys Hochst. ex Del., with
active molluscicidal properties, was reported from the Sudan (Amin et al., 1972).
The active factors of this were also saponosides (El-Kheir and Salih, 1979).
In 1977 Dossaji et al., performed tests with Polygonum senegalense*, a powerful
molluscicide in Kenya, where it is a common weed along rivers, lakes, etc. The
active components are pseudo-cyanogenetic glycosides. In West Africa, the mollus-
cicidal properties of Jatropha gossypiifolia* and J. curcas* fruits were examined by
Adewunmi and Marquis (1980) and the methanol-related extract of the fruit of J .
gossypiifolia was found to be particularly potent. Hydrocyanic acid and steroid
saponins are present in the plant.
In Securidaca longepedunculata (Polygalaceae) the molluscicidal action of the roots
is due to triterpenic saponins (see Table 4.6). In testing the molluscicidal activity of
24 saponins from various plants against Biomphalaria glabrata, Hostettmann et al.
(1978, 1982) reported that at concentrations of 32 p.p.m. and even of 16 p.p.m.
monodesmosidic triterpenoid saponins and saponins of the spirostanol series are
potent molluscicides. Bidesmosidic saponins and the aglycones (e.g. hederagin and
oleanolic acid) were found to be inactive. In Acacia nilotica galloyl tannins bind the
protein of snails, inhibiting their enzymes (Hussein Ayoub, 1984).
Swartzia madagascariensis Desv. CAESALPINIACEAE

The fruits are used in parts of West Africa, the Zambesi valley, Madagascar and Por-
tuguese East Africa as a fish poison, (although fish poisons are forbiddeen in Nigeria).
In Northern Nigeria the roots are occasionally added to the crushed fruits (Dalziel,
1937; Githens, 1949). In Senegal the roots are used in the treatment of leprosy and
syphilis and the fruits as an abortifacient (Kerharo and Adam, 1974). The heartwood
is termite and borer proof (Dalziel, 1937). In Bechuanaland the leaves are considered
a valuable means of combating the schistosoma-carrying snail and are said to have
insecticidal properties, especially against termites (Schultes, 1979).
From the heartwood, pterocarpanoid constituents have been isolated (Harper et al.,
1969). The fruit valves were found to contain a yellow flavonoid pigment which gave,
on hydrolysis, swartziol (=kaempferol), rhamnose and glucose. In addition, triter-
penoid saponosides and catechuic tannins have been reported. The seeds also contain
saponosides and are strongly haemolytic (Beauquesne, 1947; Paris and Bezanger-
Beauquesne, 1956). Harborneera/. (1975) confirm the presence of isoflavones.
The fruits have been shown experimentally to possess ichthyotoxic properties and to
kill fish in concentrations of 0.1% within 2 h, whereas they are toxic to guinea pigs
only at higher concentrations (5 g/kg given perorally) (Gaudin and Vacherat, 1938;
Beauquesne, 1947). They are also lethal to the snails transmitting bilharzia at higher
concentrations (schistosomiasis).
188
Phytolacca dodecandra l'Herit. syn. (P. abyssinica Hoffm.) PHYTOLACCACEAE

Endod, soapberry tree
In some parts of West Africa the young shoots are used as a potherb and in the Ivory
Coast as a substitute for spinach. On the other hand in East Africa and in Madagascar
the berries and the juice of the fresh leaves are said to have caused death and the
leaves are said to be the most dangerous of the Chagga abortifacients (a cheekful of
leaves and young shoots is chewed and the juice swallowed, abortion commencing
about 10 h later) (Watt and Breyer-Brandwijk, 1962). In Southern Nigeria the ashes
of the burnt plant are used for making soap and in Somalia, Ethiopia and Uganda an
infusion of the seeds or berries is used as a soap for washing clothes (Dalziel, 1937;
Watt and Breyer-Brandwijk, 1962). A higher mortality of molluscs along the rivers
in Ethiopia where the inhabitants washed their clothes with the berries induced
Lemma to study the molluscicidal properties of the plant (Lemma, 1970).
Investigations into the nature of the active principle showed that the active part was
a saponoside, endod, the genin of which could be traced back to oleanolic acid by
several authors. A freeze-dried aqueous extract was actively molluscicidal at concen-
trations of 1.25-2.5 p.p.m. (Jewers, Tropical Products Institute London, 1968
quoted in Lemma (1970)). A steroid saponin has been found in the roots (Ahmed et
aL, 1949).
After 24 h of exposure endod killed all species of snails tested in comparative
experiments with other molluscicides (N-tritylmorpholine, copper sulphate,
ethanolamine of niclosamide). The test animals were killed in all cases by concentra-
tions of less than 30 p.p.m. Whole and powdered berries kept at room temperature
(22°C) for 4 years displayed no change in their molluscicidal potency during
six-monthly tests, whilst the crushed fresh berries, and a solution prepared from
them, lost their potency within a few days. The potency of the crude berries
remained stable over a wide range of pH values and temperatures, under ultra-violet
irradiation and in various concentrations of river-bed mud. The low solubility of the
saponin from the whole berries also appears to be a notable feature. For mammals
and birds, the LD 50 is above 2 g/kg. The berries do not harm germination, growth
rate or the morphology of vegetation. They have no insecticidal or larvicidal action
and their toxicity to fish is similar to that of the above-mentioned molluscicides. In
a concentration of 4 p.p.m., leeches are killed in 6 h. The Cercariae and miracidia of
Schistosoma haematobium are killed in 10 min by 1000 p.p.m., in 1 h by 100 p.p.m.
and i n 2 h b y 5 0 p . p . m . Thus P. dodecandra seems to be a cheap and effective means
of eliminating Schistosoma in certain areas (Lemma, 1970). Only short staminate
plants produce berries and the haemolytic activity of the samples runs parallel with
the molluscicidal effect. Although in Ethiopia the unripe berries are always used for
washing clothes (highest saponin level), sometimes the over-ripe berries have also
shown a marked capacity to kill snails (Lugt, 1980). Endod has a weak ovicidal
effect: it is not ovicidal at the concentration at which it kills adult snails. This
difficulty can, however, be overcome by repeated treatment as has been
demonstrated in the field. The molluscicidal potency (CL90) for eggs of Bulinus
189
truncatus sericinus is of the order of 50-100 p.p.m. in 6 h (Lemma, 1970). The berries
show approximately equal potency against different species of snail in a 24-h
exposure at 30 p.p.m., whereas in a 6-h exposure, Physa acuta was the least and
Biomphalaria pfeifferi rupelli the most resistant species of snail examined (Lemma,
1970).
Croton macrostachyus Hochst. ex Del. syn. (C. guerzesiensis Beille)

EUPHORBIACEAE
In East Africa, the bark of this tree is reported to be used as a cathartic (Githens,
1949).
The testa, constituting 40% of the weight of the kernels, possess no molluscicidal
activity. Only alcoholic and aqueous extracts of the kernel were biologically active;
chromatographic screening showed that the seeds contain alkaloids, amino acids and
sterols as well as triterpenes or their saponins. Biological testing indicated that the
zone corresponding to the sterols and triterpenes was the only active one. Finally,
the molluscicidal action was found to be due to at least two saponins and the activity
was greatly increased by freeing the saponins from the other constituents of the
seeds. Activity was raised from 2 p.p.m. for the alcoholic extract to 0.06 p.p.m. for
the purified saponins (El-Kheir and Salih, 1979).
The crude ground seeds of this tree showed high molluscicidal activity compared to
plants previously investigated (Amin et al., 1972).
Polygonum senegalense Meisn. syn. (P. glabrum of F.T.A.) POLYGONACEAE

Polygonum senegalense forma albotomentosum R. Grah.
These plants and related species are 'pounded with native natron and rubbed into
the limbs as a remedy for rheumatic and other swellings, and applied to syphilitic
sores' (Dalziel, 1937).
The flavonoids luteolin, quercitin, luteolin-7-O-glucoside and quercitin-3-O-galac-
toside have been isolated and identified in P . senegalense (Abd El-Gawad and El Zait,
1981). As aqueous extracts of the plants release cyanate ions on alkaline hydrolysis,
the molluscicidal compounds may be chemically related to pseudo-cyanogenic
glycosides or azoxyglycosides such as cycasin and macrozamin (Dossaji et al., 1977).
In 1978, Maradufu and Ouma considered 2,4-dihydroxy-3,6-dimethoxy-chalcone
to be responsible for the molluscicidal activity.
Cut leaves of both above-mentioned varieties proved to be potent molluscicides.
Tests were carried out with aqueous extracts of P . senegalense forma senegalense on
the snails Biomphalaria pfeifferi and Lymnaea natalensis. Isolation of the highly
water-soluble active principle increased the molluscicidal effects to 70% and 60%
mortality after 1 h for Biomphalaria and Lymnaea, respectively, with concentrations
of 25 p.p.m. and 100% mortality for both species after 24 h. The activce constituent
was subsequently identified as quercetin-3(2" )-galloylglycoside (Dossaji and Kubo,
1980). The fact that the plant grows near rivers, lakes, etc. should facilitate its use in
the control of snails (Dossaji et al., 1977).
190
Jatropha gossypiifolia L. EUPHORBIACEAE

Wild cassada, red fig-nut flower
Jatropha curcas L.
Barbados nut
The viscid sap is used to cure sores on the tongues of babies (Pthrush) (Irvine, 1961)
and in India the leaves ofJ. gossypiifolia are applied to boils and carbuncles, eczema
and rashes (Chopra et al.9 1956). The rootbark ofJ. curcas, dried and pulverized, is
applied as a dressing for sores (Irvine, 1930). The seeds are a (dangerous) purgative
and are given as a remedy against venereal diseases (Dalziel, 1937).
J. curcas contains a non-drying fixed oil consisting mainly of glycerides of stearic,
palmitic, myristic, oleanic and curcanoleic acids (the latter belongs to the same
group as ricinoleic and crotonic acids) (Watt and Breyer-Brandwijk, 1962). In the
Indian plant, vitexin and isovitexin (flavonoids) were found (Sankara, 1971). The
seeds contain a mucilage and a toxalbumin, curcin, with seven protein groups
(Mourgue et al., 1961; Hufford and Oguntimein, 1978). In the fruit, roots and bark,
cyanic acid, and in the bark a steroid saponoside have been found (Watt and
Molluscicidal activity against Bulinus globulus was shown by all Jatropha spp. tested.
The methanolic extract of the fruit of J . gossypiifolia was the most potent. Its mean
lethal concentration (LC50) was 11.55-16.24 p.p.m. The LC 50 of the seed and that
of the rootbark of J . curcas were 120.55 and 125 p. p.m., respectively, and the LC 50
of the seeds and that of the stem of J. podagrica were 130.73 and 125.08 p.p.m.,
respectively. Thus these were ten times less potent than the extract of/, gossypiifolia.
The potency remained stable after UV radiation and over a wide range of pH values,
but was reduced in the presence of minerals and faecal impurities (Adewunmi and
Marquis, 1980). The molluscicidal properties of Jatropha were also examined by
Amin et al. (1972) and the antibacterial and pharmacological properties of J.
podagrica were studied by Odebiji (1980), Ojewole and Odebiji (1980) and Ojewole
(1981).
Hormones of the adrenal cortex
I Introduction: the action of plants on hormone secretion in Man

A number of plant constituents can act as a substitute for natural hormones
in cases of hormone deficiency. Some of these constituents have been found to be
chemically identical with the natural hormone (e.g. oestrone in the kernels of date
and oil palm). Other plant components have a structural similarity to the hormone
(e.g. Funtumia and Holarrhena alkaloids and corticosteroids). Others again have an
entirely different chemical structure (e.g. coumestans and isoflavones with oes-
trogenic action). All these constituents can act as a substitute for hormones and
replace them in their biological functions.
Plant components often have an indirect action on the secretion of certain
hormones by stimulating or inhibiting other areas like the hypothalamus and the
pituitary gland which can control the function of most other glands (e.g. gonado-
trophic, thyrotrophic and corticotrophic action). (For more details see Plants acting
on sex hormones.) However, great precaution should be taken in using the
hypothalamus-pituitary axis as a narrow interrelationship exists and often hormonal
or pharmacological actions other than those desired can be obtained (Bianchi, 1962;
Goodman and Gilman, 1976). Thus stimulation of lactation has been obtained with
dried thyroid gland or thyroxine (Robinson, 1947; Naish, 1954), no doubt through
indirect action via the pituitary gland and an impairment of the pituitary adrenal
response to acute stress is observed in alloxan diabetes (Kraus, 1949).
Plant constituents capable of influencing hormone-controlled metabolic actions
may also act by removing hormone-inactivating compounds such as enzymes (thus
plant constituents can inhibit insulinase in hypoglycaemic plants or certain enzymes
in antifertility plants). Also, certain plant substances can antagonize hormone-
controlled action (thiocyanates can inhibit the secretions of the thyroid gland). As
the future will no doubt reveal, there are many more ways in which the secretion of
the hormones can be stimulated or inhibited.
Those plants already described in Chapter 2 as acting on the cardiovascular system
are indicated hereunder by CV in both tables and text. Similarly, the plants already
192
described as acting on the nervous system (Chapter 3) are indicated by N and those
with an anti-infectious (antibiotic or antiparasitic action (Chapter 4)) are indicated
by I.
The plants marked by an asterisk (*) in the enumeration of the constituents are
described in this text, the others can be found in the corresponding tables.
II Plants acting like hormones of the adrenal cortex

The internal fasciculated zone of the adrenal cortex produces cortisol,
hydrocortisone and corticosterone under the control of the pituitary corticotrophin
adrenocorticotrophic hormone (ACTH) which is in turn controlled by the cortico-
trophin-releasing factor (CRF) of the hypothalamus. The external glomerulated
zone of the cortex produces aldosterone. Cortisol is mainly used for its anti-inflam-
matory action and its effect on the glucides, whilst corticosterone and aldosterone
mainly act on sodium retention. Cortisol can also act on the electrolyte balance; it is
the prototype of the glucocorticoids or glucocorticosteroids. Besides their anti-
inflammatory and immuno-depressive actions these substances can act on diuresis,
intercranial hypertension and asthma. Plant equivalents of these compounds should
thus be examined for each action separately. The role played by the pituitary-
hypothalamus axis makes this examination still more complicated. For example,
inflammatory action can be controlled not only by corticosteroids but also by other
anti-inflammatory agents which often have analgesic and antipyretic properties as
well (e.g. salicylates and phenylbutazone). In many cases it is difficult to decide
whether the action of a constituent of a given plant depends on its action on the
adrenal-pituitary axis if no indication has been given by the authors. In a few rare
cases the general action of a plant on both the adrenals and the pituitary has been
reported. Two examples of this are for the actions of Funtumia africana* and
Holarrhena floribunda*, where the anti-inflammatory action is mentioned as part of
the many other effects of the different constituents. The anti-inflammatory con-
stituents in Funtumia are glucofuntamine and funtumine and those in Holarrhena are
holamine and holaphylline. They are all steroid alkaloids.
For the reasons mentioned above the other plants with anti-inflammatory action
will be described under the heading Anti-inflammatory plants.
Two non West-African plants known to act on the adrenal cortex are Panax
ginseng and Eleutherococcus. Equivalent plants have not been reported in the area.
The stimulating action of ginseng on glucocorticoid production is believed to be
of neurogenic origin. Ginseng appears to facilitate the adaptation of the adrenocor-
ticol function to the need of the organism under changing conditions. Its effect is also
manifested after hypophysectomy so it seems to act upon the peripheral site of the
stress mechanism. Anti-inflammatory and anti-exudative as well as cardiovascular
effects of the drug have also been reported (Brekhman and Dardymon, 1969; Chul
Kim et al.9 1970).
193
Funtumia africana (Benth.) Stapf syn. (Kicksia africana Benth., K. latifolia Stapf,
F. latifolia (Stapf) Schlechter, K. zenkeri Schum.) APOCYNACEAE
False rubber tree
In Ghana the roots are mixed with palm wine and given to patients suffering from
incontinence. The dried pulverized leaves are applied as a dressing to burns (Dalziel,
1937). The latex of F. elastica Stapf has been used as a source of rubber. Its bitter
bark is used as a remedy for haemorrhoids.
The leaves of F. africana contain up to 4% of total alkaloids. The main alkaloid,
funtumine, is 3-a-aminopregnane-20-one, funtumidine is 20a-hydroxy-3-a:-
aminopregnane. The presence of glucofuntamine has also been reported (Quevauvil-
ler and Blanpin, 1960).
Funtumine has hypotensive, antipyretic and local anaesthetic properties and the
Funtumia alkaloids are similar in action and constitution to those of a related
Apocynaceae, Holarrhena floribunda (see CV) (Fig. 5.1). This similarity is also
confirmed in the hormonal activity of these alkaloids. Funtumine and holamine
(3a-amino-5-pregnen-20-one) were observed to antagonize the effects of oestrogens.
Holaphyllamine (3/3-aminopregnen-20-one) enhanced the activity of oestrogens and
testosterone in female and male animals. Funtumine, funtumidine, glucoholamine,
holaphyllamine and holaphylline (3/3-methylamino-5-pregnen-20-one) showed anti-
gonadotrophin action as well as corticotrophic activity. Funtumine antagonized the
release of corticotrophin like cortisone. All of the above-mentioned steroid alkaloids
had anti-inflammatory properties, holamine and holaphylline being the most effec-
tive, followed by glucofuntamine and funtumine. The steroids increased liver
glycogen and decreased the weight of the thymus. Holamine and holaphylline cause
sodium retention and all three holarrhena alkaloids act as diuretics in rats. Holamine
was found to decrease the protein and water content of the liver indicating an
anti-anabolic action, and funtumine and funtumidine lowered the serum cholesterol
and raised the phospholipid levels and may have anti-atherogenic properties. The six
steroids appear to share the neurotrophic effects of steroids; all potentiated the
narcotic action of pentobarbital and their toxic effect appears to be confined to the
CNS. On intravenous injection in mice their LD 50 values vary from 28 to 31 mg/kg,
holamine being slightly less toxic (the LD 50 is 37 mg/kg). All of them caused
depletion of adrenal ascorbic acid (Blanpin and Quevauviller, 1960a, b; Quevauviller
and Blanpin, 1960).
Funtumidine, holaphyllamine and to a lesser extent holamine have been found on
subcutaneous injection of 5 mg/kg to exert antipyretic effects in rabbits made
hyperthermic by injection of bacterial vaccine. An analgesic effect to thermal or
mechanical stimuli in mice has been observed only with funtumidine (25 mg/kg
given intraperitoneally). Glucofuntamine was more effective as a local anaesthetic on
rabbit skin than cocaine; funtumidine and the holarrhena alkaloids were less
effective. Funtumidine had the most consistent tranquillizing effect and was also
hypotensive in rabbits (0.2 mg/kg). Funtumine had a spasmolytic action in particular
against acetylcholine (Blanpin and Quevauviller, 1960a, b).
194
Corticosteroids are frequently prepared by hemisynthesis from plant sources such

as diosgenin (see Dioscora spp. (Chapters 2 and 3)). Many other sources are found in
West Africa, for example sarmentogenin (see Strophanthus sarmentosus (Chapter 2)),
diosgenin plus yamogenin from the fruit oiBalanites aegyptiaca (Chapters 2 and 4)
(Hardman and Sofowora, 1971) and solasodine (from Solanum torvum). Another
West African source might be costugenin (3% in Costus afer (Iwu, 1982)). Some of
these constituents have oestrogenic activity themselves.
Fig. 5.1. Holarrhenafloribunda(Don) Diir. & Schinz.

195
Anti-inflammatory plants
The inflammatory reaction
Inflammation, whatever its origin (which may be infectious, chemical or
physical), generally occurs in three consecutive phases:
(1) an increase in capillary permeability with hyperaemia and oedemas;
(2) cellular infiltration (phagocytosis by polynuclear cells and interference of
lymphocytes);
(3) proliferation of fibroblasts and synthesis of collagen fibres and mucopoly-
saccharides, forming new conjunctive tissue.
If the new conjunctive tissue is attacked in turn by phagocytes and lymphocytes, a
chronic inflammation results. Rheumatoid arthritis is a classic example of these
conditions (Lechat et al., 1978).
Some of the anti-inflammatory drugs are more active in the initial stages of the
inflammation (e.g. salicylates and Curcuma). Others tend to act in later stages
(glucocorticosteroids and Phytolacca) whilst others again are active in both stages
(Commiphora, Crateva, Terminalia and Withania).
Several pharmacological tests have been devised to measure anti-inflammatory
activity, most being based on experiments with inflammation in rats. These are:
(1) carrageenan and kaolin-induced hind-paw oedema (or rat pedal oedema),
formalin-induced arthritis of ankle joint in rats; yeast-induced paw
oedema, croton oil-induced granuloma, cotton-pellet granuloma (Winter
etal., 1962; Benitz and Hall, 1963; van A r m a n i al., 1965);
(2) adjuvant-arthritis, where injection of Mycobacterium butyricum in one hind-
paw produces inflammation in the other paws and granulations in the ears;
(3) graft- versus-host reaction in chicks (against lymphocytes of hens), which is
used to test immune reaction.
It has been noticed that drugs which block inflammatory- and arthritis-like
syndromes in animals are also effective against rheumatic diseases in Man. Inflam-
mation in patients with rheumatoid arthritis implies the combination of an antigen
(gamma-globulin) with an antibody (the rheumatoid factor) and a complement,
resulting in phagocytosis by leucocytes and release of lysosomal enzymes. These
enzymes damage cartilage and other tissues and enhance the inflammation (Wood-
bury and Fingl, in Goodman and Gilman, 1975). Prostaglandins are also formed by
leucocytes during phagocytosis. Local injection of prostaglandin Ex or E2 causes
definite vasodilatation and hyperaemia and increases the permeability of cell
membranes, and it is believed that inhibition of prostaglandin synthesis is one effect
of anti-inflammatory drugs (Ferreira and Vane, 1974; Awouters et al., 1978;
Oriowo, 1982). Other effects are stabilization of the lysosome membranes by
prevention of loss of enzymes from the lysosomal envelope, uncoupling of oxidative
phosphorylation (Whitehouse, 1965; Whitehouse et al., 1967) and inhibition of the
synthesis of mucopolysaccharides (which constitute the fundamental substance of
conjunctive tissue and cartilage (Paulus and Whitehouse, 1973; Lechat etal., 1978).
Various mechanisms interfering with antigen-antibody aggregation have also been
considered, including inhibition of antigen-induced release of histamine.
196
Interference with prostaglandin synthesis has been observed in the case of

Zanthoxylum zanthoxyloides and Terminalia ivorensis. Immuno-depressive action has
been reported for Allium and Withania somnifera, and Solarium spp.
Chemical mediators in inflammation processes are histamine, 5-hydroxytryp-
tamine (serotonin), vitexin and bradykinin (Prabhakar et al., 1981; Saxena et al.,
1982). Antihistamine action has been reported for Anthocleista, Arnebia, Callo-
phyllum, Citrus, Crateva, Cryptolepis, Curcuma and Ipomoea.
In some cases the anti-inflammatory action seems to be independent of the
pituitary-adrenal axis (e.g. that of Cypenis rotundus and Commiphora) whilst in other
cases the drugs are said to have a direct action on the adrenal cortex (e.g. curcumin
(Chandra and Gupta, 1972) and glycyrrhetic acid (Gibson, 1978)).
As the plant triterpenoids often turned out to be active anti-inflammatory
constituents, their anti-inflammatory and anticonvulsant properties were evaluated
in rodents by Chaturvedi et al. (1974, 1976). For a number of natural plant
triterpenoids the protection afforded against carrageenan-induced rat-paw oedema
ranged from 9-48% when they were given intraperitoneally in doses of 40 mg/kg.
Good correlation has been observed between the anti-inflammatory and antipro-
teolytic properties of these plant products. The latter activity was demonstrated by
in vitro inhibition of trypsin-induced hydrolysis of bovine serum-albumin and
casein. All the tested triterpenoids except friedelinoxime and acetylmethylursulate
provided 10-40% protection against pentylene-tetrazol-induced convulsions in
mice.
Active constituents of anti-inflammatory plants in West Africa

In ^ e s t Africa the most effective anti-inflammatory plants seem to be
those which have the following active constituents.
Steroid or triterpene glycosides. Steroids or their heterosides are found in Com-
miphora indica*, Costus afer*, Cyperus rotundus*, Leptadenia pyrotechnica, Solarium
torvum* and other Solarium spp. and Withania somnifera*. The triterpenic glycosides
involved are the glycyrrhetic heterosides in Lonchocarpus cyanescens* and Terminalia
ivorensis* or the oleanolic heterosides found in Boerhavia diffusa, Gymnema sylvestra,
Securidaca longepedunculata, Tetrapleura tetraptera and probably Phytolacca
dodecandra*. Triterpenoids are also present in Alstonia boonei (bark), which is
applied topically in the treatment of rheumatic pains.
Terpenes (and their heterosides). These are found in Azadirachta indica, Atractylis
gummifera c , Crateva religiosa, Xylopia aethiopica and Vernonia colorata.
Alkaloids and amides. These seem to be responsible for the anti-inflammatory
action in Anthocleista procera, Capsicum frutescens*, C. Annuum*, Cryptolepis san-
guinolenta* and Zanthoxylum zanthoxyloides*. Pungent amides are also found in
Piper guineense and P. umbellatum (chavicine and piperine) as well as in Capsicum
spp. The latter may also act through their flavonosides.
Flavonosides. Flavonosides, of which a number contain coumarins, are found in
Afraegle paniculata*, Arnebia hispidissima*, Calophyllum inophyllum*, Canscora
decussata, Citrus nobilis, Dalbergia sissoo and Hibiscus vitifolius. Few of the above-
197
mentioned plants belong to the same family; there are, however, three Solanaceae
and three Rutaceae, of which two have anti-inflammatory constituents belonging to
the same chemical group.
Sulphur heterosides. Many of the plants used in local medicine in the treatment of
rheumatic diseases are found in this group. Their constituents or scission products
often contain pungent mustard oils or amides which act as counter-irritants or
rubefacients, diverting hyperaemia by irritation of the skin or intestine, and these
have been used, mostly locally, in the treatment of arthritis, lumbago, rheumatism
bronchitis, congestion of the lungs, etc. In West Africa they are found in Cap-
paridaceae, namely glucocapparin in Capparis decidua, Crateva religiosa and Gynan-
dropsis gynandra; tropaeolin in Carica papaya seeds, glucotropaeolin (spirochine) in
Moringa oleifera and alliin in Allium sativa and A. cepa.
Other constituents. Other active constituents are reported to be tetrahydrocan-
nabinol in Cannabis sativa (the resin of which has also been found to contain
coumarin glycosides), the dyes haematoxylin and brasilin in Haematoxylum cam-
pechianum, tertiary phenylethylamines in Desmodium gangeticum and curcumine in
Curcuma domestica*. The active fraction in Salvadora persica * could be /3-sitosterol;
in Ipomoea spp. * it has not yet been identified.
Many of these plants also have an antibiotic action, which in some cases may
contribute to their effectiveness.
A number of these plants (those marked with an asterisk (*)) are described in
more detail to give a better understanding of their possible therapeutic interest and
modes of action. The others are listed in Table 5.1 (p. 211).
Plants with steroid or triterpene glycosides as active constituents.
Commiphora africana (Rich.) Engl. syn. (Heudelotia africana Rich., Balsamoden-

dron africanum (Rich.) Arn.) BURSERACEAE
African bdellium or African myrrh
In Niger country a maceration of the stembark of C. africana is given perorally in the
treatment of rheumatic diseases (Adjanohoun, 1980). In West Africa the gum-resin
is boiled for treatment of inflammation of the eyes by holding the face over the
steaming pot. For scorpion-bite the bark is applied after it has been chewed with
natron (Dalziel, 1937).
The gum-resin contains 70% alcohol-soluble resin and 30% water soluble gum. The
resin contains 7-9% of essential oil (Dalziel, 1937; Kerharo, 1968) and is composed
of free terpenoids and terpenoid glycosides and the gums are composed of
polyholosides (Boiteau etal., 1964).
In the Indian Commiphora mukul Hook, ex Stocks the essential oil has been found
to contain 4-6% of myrcene, 11% of dimyrcene and some polymyrcene. The
petroleum ether extract of the gum-resin has yielded sesamin, cholesterol and a few
other steroids (Indian Council, 1976, p. 271). A number of steroids have been
isolated and identified and the diterpenoid constituents cembrene A and mubulol as
well as some fatty tetrols have been reported (Patil et al., 1972).
198
P The oleo-resin fraction from C. mukul has shown significant anti-arthritic and
anti-inflammatory activity (minimum effective dose 12.5 mg/100 g in albino rats).
This activity has been localized in the acidic fraction of the oleo-resin and has been
shown to occur even in adrenalectomized animals (Santhakumari et al., 1964).
The aqueous extract of the oleo-gum-resin of C. mukul had suppressive action on
carrageenan-induced acute rat paw oedema and in the granuloma pouch test as well.
In adjuvant arthritis the secondary lesions were very effectively suppressed without
any significant action on the primary phase. Side-effects were negligible as compared
to those occurring in beta methasone-treated animals (Gujral et al., 1960; Satyavati
et al. ,1969).
A steroidal compound isolated from the petroleum ether extract of C. mukul
showed a dose-dependent anti-inflammatory activity on rat paw oedema which was
much more potent than that of the resin fraction. The steroid fraction had a
pronounced effect on primary and secondary inflammation induced by Freund's
adjuvant; it was less effective than hydrocortisone acetate in the primary phase but
more effective in reducing the severity of secondary lesions (Arora et al., 1972).
Furthermore, C. mukul was also found to lower the serum cholesterol in hyper-
cholesterolaemic rabbits and to protect the animals against cholesterol-induced
atherosclerosis (Satyavati et al., 1969; Nityanand et al., 1973). Long-term experi-
mental studies of its effectiveness as a hypolipaedemic agent gave satisfactory results
and showed that the effect could be attributed to (a) an increase in the rate of
removal/excretion of cholesterol, (b) a decrease in the input/synthesis of cholesterol
and (c) mobilization of cholesterol from tissues (Indian Council, 1976, pp. 272-5).
In view of the interesting results obtained with Indian myrrh, African myrrh
might be examined chemically and pharmacologically for similar properties.
Costus afer Ker-Gawl. syn. (C. obliterans Schum., C. anomocalyx Schum, C. in-
sularis Chev., C. lucanuscianus Chev.) (Fig. 5.2) ZINGIBERACEAE
Ginger lily
L C. afer is widely used as a cough medicine, either as a decoction of the stems or the
pounded fruit, or by chewing the succulent stem itself. The boiled root is applied to
cuts and sores and a soothing fomentation for rheumatic pains is prepared with the
boiled leaves (Dalziel, 1937, p. 472).
C The abundant juice of the leaves (69.7%) (Odutola and Ekong, 1968) contains 0.4%
oxalate, furan derivatives and starches.
Thin-layer chromatography of extracts of the tubers with petroleum ether and
chloroform yielded three compounds which were identical with lanosterol, tigonenin
and diosgenin. Iwu (1982) could isolate from the chloroform extract 3% costugenin,
the most abundant sapogenin (closely related to sarmentogenin), 1.5% stigmasterol
and 0.8% diosgenin. Similar sterols had been reported to be present in C. speciosus
(Bhattacharyaertf/., 1973; G u p t a s al., 1980, 1981).
P In clinical trials, 25 patients, 17 of whom were suffering from rheumatoid arthritis
and 5 from osteo-arthrosis, received, in groups of seven, differential solvent extracts
(prepared according to traditional methods by native doctors) of C. afer (30 ml doses
199
twice daily) for four days and, after an interruption of three days, the same treatment
for ten days. Two further groups of seven patients received the same treatment with
extracts of Lonchocarpus cyanescens and Terminalia ivorensis (see below for these
plants). All the patients suffering from rheumatoid arthritis were relieved of their
symptoms (Iwu and Anyanwu, 1982a, b). Three of the patients who received
Lonchocarpus and one each of those receiving Costus and Terminalia reported
complete recovery. Only two of five patients suffering from osteo-arthrosis showed
some improvement (no results with Costus).
In pharmacological tests with the same three plants the extracts reduced car-
rageenan-induced oedema in the rat paw, checked diarrhoea due to arachidonic acid
and castor-oil (Awouters et al., 1978) and ameliorated all signs associated with
adjuvant-induced polyarthritis in rats. The extracts were well tolerated in daily
doses of 100-300 mg/kg except for the chloroform extract of C. afer, which caused
the death of four out often experimental animals at that dose regimen.
Further chemical and pharmacological tests are planned by the authors (Iwu and
Anyanwu, 1982b).
Fig. 5.2. Costus af<?rKer-Gawl.

200
Cyperus rotundus L. CYPERACEAE

Nutgrass
The rhizomes are slightly fragrant and the essential oil they yield is used in Asia as a
perfume for clothes and to repel insects. In Nigeria the plant is used as cattle fodder
and the tuberous rhizomes as a cough medicine for children. In the Congo
Brazzaville the pulp of the roots is used in frictions for oedema and rheumatism
(Dalziel, 1937; Bouquet, 1969). In India the tubers are reputed to be diuretic,
emmanagogic and anthelmintic and are used for treating disorders of the digestive
tract (Chopra etal., 1956, p. 88; Hegnauer, 1964, Vol. Ill, p. 285).
The tubers contain a fatty oil, which is chiefly made up of glycerides of oleic, palmitic
and linolic acids with small quantities of essential oils. The crude volatile oil has been
noted to contain about 40% of a sesquiterpenic ketone, a-cyperone (McQuillin,
1951). In tubers collected in India, the essential oil fraction is reported to be
composed of pinene, traces of cineol, sesquiterpenoids, monoterpenic and aliphatic
alcohols and /3-sitosterol (Kalsi et al., 1969). The sesquiterpenoids were identified by
Kapadia et al. (1967). In C. esculentus cholesterol has also been found (Abu-Mustafa
et al., 1960).
The anti-inflammatory action has been studied in India on oedema induced in the rat
paw by carrageenan or by cotton-pellet implantation and was first attributed to the
petroleum ether extract of the roots. Then a triterpenoid obtained from this extract
by chromatographic separation was shown to possess an anti-inflammatory activity
which was eight times greater than that of cortisone; the fraction also had antipyretic
properties (in pyrexia induced by brewer's yeast) plus an analgesic action. On
intraperitoneal administration the LD 50 of the extract was 50 mg/kg; the ED 50 was
1.6 mg/kg (Gupta et al., 1970). Later, /3-sitosterol isolated from tubers grown in
India was found to be a powerful agent against inflammation in the above-mentioned
tests (Bach, 1978). When it was administered intraperitoneally the effect was similar
to that of hydrocortisone and oxyphenbutazone and the substance was also effective
against carrageenan-induced oedema when given perorally. Its action proved to be
independent of the pituitary-adrenal axis and to be similar to that of acetylsalicyclic
acid. /3-sitosterol showed a broad safety margin as in intraperitoneal administration
the LD 50 was more than 3 g/kg in mice and the minimum ulcerogenic dose was
600 mg/kg in rats (Gupta et al., 1980). The essential oil was reported to have
oestrogenic activity which could be attributed to cyperene I, a hydrocarbon fraction
(Indira tf al., 1956).
Solanum torvum Sw. including S. torvum var. compactum Wright syn. (S. mannii
Wright including var. compactum Wright) SOLANACEAE
The small orange-red berries are eaten cooked or sometimes raw. In Sierra Leone a
decoction of the fruit is used as a cough medicine for children (Dalziel, 1937, p. 435).
The fruits contain sitosterol D-glucoside and 0.1% of the glucoalkaloid solasonine
(solasodine-glycoside), from which solasodine is obtained. Solasodine is used as a
starting product in the hemisynthesis of cortisone and sex hormones (Chopra et al.,
1956, p. 230). The glycoalkaloid contents vary considerably during growth (Paris
201
and Moyse, 1971, Vol. Ill, p. 148). Furthermore, S. torvum yields a rare sterol, first
reported from S. cerasiferum Dun. syn. (5. xanthocarpum) (Sayed and Kanga,
1936), which has been shown to have the structure of (22R)22 hydroxy-6-oxo-4a-
methyl-5a:-stigma-7-en-3/3-yl benzoate (Beisler and Sato, 1971). S. torvum contains
as much as 0.04% of carpestrol (Bhattacharya et al., 1980).
The steroidal alkaloid solasodine has been shown to cause thymolysis in rats and to
have antiphlogistic properties in experimental arthritis in rats and in experimental
burns in rabbit ears. Investigation of the immunomodulating properties of sola-
sodine (isolated from S. nigrum) and of withanolide D from Withania somnifera
showed that both substances had an immunodepressive action in vitro (Bar and
Hansel, 1982).
Carpestrol has also been reported to produce a dose-dependent inhibition of
carrageenan-induced paw oedema in albino mice. As compared to withaferine A and
hydrocortisone it showed the highest potency, being active in doses of 0.9 mg/kg
when given intraperitoneally, whilst the LD 50 for mice of carpestrol given intra-
peritoneally is 500 mg (±8 mg)/kg and that of withaferine A is 110 mg (±5 mg)/kg.
Carpestrol has certain structural similarities to hydrocortisone and withaferine A,
both of which also have anti-inflammatory activity (Bhattacharya et al., 1980).
Withania somnifera L. SOL AN ACE AE

Winter cherry
The roots of this plant, already reported to have sedative and antibiotic properties
(N and I), have been used for centuries in folk medicine to treat rheumatism, ulcers
and skin diseases (Menssen and Stapel, 1973). The roots contain withaferine A and
several other steroidal lactones and withanolides, and these were also isolated as
minor constituents of the leaves (Abraham et al., 1975). Withaferine A is also a
tumor inhibitor (Kupchan et al., 1965).
Withaferine A and withanolide D (isolated by Menssen and Stapel, 1973) have
been shown to be active against inflammation. Six intraperitoneal doses of withaf-
erine A of 25 mg/kg every second day in one series of tests, and twelve doses of
12.5 mg/kg every second day in a second series of tests, have been shown to delay the
onset of adjuvant arthritis in rats and strongly to inhibit swelling and inflammation
of the diseased area and of the secondary lesions (Fuegner, 1973; Roshchin and
Geraschenko, 1973). Withaferine A has also been observed to inhibit the xenogenic
graft-versus-host reaction in chicks to a great extent (Fuegner, 1973; Bar and
Hansel, 1982). The mode of action of withaferine appeared to be similar to that of
prednisolone and azathioprin (purine antagonist). The similarity of their structures
and actions to those of glucocorticosteroids had already suggested that withaferine
and withanolide D might have, besides their antiproliferative effect, a complex
influence on inflammation and immune responses (Bar and Hansel, 1982). Shohat et
al. (1978) also observed that in concentrations of 1 /xg/ml withaferine A and
withanolide E showed immuno-depressive action in cultures stimulated by 1 fJLg/ml
and 0.3 /xg/ml phytohaemaglutinin and in those without mitagenic stimulation. The
functional activity of normal human T lymphocytes as assessed by local xenogenic
202
graft via host reaction was also affected by these two steroidal lactones. Apparently,
withanolide E had a specific effect on T lymphocytes whereas withaferine A affects
both T and B lymphocytes. The authors believe that rheumatism, asthma and
certain skin diseases all have an immuno-pharmacological basis.
Lonchocarpus cyanescens (Schum. & Thonn.) Benth. syn. (Robinia cyanescens

Schum. & Thonn., Philenoptera cyanescens (Schum. & Thonn.) Roberty)
FABACEAE
West African wild indigo, Indigo vine
The leaves are applied as a poultice to ulcers of the foot, etc. or as a dressing for skin
diseases. The bark and root are a remedy for jaundice and are used as a general tonic
(Dalziel, 1937). A decoction of the bark with native natron is, in certain districts, a
treatment for abdominal troubles, with flatulence in horses. The leaf decoction is
also used for the treatment of venereal disease and semen insufficiency (Ainslie,
1937).
The fresh leaves of L. cyanescens contain 0.08-0.3% of indigo, yielding 43% of
indigotin. The dried leaves can yield as much as 56% of indigotin (Dalziel, 1937).
From the chloroform extract of the roots, glycyrrhetinic acid, rotenone and
lonchoterpene have been isolated, and from the methyl alcohol extract oleanolic acid
and ursolic acid have been isolated. Four unidentified minor compounds have also
been reported from these extracts (Iwu and Ohiri, 1980). In the related Nigerian
LonchocarpuslaxiflorusGuill. & Perr., isoflavans(laxiflorinandlonchoflavan)and
pterocarpans have been reported (Pelter and Amenechi, 1969). Glycyrrhetinic acid
(also known as glycyrrhetic acid) is a pentacyclic terpene. It was first obtained by
hydrolysis of glycyrrhizin (or glycyrrhizic acid) from Glycyrrhiza glabra, which
yielded two molecules of glucoronic acid and one of glycyrrhetic acid (Bombardelli
et al., 1979).
Chloroform and methyl alcohol extracts of L. cyanescens roots reduced carrageenan-
induced rat paw oedema and adjuvant (Mycobacterium butyricum-induced) polyar-
thritis in rats. Daily doses of 100 and 200 mg/kg of the extracts partially inhibited
primary and secondary lesions of the rat hind paw and also reduced both body weight
and arthritic symptoms. In combination with phenylbutazone both extracts
alleviated all symptoms of polyarthritis in rats (Iwu and Ohiri, 1980). Glycyrrhetic
acid and some derivatives have been found to have an anti-arthritic activity similar
to that of hydrocortisone (Kraus, 1960; Parmar et al., 1964; Tangri et al., 1965).
(Linnaeus (1707-1778) himself mentions the use of Glycyrrhiza for rheumatism).
Numerous papers deal with the biochemical basis of the anti-inflammatory
properties of glycyrrhizin and were summarized in a comprehensive review by
Gibson (1978). It is generally concluded that glycyrrhizin has an aldosterone effect
in the body, causing retention of sodium ions and a plasma depletion of potassium
ions. Glycyrrhizin appears to stimulate the adrenal cortex directly increasing the
production of mineral corticoids, glucocorticoids and adrenal androgens. In ad-
dition, it inhibits the inactivation of corticoids in the liver and kidneys. These two
effects result in a continuous and elevated plasma level of corticoids (Matsuda et al.,
203
1962). Glycyrrhizin has also been found to enhance the immuno-depressive action of
cortisone and to inhibit the action of cortisone on the thymus and on liver glycogen
deposition (Kumigai, 1969; Kumigai et al., 1967a, b, c).
Glycyrrhizin and glycyrrhetic acid are also active against coughs and peptic ulcers
and have given good results in the treatment of rheumatic thrombophlebitis
(Kerharo and Adam, 1974, p. 440). The effect of glycyrrhizin in the treatment of
peptic ulcer cannot be completely explained by the anti-inflammatory action, since
the deglycyrrhinated drug is of considerable value in the treatment of ulcers
(Brodgen et al., 1974; Gibson, 1978). The anti-arthritic and anti-inflammatory
effects have also been attributed to a reduction in the activities of serum-glutamin-
oxaloacetic acid transaminase and serum-glutamic-pyruvic transaminase (Parmar et
al., 1964), and to an uncoupling of oxidative phosphorylation (Whitehouse et al.,
1967).
Another West African plant which produces glycyrrhizin, and which is used for
its commercial extraction, is Abrus precatorius (5-10% in the leaves, 1.5% in the
roots).
Terminalia ivorensis A. Chev. COMBRETACEAE

Satin wood, shingle wood
Powdered bark and bark infusions are much used in local medicine for the dressing
of wounds. They are also used in the treatment of arthritic conditions and piles and
as a diuretic (Ainslie, 1937; Dalziel, 1937). Anti-inflammatory properties have also
been reported for the related T. avicennoides (see CV).
From the chloroform and methanol extracts of the stembark, terminolic acid, ellagic
acid, sericic acid, quercetin, /3-glycerrhetinic acid and 2-8 hydroxy 18of-glycyr-
rhetinic acid have been isolated (Bombardelli et al., 1979; Iwu and Anyanwu,
1982b). The wood also contains /3-sitosterol, terminolic acid and tri- and tetra-
methyl ellagic acid and laxiflorin and sitosteryl palmitate were reported to be present
in the stembark of most Nigerian Terminalia spp. (Ekong and Idemudia, 1967;
Idemudia and Ekong, 1970).
Extracts of the stembark with different solvents (chloroform and methanol giving
the most active extracts) inhibited carrageenan-induced pedal oedema and adjuvant-
induced polyarthritis (by Rosenthale method) in the rat. Daily administration of
100-300 mg/kg of the extracts reduced primary and secondary lesions of the rat's
hind paws with concomitant reduction of body weight and reduction of the arthritic
symptoms. The chloroform extract showed an activity comparable to that of
phenylbutazone and in combination-therapy with this (100 mg/kg of each) has an
activity almost equivalent to that of indomethacin. The extracts also effectively
checked the diarrhoeas produced by arachidonic acid and castor oil. This action is
related to the ability of anti-inflammatory drugs to interfere in the synthesis of the
prostaglandins E2 and F 2 ; this in turn reduces the inflammation associated with the
prostaglandins (Awouters et al., 1978; Iwu and Anyanwu, 1982a). The authors
conclude that the results lend support to the use of Terminalia ivorensis in the
treatment of arthritis and other inflammatory conditions.
204
The antiphlogistic action of /3-glycyrrhetic acid is well known (see Lonchocarpus,

above) and the anti-inflammatory action of Terminalia ivorensis could, in the view of
Iwu and Anyanwu (1982a), be due at least in part to this acid and to the presence of
other oleanane derivatives (terminolic acid and lonchoterpene).
Phytolacca dodecandra L'Herit syn. (P. abystinica Hoffm.?)

PHYTOLACCACEAE
Endod, soapberry
This plant has anti-inflammatory as well as molluscicidal properties (I).
C The constituents have been examined in detail and it was found that up to ten
saponins (phytolaccosides) were distributed in all tissues of Phytolacca spp.
(P. americana and P. esculenta). Poly phenols have been isolated from the seeds
(Woo and Kang, 1978). The saponins contained glucose as a sugar component
except for phytolaccoside A, which contained D-xylose. The genins were found to
be: phytolaccagenic acid, phytolaccagenin, jaligonic acid, and esculentic acid in
P. americana and P. esculenta (Woo et al., 1976). In P. dodecandra the presence of
the genins oleanolic acid and bayogenin had been reported by Powell and Whalley
(1969).
P A water-insoluble saponin fraction, in doses of 30-50 mg/kg in rats, gave a 50%
inhibition of carrageenan-induced paw oedema. The LD 50 of the crude saponins was
181 mg/kg in mice and 208 mg/kg in rats (Woo et al., 1976). Investigation of the
anti-inflammatory activity of the saponins and of phytolaccagenin from the roots of
P. americana in rats and mice showed that oral administration required six times the
dose needed in intraperitoneal injection. The anti-exudative and anti-granulomatous
properties were eight times higher than those of hydrocortisone, but in higher doses
(160 mg/kg) the saponin produced severe thymolysis in rats (Woo and Shin, 1976).
Phytolaccoside B (1) and Phytolaccoside E (2) administered intravenously to rats
inhibited exudate formation after sponge pellet and carrageenan-induced oedemas.
The haemolytic activity of (1) was greater than that of (2). The LD 50 doses for (1) in
mice and rats were respectively, 4.5 and 10.8 mg/kg, and for (2) they were 23.6 and
42.3 mg/kg, respectively. Toxic and anti-inflammatory effects of the phytolaccosides
were less than those of aescin (Shin et al., 1979).
Plants with alkaloids and amides as active constituents.

A Menispermaceaous alkaloid, tetrandine (in Tiliacora spp.), showed anti-inflam-
matory action when given intramuscularly but was not active when given perorally.
This suggests that it probably acts by stimulation of the adrenals (Yamahara et al.,
1974).
Capsicum frutescens L., C. frutescens var. minimum SOLANACEAE

Cayenne pepper, African pepper, paprika, piment enrage
C. annuum L.
Capsicum pepper, piment doux
L The fruits of these plants are popular spices and are used medicinally as rubefacients
205
and counter-irritants. The small-fruited varieties are the chillies; when crushed and
powdered, the fruits produce the condiment known as Cayenne pepper, which is
sold commercially. C. annuum has bigger, less pungent fruits than C. frutescens.
The pungency is due to the presence of a volatile phenolic compound, capsaicin,
which is closely related to vanillin as it is a vanillylamide of 8-nonene-6 carboxylic
acid (it has been called capsicin by some authors). C. annuum contains 0.1%, C.
frutescens about 0.5% of capsaicin, but the figure varies-it may exceed 1% in both
species and be as little as a tenth of this in some varieties. Furthermore, the presence
of a steroid saponin, capsicidin, has been reported (Gal, 1964, 1967). The fruits are
a source of vitamin C (7.3 mg/kg and 12 mg/kg for C. frutescens and C. annuum,
respectively) and are also relatively rich in vitamin A and mineral elements. Fifteen
to thirty per cent of the seed content has been extracted in the form of an oil rich in
triolein.
The counter-irritant and carminative actions are due to capsaicin, which, according
to Molnar (1965), acts as a toxic stimulant of the receptors involved in the circulatory
and respiratory reflexes. In small doses it increases intestinal peristalsis and the
production of gastric acid but higher doses inhibit these effects.
Capsaicin is mainly used in local applications as a revulsive in rheumatism,
lumbago, neuralgia, respiratory tract diseases, chilblains, etc., in the form of
impregnated cotton-wool (Paris and Moyse (1971) Vol. Ill, p. 200). Capsicidin has
a definite antibiotic action on certain microorganisms and on Saccharomyces cerevisiae
(Gal, 1964).
Cryptolepis sanguinolenta (Lindl.) Schltr. PERIPLOCACEAE

Cryptolepine, an alkaloid obtained from the roots, among other pharmacological
properties (see CV and I), inhibited carrageenan-induced oedema of the rat hind paw
in doses of 1, 5, 10 and 20 mg/kg. The effect was dose-related but was much less
potent than that of aspirin or indomethacin. In doses of 1-20 /JLg/m\ in the bath fluid
cryptolepine did not inhibit prostaglandin synthesis in the isolated lizard lung, but
it antagonized prostaglandin E2 and not 5-hydroxytryptamine on a perfused isolated
stomach strip of the rat. It also antagonized the action of histamine and of
acetylcholine on the isolated guinea pig ileum. These observations seem to indicate
that the inhibitory effect is probably receptor-mediated. Cryptolepine has been
shown to be only slightly less potent than phentolamine in blocking adrenoreceptor
stimulation (Noamesi and Bamgbose, 1980; Bamgbose and Noamesi, 1981). Further
tests revealed that cryptolepine has preferential presynaptic a-adrenoreceptor
blocking action (Noamesi and Bamgbose, 1982).

F. senegalensis Chev.) RUTACEAE
Prickly ash, candlewood, toothache bark
The rootbark of this plant, which also has cardiovascular and anti-infectious
properties (see Chapters 2 and 3), contains, amongst other constituents, fagaramide,
which has been shown to reduce inflammation. Fagaramide has been shown to
206
reduce carrageenan-induced paw oedema in rats but is approximately twenty times

less potent than indomethacin. The acute inflammatory reaction is characterized by
a sequential release of mediators: histamine, 5-hydroxytryptamine, bradykinin and
prostaglandin (Di Rosa et al., 1971). The prostaglandin phase of acute experimental
inflammation is usually assumed to cover events taking place from about one hour
after carrageenan injection. This phase was modified by fagaramide and it was noted
that in vitro fagaramide inhibited prostaglandin synthesis in a dose-dependent
manner but had no effect on prostaglandin E induced potentiation of carrageenan-
oedema in indomethacin-treated rats (Oriowo, 1982). Oriowo (1982) suggests that at
least part of the anti-inflammatory effect of fagaramide is attributable to inhibition
of prostaglandin synthesis.
Plants withflavonosidesas active constituents.

Afraegle paniculata (Schum. & Thonn.) Engl. syn. (Citrus paniculata Schum. &
Thonn., Balsamocitruspaniculata (Schum. & Thonn.) Swingle, A. barteri Hook.)
RUTACEAE
L In Lagos an agbo infusion is made of the fruit and leaves and sometimes the bark of
A. paniculata, to be taken both internally and as a wash in rheumatic conditions
(Dalziel, 1937). Sometimes Clausena anisata is added to the infusion (Irvine, 1961).
C The coumarins scoparone, imperatorin and xanthoxyletin have been isolated from
the stembark (Adesina and Ette, 1982). The fruit contains imperatorin, y-sitosterol
and another coumarin, xanthotoxin (Quartey, 1963). In addition, free aliphatic acids
and a triacid triglyceride have been isolated from the bark and fruits (Adjangba etal.,
1974).
The dried seeds yield 46% lipids; besides 34% oleic acid, stearic, palmitic,
linoleic, linolenic and palmitoleic acids have been reported (Busson, 1965), and a
mucilage of the fruit produced through partial hydrolysis 6-O-/3-D-glucuronosyl
D-galactose (Torto, 1961). The leaves contain 47.3% of glucides, 27.1% of protides
and mineral elements with a predominance of calcium.
P The three coumarins xanthotoxin, xanthotoxol and imperatorin isolated from A.
paniculata were tested for their anti-inflammatory properties following oral adminis-
tration of 100 mg/kg to mice. Xanthotoxin had some activity but the other two had
none. The oral LD 50 of xanthotoxin was more than 4000 mg/kg in rats and over 1000
mg/kg in mice (Adjangba etal., 1975).
Scoparone was found to have anticonvulsant properties while the other two
coumarins found in the stembark proved to be mildly sedative and anticonvulsant
(coumarin itself is a mild sedative). The structurally related compounds scopoletin
and angelicin have been reported to possess anticonvulsant properties (Adesina and
Ette, 1982).
Arnebia hispidissima (Sieber and Lehm) DC. syn. (Lithospermum hispidissimum

Sieber ex Lehm, A. asperrima (Del.) Hutch. & Dalz.,Anchusa asperrima Del.)
BORAGINACEAE
L A red or purple dye is obtained from the root.
207
Vitexin (8/3-D-glucopyranosyl-apigenin) was isolated from the flowers of A. hispidis-

sima and Ochrocarpus longifolius L.
Vitexin showed potent hypotensive, anti-inflammatory and non-specific antispas-
modic properties. The hypotensive effect was attributed to its ganglion-blocking
properties and the anti-inflammatory effects to its antihistamine, anti-bradykinin
and anti-serotonin properties (Prabhakar etal., 1981).
Vitexin has also been reported to be present in the leaves of Lophira lanceolata van
Tiegh. ex Keay (Jacquemain, 1971), which are used in Senegal as an antitussive
(whilst the stembark is said to cure oedemas) (Kerharo and Adam, 1974, p. 614).
Vitexin heterosides have also been noted in the leaves of Combretum micranthum
(JentschtfflZ.,1962).
Calophyllum inophyllum L. GUTTIFERAE

Mesuaferrea L.
Both introduced into West Africa
In its country of origin (South India) the oil of the seeds of Calophyllum is specifically
used to treat skin diseases and is also applied topically in cases of rheumatism. The
gum and the juice are said to be purgative and the bark astringent in patients with
internal haemorrhage. The leaves are used as a fish poison.
From the leaves of C. inophyllum, friedelin and triterpenes of the friedelin group,
namely canophyllal, canophyllol and canophyllic acid (Govindachari et al., 1967),
and from the heartwood xanthones (mesuaxanthone B and calophyllin B) have been
isolated (Govindachari et al., 1968). A number of 4-phenylcoumarin derivatives
have successfully been isolated from the seeds (Mitra, 1957a; Farnsworth and
Cordell, 1976, p. 424); they include calophyllolide, inophyllolide and calophyllic
acid. In plants collected in India all three of these compounds were present, while in
Indochina and Tahiti only calophyllic acid has been found (Polonsky, 1957).
Furthermore, inophyllic acid (Mitra, 1957b) and two more 4-phenylcoumarins,
ponnalide (Adinarayana and Seshadri, 1965) and calaustrin (Bhusan et aL, 1975)
have been reported.
The pharmacological properties of calophyllolide have been examined by Arora etal.
(1962), who reported that in the isolated perfused rabbit heart it decreased the
amplitude of contraction but increased coronary flow. It suppressed ventricular
ectopic tachycardia resulting from acute myocardial infarction in dogs as effectively
as quinidine and had vasoconstrictive action on the peripheral vessels. Its effective-
ness as an anticoagulant puts it between dicoumarol and tromexan for this purpose
(Arora et al., 1962). Also, Saxena et al. (1982) found calophyllolide to be effective in
reducing the increased capillary permeability induced in mice by various chemical
mediators involved in inflammation processes, namely histamine, 5-hydroxytryp-
tamine and bradykinin. Pretreatment of the mice with calophyllolide afforded
significant protection against the inflammation induced by these mediators. When
evaluated against carrageenan-induced rat pedal oedema, at 40 mg/kg given intra-
peritoneally, calophyllide and inophyllide reduce oedema by 60.7% and 29.8%,
respectively. In this study hydrocortisone given intraperitoneally at a dose of 10
208
mg/kg reduced the inflammation by 44% (Chaturvedi et al., 1974). The safety
margin of calophyllolide is very similar to that of oxyphenbutazone (21.4 mg/kg and
25 mg/kg, respectively) (Bhalla et al., 1980), which would warrant clinical studies of
different inflammatory diseases with this compound (Saxena et al., 1982).
The xanthones of C. inophyllum and M. ferrea, namely dehydrocycloguanandin,
calophyllin B, jacareubin, 6-deoxyjacareubin and mesuaxanthone, produced in
mice and rats various degrees of CNS depression (sedation, decreased spontaneous
motor activity, loss of muscle tone, potentiation of barbitone sleeping time and ether
anaesthesia). None had analgesic, antipyretic or anticonvulsant activities (Chatur-
vedi et al., 1974). The xanthones displayed, both by intraperitoneal and oral routes,
anti-inflammatory activity in rats in carrageenan-induced hind paw oedema, cotton-
pellet granuloma and granuloma pouch techniques both in normal and in adrenalec-
tomized rats. The xanthones did not have any mast cell membrane effect and did not
alter the prothrombin time in rats (Gopalakrishnan et al., 1980).
Plants with other active constituents.
Curcuma domestica Valeton syn. (C. longa L.) ZINGIBERACEAE

Turmeric
Next to the anti-infectious and choleretic activities of the root already mentioned (I),
the volatile oil obtained from the rhizome of C. longa has been noted to have
significant anti-inflammatory properties in rats, comparable to those of hydrocorti-
sone acetate and phenylbutazone. In oral doses of 0.5-1 mg/kg, curcumin inhibited
carrageenan-induced oedema in rats and mice as well as formalin-induced acute
oedema in mice and subacute arthritis and cotton pellet-induced granuloma forma-
tion in rats (Arora et al., 1971; Srimal and Dhawan, 1973). Curcuma oil also strongly
reduced the histamine content of the skin of the rat (by 50% as compared to a 42%
reduction by hydrocortisone). This antihistamine effect is believed to explain the
protective action of the volatile oil (0.01 ml/kg) in early inflammation lesions in
adjuvant arthritis in rats. The inhibition of the late arthritis changes may be due to
the activation of the adreno-hypophyseal axis (Chandra and Gupta, 1972). The
volatile oil was also found to act on the proteases responsible for the acute
inflammatory process as it was found to inhibit trypsin as well as hyaluronidases
(Tripathiâ/., 1973).
In addition to the anti-inflammatory properties, aqueous extracts of the rhizome
of C. domestica had a 100% antifertility action in albino rats at a dose of 100 mg/kg
body weight. The petroleum ether extract had an 80% antifertility effect and also
caused resorption of the implants (Garg, 1971). Furthermore, sodium curcuminate
has long been known as an active choleretic (Ramprasad and Sirsi, 1956). Curcumol
and curdione are reported to be active in the early stage of cervical cancer (Xaio,
1983).
209
Salvadora persica L. SALVADORACEAE

Salt bush or toothbrush tree
The twigs and roots are used as a toothbrush. In Senegal the roots are mainly used as
a diuretic and are sometimes used associated with kinkeliba leaves for blackwater
fever, rheumatism and venereal diseases (Kerharo, 1968). In the Eastern Sudan the
bark is pulverized and made into a paste with water, which is applied to the head in
cases of serious febrile diseases. Dried leaves are taken for flatulent dyspepsias
(Dalziel, 1937).
The leaves and bark contain the alkaloid trimethylamine and the leaves and seeds
yield about 45% of a fatty oil (composed of ±20% lauric acid, ±55% myristic acid
and ±19% of palmitic acid (Gunde and Hilditch, 1939)), which is used for making
candles and which contains a small proportion of volatile oil (mainly benzyl-mustard-
oil) (Wehmer, 1935). From an extract of the roots, /3-sitosterol and elemental and
monoclinic sulphur were isolated (Ezmirly et al., 1979) and from the leaves
polyphenols (quercetin and caffeic and ferulic acids) were isolated. In the rootbark,
the presence of small amounts of tannins and saponins has also been reported
(Farooqi and Srivastava, 1969).
Extracts of S. persica root have shown antibacterial, weak anti-inflammatory and
mild hypoglycaemic properties (Ezmirly et al., 1979).
Ipomoeapurpurea(L.)Roth. CONVOLVULACEAE
Ipomoea pes-caprae (L.) Sweet subsp. brasiliensis (L.) Oostr. syn. Convolvulus
brasiliensis L., /. pes-caprae Roth.) (Fig. 5.3)
Goat's foot convolvulus
Fig. 5.3.1pomeapes-caprae (L.) Sweet.

210
/ . pes-caprae is a good sandbinder near the sea. The starchy root is a common Indian
drug used for rheumatism, dropsy and colic (Dalziel, 1937) and the juice is given as
a diuretic in cases of oedema whilst the bruised leaves are applied to the swelling
(Chopra**al.,1956, p. 142).
The whole plant contains 7-8% of total resin, 0.05% of an essential oil, triaconthane,
pentatriaconthane, a sterol, behenic acid and melissic, butyric and myristic acids
(Cwalina and Jenkins, 1938; Dawalkar and Dawalkar, 1960). The roots contain
glycorrhetins similar to those of other Ipomoea resins (Hegnauer, 1962-68, Vol. Ill,
p. 551;Shellard, 1962).
In Indonesia the plant is used against inflammation and cancer. An antihistamine
action was reported for this plant by Wasuwat (1970), who noted that a volatile
fraction of 6 x 10~5 M antagonized the contractile effect of histamine (2 x 10~6 M)
on the guinea pig ileum in a similar fashion to benadryl or antistine (1 x 10~6 M). It
also antagonized the contractile effect of jellyfish as effectively as did these antihis-
tamines. /. purpurea (L.) Roth, which is naturalized in West Africa, produced 60%
inhibition, in doses of 100 mg/kg, in carrageenan-induced rat paw oedema when the
dose was repeated at 150- and 30-min intervals before carrageenan administration,
when tested on Indonesian plants (Benoit el aL, 1976).
Table 5.1. Additional anti-inflammatory plants
The abbreviations used are as follows: adj. arthr., adjuvant arthritis; cam, carrageenan; cotton p. gran., cotton pellet induced granuloma; crot. i., croton oil
induced; equiv. = equivalent; form., formalin; i.r.p.o., induced rat paw oedema; i.p., intraperitoneally; i.v., intravenously; p.o., perorally; s.c, subcutaneously
Plant
Family Part used Active constituent(s) Action/acts on Pharmacological tests Comments References
Allium sativum, A. cepa Bulb Alliin Rheumatism, Allicin immunodepressive, Ayoub and Svendsen
Liliaceae Allicin hypoglycaemic also hypotensive and (1981)
antibiotic Xaio(1983)
Alstonia boonei syn. (A. Bark Triterpenoids External application Dalziel(1937)
congensis) in rheumatism Esdom(1961)
Apocynaceae Hager's Handbuch
(1967-80, Vol. II,
r\ 1737^
p . LZ.D 1)
A nthocleista procera Leaves Gentianine (partly formed Anti-histamine, 90 mg/kg given i.p. protects Preventive protection Chen-Yuetal. (1959)
Loganiaceae from precursor anti-inflammatory, guinea pig against greater than that of Keng-Tao Liu et al.
(also see Chapter 2) swertiamaroside) also analgesic histamine aerosol and chloroquine or (1959)
prevents albumin- or cortisone La vie and
formol-i.r.p.o. gentianine Taylor-Smith
= immunopotentiating (1963)
Atractylis aristata Rhizomes Diterpene carboxyl- Anti-inflammatory Related species Bombardelliefa/.
Compositae atractyloside Inhibit carr. i.r.p.o. (1979)
Azadirachta indica Seed oil Nimbidin Anti-arthritic, anti- 40 mg/kg inhibits carr. and Equiv. to 100 mg/kg Pillayera/. (1978)
Meliaceae (triterpenoid) inflammatory also kaolin i.r.p.o. form, arthr. phenylbutazone Okpaniyi and
antipyretic and and croton oil gran, in and to prednisolone Ezeukwu(1981)
anti-ulcer action rats. Low oral toxicity (13 Pillay and
g/kg) in mice. Important Santhakumari
anti-gastric ulcer effect (1981)
{Table continued)
Plant
Boerhavia diffusa Roots Flavones(quercetin, Anti-inflammatory, 4 mg/100 g of aqueous and of In arthritic animals Chopra tf al. (1956)
B. punamava (name given to quercitrin), oleanolic also in internal acetone extract inhibits aqueous extract Subramanian and
white-flowered variety in glycoside, /3-sitosterol inflammations, carr. i.r.p.o. andcarr. i. inhibits serum Ramakrishnan
India) (also contains an oedemas and gran, pouch arthritis aminotransferase (1965)
Nyctaginaceae alkaloid) asthma (diuretic) like hydrocortisone Subramayan et al.
(1965)
1971)
Misra and Tiwari
(1971)
Singh and Udupa
(1972a, b,c)
Srivasta etal.
(1972)
Mudgal(1975)
Cannabis saliva Resin A -tetrahydrocannabinol Anti-inflammatory Various rat paw oedema Like hydrocortisone Sofiaera/.(1974)
Cannabinaceae models and aspirin Biswas etal. (1975a)
Canscora decussata Plant Mangiferin (xanthone Anti-inflammatory, Ghosal era/. (1971)
Gentianaceae heteroside) anti-arthritic, Ghosal and Biswas
depresses CNS (1979)
Shankaranarayan et
al. (1979)
Capparis decidua Seeds Glucocapparine Rheumatism, Gaind and Junega
(1970)
Capparidaceae revulsive Ayoub and Svendsen
(1981)
Carica papaya Seeds, Tropaeaoline, papain Anti-inflammatory Rigaudetal. (1956)
Caricaceae latex Yarington and
Bestler(1964)
Citrus nobilis Rootbark Suberosin, xanthyletin Anti-inflammatory Also antipyretic Paris and Delaveau
Rutaceae (crenulatin, suberenol) and antihistamine (1977)
(coumarins) In Traditional Reisch era/. (1980)
Medicine,
antirheumatic
"Jrateva religiosa Bark, Lupeol (triterpene), Anti-inflammatory Inhibits carr. and histamine Chakravarti et al.
Dapparidaceae seeds glucocapparine ? revulsive induced inflammation in (1959)
rats, and early and delayed
inflammatory lesions in Biswas etal. (1975b)
form, i.r.p.o.
Dalbergia sissooc. Wood, Dalbergichromene Anti-inflammatory, Mukerjeeefa/.
Fabaceae stem neoflavonoids anti-arthritic (1971)
For Indian spp.:
Kishore and Tripathi
(1966)
Singh and
Chaturvedi(1966)
Tripathi and Kishore
(1967)
HyeandGafur(1975)
Destnodiwn gangeticum Roots Aqueous extracts, tertiary Anti-inflammatory, Non-toxic in toxicity tests Ghosal and Baner jee
Fabaceae phenylethylamines, also also antimicrobial (1971)
also hypaphorine Prema(1968)
alkaloid Ghosal and
Bhattacharya
(1972)
Gymnema sylvestre Leaves Potassium salts of 43% inhibition in p.o. in 2 doses of 100 mg/kga Rao etal. (1972)
Asclepiadaceae gymnemic acids carr.r.p.o. (plants collected in India) Benoitera/. (1976)
(gymnagenin = hexa-
hydroxy A12-oleanene
Gynandropsis gynandra Leaves Glucocapparine Counter-irritant Arthritis Dharetal. (1968)
Capparidaceae
Haematoxylum Wood Brasilin, haematoxylin Both substances anti- 10 mg/kg perorally in carr. Brasilin, in doses of Hikinoera/. (1977)
campechianum inflammatory i.r.p.o. and fertility egg 100 mg/kg in the
(introduced) test r.p.o. and fertility
Caesalpiniaceae egg tests, is more
active than berber-
ine hydrochloride
In the cotton
p. gran, test
activity of
brasilin is
equivalent to that
ofberberine
hydrochloride
Hibiscus vitifolius Petals Gossypin (bioflavonoid) Antiflammatory Parmarâ/. (1978)
Malvaceae
(Table continued)
Plant
Leptadenia pyrotechnica 2 triterpenoids, steroid Gout, rheumatism Iyer et al. (1974)

Asclepiadaceae glycosides (5-tri- Manavalan and
triaconten-17-one, Mithal(1980)
sitosterol, stigmasterol,
18-pentatriacontanol)
Moringa oleifera syn. Roots, Glucotropaeoline External counter- Chopra etal. (1956)
(M. pterygosperma) seed oil (benzylisothiocyanate irritant (oil) Dalziel(1937)
Moringaceae derivatives) Kerharo and Adam
(1974,p.599)
Securidaca longepedunculata Roots 4% methylsalicylate Revulsive, Also anticonvulsive Dalziel(1937)
Polygalaceae saponin (oleanolic antitussive Kerharo (1968)
glycoside) Odebiji(1978)
Tetrapleura tetraptera Bark, Saponosides, oleanolic Lumbago, Also anticonvulsive Odutola and Ekong
Mimosaceae Roots triglycoside antitussive (1968)
Adesina and
Sofowora(1979)
Vernonia colorata Flowers, Vernolid, sesquiterpenic Inhibition of Vernolid is also cytostatic Satoda and Yoshi
Compositae bark lactone, glycosides carr.i.r.p.o. (100 mg/kg) given twice" (1962)
inflowers11%, (plants from Nigeria) Benoitetal. (1976)
in bark 19%
Xylopia aethiopica Dun. Fruit Kauren-diterpenes Anti-inflammatory Ekong and Ogan
Annonaceae (1968)
Ekong et al. (1969)
Boakaiji Yiadom et
al. (1977)
"Second dose given 2 h after first dose.

Sex hormones and thyroid hormones
I Sex hormones
(a) Female sex hormones

Oestrogens are the hormones concerned with the maturation of the female
genital tract, the development of the secondary sexual characteristics and bone
formation. The main oestrogens, oestradiol and oestrone, are secreted by the theca
interna and appear in the fluid of the Graafian Follicles. Oestrogens are also secreted
by the placenta and to a much lesser degree by the adrenal cortex. They are rapidly
metabolized in the liver.
Progesterone is the hormone concerned with the maintenance of pregnancy. It is
secreted by the corpus luteum and acts only on tissues formerly sensitized by
oestrogens. It inhibits ovulation during pregnancy, depresses the action of oestro-
gens and produces further development of the breasts. It also plays a role in the
development of the placenta and depresses uterine contractility.
The production of steroid hormones is controlled by the pituitary gonadotrophins
(follicle-stimulating and luteinizing hormones). In large doses oestrogens can
depress the gonadotrophic and lactogenic activities of the anterior pituitary gland.
Because of their rapid metabolism by the liver, oral administration of the natural
oestrogens is less effective than parenteral administration, with the possible excep-
tion of oestriol, which is claimed to be as potent when given orally as when given by
injection.
The oestrogens are used to treat menopausal disturbances and cases of dysmenor-
rhoea and menorrhagia. Progesterone is used chiefly in the treatment of functional
uterine haemorrhagia. Both oestrogens and progesterone are used in the contracep-
tive pill.
Plants with oestrogenic constituents

The first plant constituents capable of replacing oestrone in hormone
deficiency were found to be chemically identical with the animal hormone and were
reported as early as 1933 (Butenandt and Jacobi, 1933; Skarzynski, 1933). It was,
however, not until thirty years later that the oestrogenic substances in plants were
216
investigated further. A review of the steroid oestrogens in higher plants was

published by Heftman in 1967.
Other plant substances, although chemically not identical to them, were sub-
sequently found to be able to replace the biological functions of the hormones (Shutt,
1976). Bennets and his coworkers (1951) noted the infertility observed in sheep
which grazed exclusively on clover for a certain length of time in Australia. A
compound isolated from clover was found to be oestrogenic (Biggers and Curnow,
1954) and was identified as genisteine, an isoflavine. Failure of sperm transport was
later found to be the cause of the infertility of the ewes (Lightfoot et al., 1967).
Subsequently, other isoflavones with oestrogenic activity were found in forage and
other plants (Shutt, 1976; Adams, 1977; Livingstone, 1978). Also reported to be
present in plants was another group of chemical compounds, the coumestans
(skeletal structure 6H benzofuran 3-2-c-benzopyran-6-one), which have a higher
oestrogenic activity than the isoflavones. A striking similarity of the skeletal
structures of the isoflavones and coumestans with that of the synthetic oestrogen
stilboestrol was noted by Farnsworth et al. (1975b). Of the constituents tested by
these authors, the natural steroid oestrogens were found to be the most active,
followed by the coumestans and then the isoflavones. It was further shown that
daidzin (in Pueraria thunbergiana (Sieb. & Zucc.) Benth.) was the most active
isoflavonoid derivative in the mouse uterine weight assay. Biochanin (in Dalbergia
sissoo and spp. and in Lupinus tassilicus Maire) and genisteine (in Trifolium
baccarini Chiov.) were of lesser but approximately equal activity (Farnsworth et al.,
1975a).
In search of plants with fertility regulating action, Farnsworth et al. (1975b) have
listed the plants containing oestrone and oestriol. Some of these are found in West
Africa: the date palm Phoenix dactylifera; the oil palm Elaeis guineensis; rice, Oryza
sativa L.; wheat, Triticum aestivum L. and vegetable beans, Phaeseolus vulgaris L.
Phoenix dactylifera L. PALMAE

In Northern Nigeria dates, together with bran and the seeds oiSterculia tomentosa,
are given to young heifers long before they are mature in order to cause them to
become prolific breeders (Dalziel, 1937, p. 509). The pollen grains of the date palm,
which is dioecious, are reported to act like gonadotrophins (El Ridi, 1960). Oestrone
has been reported to be present in the kernels (Hassan and El Waffa, 1947; Heftman
et al., 1966; Paris and Moyse, 1967, Vol. II, p. 10), which also contain 5% protides
and 8% lipids.
Elaeis guineensis Jacq. PALMAE

Disparity in results obtained by different investigators when analysing palm kernels
for oestrone content can be explained by the fact that different varieties of oil palm
produce fruits with a varying thickness of mesocarp and size of kernel and extremes
of being shell-less and kernel-less. The oestrone content of certain varieties could be
confirmed (Butenandt and Jacobi, 1933; Bradbury and White, 1951).
217
Triticum aestivum L. syn. (Triticum sativum Lam. (wheat) GRAMINEAE

Oryza sativa L. (rice)
The seeds of these and other cereals mainly contain starches but the embryo (germ)
at the base of the grain contains 10-20% lipids compared to the 1-2% in the albumen.
The lipid fraction contains the sterols and the tocopherols (vitamin E). Thus
wheatgerm-oil contains 85% of glycerides of non-saturated fatty acids, sterols and
vitamins (mainly vitamin E). The oil is administered in cases of sterility in women
and is also used in veterinary medicine in epizootic abortions.
It is interesting to note that vitamin E (a-tocopherol mainly) is found in the germs
of cereals and also in different oils (palm oil, castor-oil (1%) and olive oil (Langlois,
1941)) and that deficiency of tocopherols is characterized by gestation troubles in
females and testicular modifications in males (vitamin E is known to be a fertility
factor (Bacharach, 1940)). Oryza sativa c. and Avena sativa c , both containing
oestrone (Farnsworth et at., 1975 b), have been shown to induce ovulation (Heftman,
1967; Paris and Moyse, 1967, Vol. II, p. 26).
Phaseolus vulgaris L. FAB ACE AE

The vegetable bean, also cultivated in some parts of West Africa, contains oestrone,
oestriol and 17a-oestradiol (Kopcewicz, 1971). It contains more proteins (20-25%)
than the cereals (8-15%) and only 1-7% lipids, including sterols and vitamin E, but
has 61.6% glucides (Paris and Moyse, 1971, Vol. Ill, p. 201).
Arachis hypogeae L. FAB ACE AE

Another very important food plant, the groundnut, already mentioned in Chapter 2
(CV) contains an oestrogenic factor and a goitrogenic compound. The plant is
treated in more detail below under Thyroid hormones.
Groundnuts contain an average of 42.8% of lipids and 26.2% of proteins and small
quantities of vitamins, including vitamin E (Adrian and Jacquot, 1968).
Medicago sativa L. FAB ACE AE

Also cultivated as a food plant, M. sativa contains coumestrol and is rich in vitamins;
mainly vitamin E is reported (Paris and Moyse, 1971, Vol. Ill, p. 391). Vitamin E is
considered to be an antisterility factor (Bacharach, 1940). The activity of these
oestrogenic food plants seems to be mostly concentrated in the germs and kernels.
Other sources of oestrogens in West Africa might be the following plants.
Cyperus rotundus L. CYPERACEAE

The essential oil from the tubers shows oestrogenic activity. Fractionation of the oil
produces an active hydrocarbon, cyperene I, which has a slightly less potent
oestrogenic action than the oil and which also has an antispasmodic action on the
uterus (Indira et al., 1956a, b; Abu-Mustafa et al., 1960) (see also Anti-inflammatory
plants (Chapter 5)).
218
Holarrhena floribunda (Don.) Dur. & Schinz. APOCYNACEAE

A root decoction of Holarrhena is prescribed for sterility (Kerharo and Adam, 1974).
The roots contain many steroid alkaloids. One of these, holophyllamine has
significant oestrogenic activity (see more details under Plants acting like hormones
of the adrenal cortex (Chapter 5)).
Funtumia africana (Benth.) Stapf APOCYNACEAE

The main alkaloid of the leaves, funtumine, is a 3a derivative of allopregnane with
a ketone function at C-20. It is suggested that it might be of use in the hemisynthesis
of hormones. Funtumine itself antagonizes the effects of oestrogens (see under
Plants acting like hormones of the adrenal cortex (Chapter 5)).
It is only in the last few years that pharmacological and clinical details of the
phyto-oestrogens have been mentioned. Most of the scientific data have been
obtained in connection with the development of new methods of fertility regulation
(Farnsworth et a/., 1975a, b, 1983; Farnsworth and Waller, 1982). This application
of the sex hormones currently represents by far the biggest practical demand. I have
limited the other applications of the hormones to a few examples only.
Phytoandrogens are hardly mentioned in the literature. An androgenic steroid
with an anabolic action in the healing of fractures has been found in Cissus
quadrangularis (see Chapter 3).
(b) Plants in birth control

In order to be able to decide which of the very many species of plants
should be tested for their effectiveness in birth control it has been necessary to
consider the mechanisms by which the constituents exert their effect and to classify
them according to the anatomical sites involved. This has greatly contributed to a
better understanding of the plant oestrogens. Farnsworth et al. (1975a, b) have
therefore enumerated the different antifertility mechanisms in laboratory animals.
These are described briefly below.
The oestrogens are of interest in studies on fertility regulation because they can act
as contraceptives by inhibiting the mid-cycle surge of pituitary gonadotrophin that
is associated with ovulation.
Antifertility mechanisms
The organs on which antifertility agents may act in females are the
hypothalamus, the anterior pituitary, the ovary, the oviduct, the uterus and the
vagina. An antifertility agent can be classified by its action on each of these organs.
The pituitary. The functioning of this organ is under the close control of the
hypothalamus via the follicle-stimulating and luteinizing-hormone releasing factors
219
(Goodman and Gilman, 1980, pp. 1389-92). Therefore, antifertility action at this
level should include: (a) disruption of the normal hormonal functions of the
hypothalamus and/or pituitary, e.g. by oestrogenic steroids and (b) interruption of
the neural pathways to the hypothalamus that control the liberation of gonado-
trophin-releasing factors.
Since the hypothalamus receives contributions from other areas of the brain,
substances having CNS depressant activity and/or effects on neuro-hormonal
transmission could be expected to alter gonadotrophin transmission. And indeed
pentobarbital, morphine, atropine, tranquillizers (reserpine), anaesthetics and
adrenergic (as well as cholinergic) blocking agents have been shown to block the
ovulatory surge of luteinizing hormone in laboratory animals by having inhibitory
effects on the hypothalamus (Smith, 1963).
Studies on laboratory animals such as the rat, mouse, hamster and guinea pig
provide much information but the reproductive cycles of these animals exhibit
species-specific differences as do those of men and primates, and different results
with a given compound are often obtained.
Interference with gonadotrophin secretion may have post-ovulatory antifertility
effects, but the antifertility usefulness of drugs having such effects is questionable
not only because they have other pharmacological actions but also because animals
(e.g. rats) sometimes become coitus-induced ovulators following blockade of their
gonadotrophin surge (Farnsworth etal., 1975a).
In the guinea pig the pituitary can be removed after the third day of gestation
without affecting the pregnancy and hypophysectomized women induced to ovulate
by consecutive administration of follicle-stimulating hormone and human chorionic
gonadotrophin have become pregnant without further gonadotrophin replacement
therapy (Farnsworth et al., 1975a).
The ovary. Substances having antifertility properties may exert their effects at the
ovarian level by inhibiting ovulation and/or steroidogenesis. Oestrogen adminis-
tration early in the luteal phase has been shown, in monkeys and women, to decrease
progesterone secretion and to hasten the onset of menstruation (Knobil, 1973). The
lowering of post-ovulatory plasma progesterone levels may be at least one mechanism
by which post-coitally administered high doses of oestrogen exert their antifertility
effect in women.
The oviduct. Since successful implantation depends on the correct timing in the
menstrual cycle of the arrival of the blastocyst in the uterus, disturbances of tubal
transport may be accompanied by failure of implantation. Accelerated transport of
ova results in a reduction in fertility, either through expulsion of the fertilized ova
from the reproductive tract or through degeneration of fertilized ova that arrive (too
early) in the non-receptive uterus. Either oestrogenic or anti-oestrogenic compounds
may play a role in this inhibition. Anti-oestrogenic compounds are compounds
which inhibit the effects of standard oestrogens such as oestrone, oestriol and
oestradiol. Androgens and progestogens may show this activity and the weak plant
oestrogens coumestrol and genisteine have also been shown to have this inhibitory
220
effect (Folman and Pope, 1966). The anti-oestrogenicity of a compound can be

demonstrated by the blocking of a step in the reproductive cycle that requires
oestrogen.
The uterus. Antifertility agents that prevent ovulation and/or fertilization are
called contraceptive agents whilst those that act after implantation has taken place
are usually called abortifacients. The term 'interceptives' refers to compounds that
act after fertilization has occurred to prevent implantation from taking place. Their
earlier or later administration might render some of them contraceptive or aborti-
facient, respectively.
Inhibition of implantation has been observed with a number of compounds and it
appears possible that non-physiological treatment of the endometrium may impair
fertility in the human. It has been suggested that an excess amount of oestrogen
present in the uterus shortly after ovulation (in mammals) may prematurely sensitize
the uterus so that the latter is in a non-receptive state at the time of arrival
of the blastocyst. Other substances, instilled locally in the uterus, can impair
fertility by affecting the endometrium or by causing physical obstruction of the
lumen.
An abortifacient type of antifertility effect can be produced by compounds that
stimulate uterine contractility. The hormone oxytocin can be used close to term to
induce labour but is effective as an abortifacient if used earlier in a pregnancy.
Prostaglandins, however, are now being widely used for the latter purpose. They
appear to promote myometrial contractility, acting on both contraction and stretch-
ing of the myometrial wall. This produces a decrease in the levels of oestradiol and
progesterone and the resulting endogenous stimulatory mechanism may be
sufficient to complete abortion. If it is not, additional prostaglandin or oxytocin may
be used.
Cervix or vagina. Antifertility activity exerted at the level of the cervix or the
vagina can be based on the production of a cervical mucus that is 'hostile' to sperm
penetration. Some of the spermicidal preparations are based on a trypsin-like
protease (acrosin). Oestrogenic compounds produce vaginal keratinization
(Farnsworthera/., 1975a).
Anovulation has also been observed in a number of cases as a result of inhibition of
hypothalamic-hypophysial function, for example in Rhesus monkeys treated with
reserpine (from Rauvolfia vomitoria) (Bianchi, 1962). But, as mentioned earlier, the
suitability of using plants that act in this non-specific way is questionable because of
the many different hormones that are controlled by this axis, for example the
gonadotrophins (oestrogenic, luteinizing, prolactin, androgenic), thyrotrophin, and
corticotrophin, and the changes in target organ function that result from effects on
these hormones.
It has been reported that contraceptive steroids produce changes in metabolic
processes, for example deterioration in glucose-tolerance tests and an increase in
lipoproteins (Briggs, 1976; Briggs and Briggs, 1981). The authors further note
alterations in plasma proteins and a certain action on the pituitary: basal prolactin
221
and plasma growth hormone are enhanced, and the concentration of thyrotrophin
remains unchanged but adrenocorticotrophin is suppressed. Also, the pattern of
plasma androgen is altered. The levels of plasma cortisol and to a lesser extent of
plasma aldosterone are increased.
Plants having antifertility effects in females

Most of these plants have either anti-implantation, uterine stimulant or
abortifacient action. Bioassays which can be used to evaluate the alleged fertility
regulating effects of the plants include in vitro evaluation using the rat uterus and
confirmation in the 29-day pregnant rabbit for utero-evacuant activity. A third
bioassay involves testing for anti-implantation effects, initially in rats, with confir-
mation in hamsters.
The active principles of some Fabaceae, such as Sophora occidentalis L.,
Sesbania bispinosa (Jacq.) Wight and Cajanus cajan (L.) Mill., were found to be
isomeric quinolizidine alkaloids; they had some value as ecbolics but were ineffective
for inducing abortion during the early stages of pregnancy (Farnsworth et aL,
1975b). The activity of a principle of another Fabaceae, Pisum sativum L. (the
common garden pea), m-xylohydroquinone (2,6-dimethylhydroquinone) has been
studied extensively in women in India. However it proved to be only about 60%
effective in preventing conception in the groups studied and was abandoned as a
potentially useful fertility regulator (Sanyal, 1956, 1958; Sanyal and Rana, 1959;
Furuya and Galston, 1965).
From numerous reviews on plants as sources of antifertility agents (Casey, 1960;
Chaudhury, 1966; Vohora et aL, 1969; Brondegaard, 1973; Barnes et aL, 1975;
Prakash and Mathur, 1979 and many others), Farnsworth etcl. (1975a, b) concluded
that for the estimation of the potential value of new antifertility agents results
from animal experiments were difficult to interpret, and a WHO meeting was
convened in Mexico City in 1976 in order to develop a programme for a more
systematic evaluation of antifertility plants. Priorities were set on the study of male
contraceptives and 'morning after' and anti-implantation agents for use in the
female.
In January 1978, six collaborating centres in different parts of the world were
selected to contribute to the collection, testing and subsequent identification of
antifertility agents from plants identified by an extensive computer analysis of
published information (Soejarto et aL, 1978). In further research in the course of the
fulfilment of this worldwide programme, Bingel and Farnsworth (1980) pointed
out that plants tending to interfere with implantation in the female (Naqvi and
Warren, 1971; Morris and van Wagenen, 1973; Mishra et aL, 1979) and those
which may interfere with sperm formation and/or maturation in the male (Setty
et aL, 1976; Banerji et aL, 1979) were those of particular interest to the antifer-
tility programme. They found, however, that there are other factors to be
considered.
222
Abortion or interception has frequently been found to be caused by cytotoxic

plant constituents (Hartwell, 1976; Pakrashi et al., 1977). Many cytotoxic agents
have been found to be anti-spermatogenic, for example, vinblastine and vincristine
from Catharanthus roseus (Fern, 1963) and cardenolides from Calotropis procera,
(Atal and Sethi, 1962; Vilar, 1974; Atal, 1980). The use of such drugs entails the
danger that neoplastic agents may induce chromosomal aberrations and thus not
only affect the sperm number but also cause other adverse reactions. Therefore the
usefulness of cytotoxic agents for interrupting pregnancy is limited by their potential
toxicity to the maternal organism and by the possibility of their producing
teratogenic effects in the surviving fetuses, when given in marginal doses or at
marginal times (Morris, 1970, in Bingel and Farnsworth, 1980). In the case of Abrus
precatorius, abortive action seems to be limited to a steroidal oil and the teratogenic
action to an aqueous extract of the protein fractions. Separation of these two effects
may be possible by extraction.
Cyanogenic agents have also been noted to influence reproduction and neonatal
development in rats (Dlusi et al., 1979) and rabbits (Eshiett et al., 1980). Also, a
correlation between the spermicidal activity and the haemolytic index of certain
plant saponins has been reported (Ad Elbary and Nour, 1979).
Kamboj and Dhawan (1982) endeavoured to reduce the list of Indian plants used
for contraceptive purposes in females. They reviewed the literature on these plants
published in India together with the unpublished data of the Central Drug Research
Institute and gave most attention to the identification of plants with interceptive
properties. They concluded that in many cases the evaluation showed results which
varied from no activity to 100% activity for the same plant. Lack of proper botanical
authentication and inconsistent results in repeat tests or lack of facilities were
indicated as possible reasons. (They also suggested modification to the feeding
schedule of the plants to be screened.)
Of the plants examined, Kamboj and Dhawan (1982) excluded follow-up of
Hibiscus rosa-sinensis and Plumbago zeylanica on the basis of preliminary toxicity
studies. They recommended, in order of priority, follow-up of Achyranthes aspera
(stembark), Sapindus trifoliatus (seed) and Abrus precatorius (seed). Because of
similarities in the climates of parts of India and tropical West Africa, a certain
number of these plants also occur in the area discussed in this book, and a selection
of them (and of those indicated by Farnsworth et al. (1983)) is listed in Table 6.1. It
should be noted that the African plants will have to be examined for analogy in
chemistry and action with the Indian varieties.
Plants having antifertility effects in males

Plants used for regulating male fertility have to interfere either with sperm
production and maturation (Parkhurst and Stolzenberg, 1975) or with sperm storage
or with their transport in the female genital tract. Ideally, these plants should not
exert any effects on non-reproductive systems and enzymes. With these objectives
223
in mind, Bingel and Farnsworth (1980) selected from plants found worldwide a
number of promising and interesting species (see also Farnsworth and Waller,
1982). Of these, those species which are found in tropical West Africa are listed in
Table 6.2. Of course it will have to be checked whether the plants growing in West
Africa have the same constituents and properties as the same species grown
elsewhere.
As well as being included in the tables, a few antifertility plants which are of
particular interest to West Africa have been described in more detail.
Fig. 6.1. Albizia lebbeck Benth.

224 225
Table 6.1. Plants with antifertility action in females
Plant
Family Part used Active constituent(s) Observed activity References
Abrus precatorius L. Seeds, Aqueous extract of seeds See text. 150 mgof steroidal oil produces 80% Desai and Rupawala (1966)
Fabaceae roots (proteins), steroidal oil, sterility in rats. Oral doses of 300 mg of root Desai and Sirsi( 1966)
ethanol extract of root extract per kg body weight 100% interception. Dijkman etal. (1966)
LD 50 in mice is 2 mg/kg. Oxytocic Desai and Rupawala (1967)
Gupta etal. (1968)
Agrawalcia/. (1969,1970)
Achyranthes aspera L. Bark Oleanic acid saponin Abortive and anti-implantation activity in mice CV
Amaranthaceae using 50 mg benzene extract per kg body Gopolachari and Dhar (1958)
weight on Days 1—5 post coitum Hariharan and Ran jaswani (1970)
Kamboj and Dhawan (1982)
Ananas comosus (L.) Merr. Leaves Stigma-5ene-3/37a-diol, Anti-fertility activity in mice, abortive 50 ml I
syn. (A.sativa Schult.) stigma-5ene-3/37£-diol unripe fruit-juice on Day 1-7 post coitum Shukla and Krishnamurti (1961)
Bromeliaceae /Jsitosterol causes 60% interception Sakkawalaefa/. (1962)
Bhaduri«a/.(1968a)
PakrashieJa/. (1975a, b)
Carica papaya L. Fruit, Papain? Ethanol extract at doses of 100 mg/kg exerted 60% CV
Caricaceae (unripe) anti-implantation activity, higher doses hardly I
latex any. Early abortifacient effect. Oxytocic Chandrasekar«a/.(1961)
antiovulatory GargandGarg(1974)
Kapoor«a/.(1974)
Curcuma domestica Valeton Rhizome Essential oil, curcumin 100-200 mg petroleum ether extract per kg body I
syn.(C. longaL.)c. weight on Days 1—7 post coitum produces Arora eta/. (1971)
Zingiberaceae 80-100% anti-implantation. May act on Chandra and Gupta (1972)
adrenal-hypophysial axis. Essential oil inhibits Garg(1974)
hyalorunidase Gargetal. (1978)
Hibiscus rosa-sinensis Flower Ethanol extract, On tenth day of pregnancy rats having received Batta and Santhakumari (1970)
Malvaceae hibiscetin?? benzene extract showed 80% reduction in Singh etal. (1982)
implantation. No early abortifacient effect was
noted. Ethanol extract is said to alter sex ratio
of the pups
Hyptis suavolens ( L.) Poi t. Leaves Essential oil? Alcohol extract of leaves shows anti-implantation Garget a/. (1978)
Labiatae activity. Further investigation advised Bingel and Farnsworth (1980)
Oldenlandia affinis Whole Polypeptide (molecular Polypeptide isolated from aqueous decoctions of Gran(1973a,b,c,d,e)
(Roem.& Schult.) DC. plant, weight 4000), serotonin aerial parts of the plant produced, in vitro, Bingel and Farnsworth (1980)
syn. (O. decumbens) aerial parts contractions of pregnant uterus. Action
(Hochst.) Hiern. Hedyotis absent or doubtful in situ
affinis(Roem. & Schult.)
Rubiaceae
Plumbago zeylanica L. Whole Plumbagin (2-methyl-4- Abortive in vitro, no abortion in pregnant rabbits I
Plumbaginaceae plant, hydroxy-1 -4-naphtho- or guinea pigs. In rats 75-100% mortality after Bhatia and Lai (1933)
roots quinone) 3-4 doses. Oxytocic in vitro Ko(1933)
Premakumari el al. (1977)
Bingel and Farnsworth (1980)
Santhakumari and Sujantham (1980)
Rhoe spathaceae (Sw.) Plant Antifertility and anti-nidatory. Stimulative Wenigereta/. (1980)
Steam syn. (R. discolor) action on mouse uterus Weniger eta/. (1982)
Hance
Commelinaceae
Sapindustrifoliatus(L.) Seed, Saponin An ethanol extract administered 1-7 days post CV
Sapindaceae fruit-pulp coitum in rats produced 80% interception in Bodhankar«o/.(1974)
100 mg/kg doses and 100% interception with Garget a/. (1978)
500 mg/kg doses. A methanol fraction of the
ethanol extract acted orally in doses of 25 mg/kg
when given on Days 4 and 5 of pregnancy
"Where a plant has been discussed in another chapter, reference is made to that chapter. Thus CV refers to Chapter 2 (Cardiovascular plants) and I refers to Chapter 4 (Anti-infection
therapy).
Table 6.2. Plants with antifertility action in males
Plant
Family Part used Active constituent(s) Observed activity References'2
Aeschynomene indie a L. Whole Saponins Spermicidal at a concentration of 2% Seny etal. (1976,1977)

Fabaceae plant (instantaneous immobilization) for human and
rat semen in vitro
Albizia lebbeck Benth. syn. Seedpod, Echinocystic and oleanic SpermicidaP at a concentration opf 2%; according I
{Mimosa lebbeck L.) (root), acid saponins, to test used, the minimum effective doses of Dharera/. (1968)
(naturalized) (Fig. 6.1) (wood) lebbekanin E pod and root are, respectively, 0.125-0.6% and Setty etal. (1976)
Mimosaceae (heteroside of acacic 0.125-1.0%, for human spermatozoa in vitro Tripathi and Dasgupta (1974)
acid) An abortifacient glycoside, albitocin, found in Varshneyera/. (1979)
Albizia spp. has shown high toxicity Lipton(1967)
Anagallis arvensish. Whole Anagalligenin saponin Spermicidal* to human sperm I
Primulaceae plant (triterpenoid) Banerjiera/. (1978b, 1979b)
Yamadaetal. (1978)
Bezanger-Beauquesneera/. (1980)
Azadirachta indica (Seeds), Sodium nimbinate 1 ml of extract daily given orally, for one month I
Meliaceae leaves, (triterpene) produced in mice an 80% reduction in Sharmaand Saksena(1959)
water pregnancies. The males regain 100% fertility Ekongetal. (1969)
extract 45 days after stopping of treatment. Activity Gargetal. (1970)
has been attributed to loss of libido in treated Luscombe and Taha (1974)
animals Thompson and Anderson (1978)
Deshpandeetal. (1980)
Farnsworth and Waller (1982)
Blighia sapida Koenig Fruit Hederagin and oleanolic At a concentration of 2% spermicical6 against Banerjietal. (1979b)
(Akee apple) saponins human semen in vitro
Sapindaceae
Calotropis procera Ethanol Cardiac heterosides In gerbils 20 mg/animal orally every second day CV
(Ait.)R.Br. extract of (cytotoxic) for 30 days caused testicular necrosis and severe I
Asclepiadaceae flowers degenerative changes in the sexual organs and Atal and Sethi (1962)
also liver damage. Fractionation of the active Croutera/.(1964)
extract to separate the toxic factor is needed Hartwell(1976)
Garg(1979)
Farnsworth and Walker (1982)
Carica papaya L. Seeds Oleanolic glycoside? 20 mg/rat given perorally in aqueous suspension Garg and Garg (1971)
Pawpaw. Widely (76-78% of oleic acid in for 8 weeks to males reduced the ability to Bodhankare*a/.(1974)
cultivated oil of seeds) fertilize females by 40% although the weight Das(1980)
Caricaceae and histology of the genitals, and Farnsworth and Waller (1982)
spermatogenesis, seemed unaffected
Catharanthus roseus (L.) Don (Roots), Vinblastine, vincristine Intraperitoneal injection of the total leaf alkaloids I
syn. (Vinca rosea L., leaves (alkaloids) produced degenerative changes in the Joshi and Ambaye (1968)
Lochnera rosea Reichb.) spermatogenic elements of the testes in animals Bustos-Obregon and Feito (1974)
Apocynaceae and oligospermia in men Vilar(1974)
Cookeral. (1978)
Parvinenefa/. (1978)
Centella asiatica Urban syn. Whole Saponin, according to At a concentration of 2% the total saponins were N
(Hydrocotyle asiatica L.) plant provenance, asiaticosid active in vitro against rat and human sperm but Dutta and Basu( 1967)
Umbelliferae or brahminoside pure saponins showed no spermicidal* or AppaRao etal. (1969)
spermostatic action RaoandSeshadri(1969)
Setty etal. (1976)
Gossypium spp. Seed oil Gossypol (dimeric Spermicidal* action studied; widely used in men I
Malvaceae sesquiterpene) in China (see text) Aizikov and Kurmukov (1973)
Kalla and Vasudev (1980)
W a l l e r s / . (1980)
Ridley and Blasco (1981a, b)
Hibiscus rosa-sinensis L. Flower Ethanol extract, Ethanol and benzene extracts have antispermato- Kholkuteetal. (1972; 1976a, b; 1977)
Malvaceae petals, hibiscetin?? genic effect (see text) KholkuteandUdupa(1974,1976,
1978a,b)
Kholkute(1977)
Leucena glauca (L.) Benth. Leaves, Mimosine (3% in leaves, Feeding of male rats prior to mating with a ration Willetrt al. (1942-44)
syn. {Mimosa glauca) seeds 5% in seeds) = containing 15% of leafmeal caused an important Luna (1963)
Mimosaceae cytotoxic amino acid decrease in pregnancies. Leafmeal produces Farnsworth and Waller (1982)
alopoecia in sow and rabbits; addition of a
mimosine-inactivating agent impairs the effect
Lupinus tassilicus Maire Seeds Debittered seeds through Animals treated with a ration containing 27% of I
syn. (L. tennis Forsk.) hot water treatment debittered seeds for nine weeks showed Tannous and Nayfeh (1969)
Fabaceae decreased sperm production. Possibility of Tripathi and Dasgupta (1974)
limited testosterone production is mentioned Farnsworth and Waller (1982)
Mimusops elengi L. Seeds, Bassic acid saponin A 6:100 dilution of the saponin in Sorensen's Bannerjiera/. (1978a, 1979a, b)
(generally cultivated) (bark) isotonic phosphate buffer solution had
(Fig. 6.2) spermicidal* activity on human semen
Sapotaceae
(Table continued)
Plant
Family Part used Active constituent(s) Observed activity References"
Momordica charantia L. Fruit Ethanol extract of fruit, Subcutaneous or oral doses of 200-400 mg for two I
(African cucumber, momordicine ? weeks of an alcoholic extract of the fruits to Dhalla era/. (1961)
bitter gourd) gerbils and of 1.75 mg daily for 60 days to dogs Sucrow(1966)
Cucurbitaceae reduced testicular weights and spermatogenesis Morton (1967)
without affecting the seminal vesicles or Stepkaera/. (1974)
prostate glands. Additional studies required Olaniji(1975)
Dixitera/. (1978)
Khanna era/. (1981)
Phytolacca dodecandra Berry Oleanic acid saponin, Crude extracts as well as lemmatoxin and oleano- I
l'Herit. lemmatoxin glycotoxin are more active spermicidals than Ahmed etal. (1949)
(Endod, soapberry) nonoxynol-9, a widely used vaginal contracep- Shaaban and Ahmed (1959)
Phytolaccaceae tive. They avoid pregnancy in most cases or Stolzenberg and Parkhurst (1974)
reduce embryonic counts in the horns of Parkhurst and Stolzenberg (1975)
treated rats to low levels. Doses used are 500 Stolzenberg etal. (1975)
and 100 /xg of saponin extract or 500 /xg of
lemmatoxin on Days 1,4 and 6 post coitum or
100 /jig of oleanoglycotoxin on Day 4 only
Samanea saman J acq. & Aerial parts Glycoside of acacic acid Spermicidal* to rat and human sperm (in spot and Gargera/. (1976)
Merr. syn. (Pithecellobum (4 different sugars) jpppc tests'* minimum activity with 1-5% in Setty etal. (1976)
samawBenth. jacq., vitro). The spermicidal activity of the plants Setty etal. (1977)
A Ibizziaflavovirens tested by Setty et al. (1977) was found to be Varshney and Khanna (1978)
Hoyle) associated with the /3-amyrin C28-carboxylic
Mimosaceae acid type of sapogenin linked to a particular
sequence of sugar moieties
Sapindus trifoliatus L. Fruit Saponin The concentrate of a water-ethanol extract (3—4 Bodhankaretal. (1974)
(naturalized) extractions) was systematically fractionated. A Garg etal. (1976)
Sapindaceae 2% concentration of the n-butanol fraction of a Setty etal. (1976)
water-soluble part of the concentrate had Dixit and Gupta (1983)
spermicidal* activity against human sperm in
vitro. The saponin fraction used as a vaginal
cream was non-toxic in rabbits and rhesus
monkeys
TrigonellafoenwngraecumL. Seeds Hederagin glycosides A 2% concentration of the saponin fraction Setty etal. (1976,1977)
(cultivated in the north) (isolated like that ofSapindus) showed in vitro
Papilionaceae spermicidal* action against rat and human
semen. Minimum effective spermicidal doses
were 0.25 and 1.5% in spot and IPPF tests,
respectively
Withaniasomnifera(L.) Root Flavonoids?withaferin, 25 mg dried root powder administered daily for 10 N
Dunalsyn. (Physalis withanolides?? days to male and female mice decreased the Watt and Breyer-Brandwijk (1962)
somnifera L.) number of pregnancies and produced small Garg and Prasar( 1965)
Solanaceae litters. Additional studies required. Locally Menssen and Stapel (1973)
used in South African tribes to remove retained Abraham et al. (197 5)
conception product in miscarriage Setty etal.{\976)
BaerandHaensel(1982)
"Where a plant has been discussed in another chapter, reference is made to that chapter. Thus CV refers to Chapter 2 (Cardiovascular plants), N refers to Chapter 3 (The nervous system)
and I refers to Chapter 4 (Anti-infection therapy).
''No revival of sperm motility by buffered glucose solution.
'International Planned Parenthood Federation.
^Tests based on activity against human sperm in vitro.
230
Abrus precatorius L. (Fig. 6.3) FABACEAE

Crabs eye, lucky bean
(See also Chapter 2 and Sweetening agents (Chapter 7).) Under the name ofjequirity
the seeds have long been known for their topical effect in the treatment of chronic
granular conjunctivitis. However, absorption of the granulations may cloud the
cornea, resulting in blindness. This use has therefore been abandoned as it is too
dangerous (Dalziel, 1937, p. 124).
The seeds contain a toxalbumin, abrin, which agglutinates erythrocytes and causes
haemolysis and enlargement of the lymphatic glands (Oliver, 1960). An aqueous
Fig. 6.2. Mimusops elengi L.

231
extract of the seeds was found to contain five protein fractions (Desai and Sirsi,
1966). The seeds also contain a steroidal oil, terpene, /3-sitosterol, stigmasterol and
three indole derivatives, iV-methyltryptamine, Af-methyltryptophan and
hypaphorine (Desai and Rupawala, 1966; Gupta et al., 1968). The roots, leaves and
stems contain glycyrrhizin in higher doses than Glycyrrhiza root and are used for its
extraction (Boiteau et al., 1964).
The seeds were found to be abortive and teratogenic (Desai and Rupawala, 1966).
Detailed histopathological studies on the fetuses, placentae and uteri of rats and mice
showed that oral administration of 150 mg/kg of body weight of the steroid oil of the
seeds on Days 1 and 5 post-coitum produced 100% sterility;.such administration on
Days 1 and 2 or on Day 5 post coitum produced 80% interception. The LD 50 of the
Fig. 6.3. Abrusprecatorius L.

232
aqueous extract in mice was 2 g/kg (Desai and Sirsi, 1966; Desai and Rupawala,
1967). Petroleum ether and alcoholic extracts of the roots (100 mg/kg body weight)
administered on Days 1 and 5 post coitum produced 75-80% of anti-implantation
effect in rats and mice. The aqueous extracts of the seeds were found to have high
cytotoxicity in vitro: 0.072 g inhibited growth by 50% as compared to the control
(Dijkman et al., 1966; Oliver-Bever, 1971). Oral administration of 300 mg/kg of
body weight of alcoholic extracts of the roots to rats prevented implantation in 100%
of the cases (Agrawal et al., 1969, 1970).
As Abrus roots have (like the leaves and stems) a high glycyrrhizin content, the
oestrogen antagonistic action of this substance should also be taken into consider-
ation; it seems to point to significant inhibition of the oestrogenic response (Agrawal
et al., 1969, 1970). Interference with enzyme systems essential for either oestrogen
absorption or oestrogenic stimulation of the target organs, which is mediated
through the hypophysis, appears to Kraus and Kaminskis (1969) to be the most
likely explanation of this action.
Gossypium spp. MALVACEAE

Cotton plant
In Nigeria the root is believed to be an emmenagogue with an action like that of
ergot; the active principle is in the rootbark (Dalziel, 1937). T h e use of the root to
procure abortion is known amongst American negroes but not in the Orient, the
knowledge of this property appears to be indigenous to Africa' (Dalziel, 1937, p.
126). Women of the Wolof tribe in Senegal use a decoction of the root to treat
amenorrhoea (Kerharo and Adam, 1974, p. 521). The South American Africans
used a decoction of the roots as a contraceptive (Brondegaard, 1973).
The rootbark contains a resin, 1-2% gossypol, vitamin E and a 'not yet isolated'
oxytocic and vasoconstrictive compound (Paris and Moyse, 1967, Vol. II, p. 254).
Gossypol is an orange-red polyphenolic pigment which is insoluble in water and
soluble in ether and chloroform. It is a dinaphthyl derivative with six phenolic OH
groups and two aldehyde functions, and exists in three isomeric forms (a, (3 and y).
The compound is unstable and can be destroyed by heating and thus eliminated from
the oil-cake on which it confers a certain toxicity. The oil-cake contains about 1% of
gossypol, is rich in protides and contains a small quantity of flavonoid pigments
(Paris and Moyse, 1967, Vol. II, p. 254).
Oral administration of gossypol acetic acid (5-10 mg/kg daily for 12 weeks) induced
sterility in male hamsters and rats (Hadley etal., 1981; Hahnetal., 1981). Dead and
abnormal sperm were observed in the male tracts and there was a decrease in
implantation sites and failure of pregnancy in the females mated to the gossypol-
treated males. Similar treatment of male rabbits (with doses varying from 1.25-
10 mg/kg for 5-14 weeks) produced poor motility of the sperm (Ridley and Blasco,
1981a, b) but had no other consequences (Chang et al., 1980) and after the treatment
was stopped recovery of fertility was observed (Zhou and Lei, 1981).
The emmenagogic properties of the root of Gossypium were confirmed by
Planchon and Bretin (1946), who also reported that it acts as a haemostatic on the
233
uterus and produces uterine contractions that are similar to the spontaneous
contractions of the uterus during childbirth, but without the tetanizing effect of rye
ergot. Gossypol is a nerve and cellular poison and has been tested as an anticancer
agent (Paris and Moyse, 1967, Vol. II, p. 255).
Studies on gossypol for human contraception were started in China in the early
1970s but were not published in English until 1978. The status of gossypol as a male
contraceptive was summarized by Zatuchni and Osborne (1981) and Prasad and
Diczfalusy (1981). In 1972 semen analyses were carried out on five male subjects.
After administration of gossypol for 35-42 days, at a dose of 60-70 mg daily, four of
the men were azoospermic and one was necrospermic (Wu, 1972; Qian et al. in
Turner, 1981 (from Farnsworth and Waller, 1982); Xue, 1981).
By 1980 more than 8000 men in the Republic of China had been treated with
gossypol, gossypol acetic acid (more stable) and gossypol formic acid (there appears
to be no significant difference in the action of the three compounds). The usual dose
administered was 20 mg daily for 60-70 days followed by a maintenance dose of
about 60 mg/week (Liu et a/., 1981; Prasad and Diczfalusy, 1981). In 99% of the
cases a marked decrease in sperm count, usually to 4 million/ml or less, was noted
2-3 months after the dosing began.
Gossypol was reported to cause a degeneration of the germ cells in the seminiferous
tubules of Man and animals when given orally, and to lead to absence of sper-
matogenesis. It might, however, find application as a vaginal contraceptive, and
Waller et al. investigated the possibilities of appropriate chemical forms for this
purpose (Wallers al., 1980, 1981).
Results of chromosome studies reportedly showed that gossypol was not
mutagenic. Gossypol is a lipid-soluble compound which has been shown to be
eliminated from the body slowly and cumulative toxicity is a possibility (de Peyster
and Wang, 1979). Clinically, the chief side-effect reported was passing weakness
occurring early in therapy. The relationship, if any, between gossypol intake and the
hypokalemia (Qian, 1980), mild electrocardiographic changes and transient elev-
ations in serum glutamic pyruvic transaminase level observed in some patients
remains to be determined (Bingel and Farnsworth, 1980).
Optically active gossypol has also been obtained from Thespesia populnea (L.)
Soland. ex Corr., (Malvaceae) a coastal tree (King and de Silva, 1968).
Hibiscus rosa-sinensis L. (Fig. 6.4) MALVACEAE

In nine different countries, including China, India, Indonesia, New Guinea,
Trinidad and Peru, the flowers are used as an emmenagogue and in a number of these
countries the leaves are used as an oxytocic. The leaves and flowers together are said
to be labour-inducing; in Indonesia, New Caledonia and Vietnam the flowers are
said to be abortifacient, whilst in India an antifertility effect has been attributed to
them (Farnsworth et al., 1983).
Cyanidin diglucoside has been reported to be present in the flowers by Hayashi
(1944). Agrawal and Rastogi (1971) have isolated taraxeryl acetate and sitosterol
from the leafy stems. Furthermore, cyanidin, quercetin, hentriacontane, cyanidin
234
diglucoside, calcium oxalate, thiamin, riboflavin, niacin and ascorbic acid have been
detected in this plant but none of these has been found to have antifertility activity
(Singh etal., 1982).
Kholkute and co workers observed in 1972 that extracts of//, rosa-sinensis flowers
showed antispermatogenic activity in rats. Feeding an ethanol extract of the flowers
to male rats for 30 days in doses of 50, 150 and 250 mg/kg produced practically no
effect at the lower doses. With the highest dose, however, histological examinations
showed that after 30 days there was shrinkage of the seminiferous tubules, destruc-
tion of spermatogonial cells and complete disorganization of the testicular tissue.
Ley dig cells were absent and germinal cells were distinctly affected, whereas Sertoli
cells were hardly affected and the seminal vesicles and prostate were unchanged
(Kholkute, 1977). Later, the investigators noted in male rats a loss of secretory
activity and degranulation of the gonadotrophs in the pituitary gland. The authors
suggested that the antifertility results were obtained through inhibition of gonado-
trophin release. They noted that the effects were reversible after discontinuation of
the treatment (Kholkute et al., 1976a, b, 1977, 1978a, b).
Injection of a single 7.5 mg dose of//, rosa-sinensisflowerextract subcutaneously
in a group of reproductively active male bats (Rhinopoma kinneari) followed by
measurement of the six testicular lactate dehydrogenase (LDH) isozymes showed
that lactate dehydrogenase (LDH X ) disappeared from the isozymograms on Days
2-A but reappeared on Day 5 after the injection. In further investigations (Kholkute,
1977) in which a benzene extract of the flowers and seeds was screened for post-coital
antifertility in female albino rats (Kholkute and Udupa, 1978a, b) the authors
observed that only the flowers were active, the leaves, stem and stembark being
Fig. 6.4. Hibiscus rosa-sinensis L.

235
devoid of activity (Kholkute et al., 1976a). Allied Hibiscus spp. failed to show any
significant effect. Seasonal variations were important, the highest activity being seen
in winter (100%) whilst in spring and summer this was reduced (to 75% and 50%,
respectively) (Kholkute and Udupa, 1974; Farnsworth and Waller, 1982). Of
various extracts of H. rosa-sinensis flowers studied in female albino rats for their
antifertility effect, the benzene extract was found to be the most effective (Kholkute
and Udupa, 1976).
In an attempt to isolate the active constituents of this benzene extract by
fractionation, it was noticed that the ether-soluble portion of the water-insoluble
fraction showed significant anti-implantation and abortifacient activities. Thus,
after doses of 73 mg/kg body weight daily from the first to the tenth day of
pregnancy, no implantations were found on the eleventh day (day of laparotomy).
For confirmation of the abortifacient effect ten pregnant rats were given a daily dose
of 73 mg/kg from the fourteenth to the twentieth day of pregnancy. In no case was a
delivery recorded (Singh et al., 1982).
The antifertility effect of the flower petals of H. rosa-sinensis had formerly been
reported by Nadkarni and Nadkarni (1954) and Batta and Santhakumari (1970),
who noted an antifertility activity of 80% (as shown by an 80% reduction in
implantation sites on the tenth day of pregnancy) of the benzene extract in fertile
female rats and mention an effect on the sex ratio of the pups born to experimental
animals treated with the ethanol extract.
Rats receiving 50—250 mg/kg doses of benzene extract daily for thirty days showed
follicular atresia and reduced ovarian, uterine and pituitary weights; this
demonstrated anti-oestrogenic as well as oestrogenic activities of the extract (Khol-
kute et al., 1976a). Experimental studies could thus show the anti-oestrogenic,
antifertility, anti-implantation and oestrous-cycle disrupting effect of the benzene
and ethanol extracts given orally to rats (Farnsworth et al., 1983).
Some clinical tests confirmed the contraceptive value ofH. rosa-sinensis (Tewari,
1974; Tewari etal., 1976).
Achyranthes aspera L. AMARANTH ACE AE

This plant, already described in Chapter 2, is a common weed, very variable in
height (36-180 cm) and sometimes woody. (These details are mentioned because it
is reported by Pakrashi et al. (1975b), Pakrashi and Bhattacharya (1977) and by
Kamboj and Dhawan (1982) that an extract of the stembark prevents pregnancy.
Perhaps the botanical identity should be controlled.)
Fifty mg of the benzene extract of the plant tested by these authors per kg body
weight inhibited pregnancy by 100% when given orally on Days 1 or 6 post coitum
in mice. The benzene extract was also active in rabbits on Day 8 of pregnancy. In the
1-7 days post-coitum schedule the benzene extract and a 50% ethanol extract
(200 mg/kg) were inactive in rats (Pakrashi et al., 1975b; 1977). Administration of
75 mg/kg in mice every twenty-first day for 6 months had no toxic effects, nor had a
single dose of 1 g/kg body weight in mice (Pakrashi et al., 1975b; Pakrashi and
Bhattacharya, 1977).
236
The benzene extract was reported to be devoid of oestrogenic, anti-oestrogenic

and androgenic properties in mice (Kamboj and Dhawan, 1982). The active
component is believed to be oleanolic acid 3/3-glucoside (Pillay et al., 1977).
Sapindus trifoliatus L. i. SAPINDACEAE

This plant is also described in Chapter 2.
C The plant contains a saponin (Chopra et al., 1956, p. 221).
P In rats ethanolic extracts produce 80% inhibition of implantation when administered
to rats 1-7 days post coitum in 100 mg/kg doses and 100% inhibition when
administered in 500 mg/kg doses. (Taking into consideration the fact that 10-20 mg/
kg produce a dose-dependent decrease in blood pressure and heart rate (Singh et al.,
1978), this treatment seems less recommendable.) A methanol fraction of the
ethanol extract had oral antifertility action at doses of 25 mg/kg when given on Days
4 and 5 of pregnancy (Bodhankar et al., 1974; Garg et al., 1978; Kamboj and
Dhawan, 1982).
Garg et al. (1980) took out a patent for the use of saponin- (including oleanolic
aglycones) bearing plants such as Sapindus trifoliatus, Blighia sapida, Samaena saman
based on their spermicidal activity.
Momordica charantia L. CUCURBIT ACEAE

Bitter gourd
(See also Chapter 7 (Hypoglycaemic plants).)
P Antifertility activity of this plant has been studied in both males and females.
Concerning the spermatocidal action, Dixit et al. (1978) observed that an ethanol
extract of M. charantia fruits administered orally or subcutaneously to adult male
gerbils (Meriones hurrianae) in doses ranging from 200 to 400 mg/kg during two
weeks disrupted spermatogenesis and reduced testicular weights. The seminal
vesicles and prostate did not seem to be significantly affected by this administration.
Chronic administration of an ethanol extract of M. charantia fruit (1.75 g daily)
orally to male dogs for 60 days caused testicular lesions resulting in mass atrophy of
the spermatogenic elements: 75 ± 8.9% of the seminiferous tubules completely
lacked step 1-8 spermatids. Serum enzymes, serum protein, cholesterol, bilirubin,
blood sugar and blood urea levels were within normal ranges. Haematological
studies showed no deviations except a slight rise in total leucocyte count, which has
been attributed to emotion or strenuous exercise at the time of blood sample
collection (Dixit et al., 1978). The authors conclude that the extract induced a state
of infertility without altering general metabolic activities.
The roots have been found to have an abortifacient effect in females (Jamwall and
Anand, 1964). Several constituents of the fruits, such as charantin, 5-hydroxytryp-
tamine, diosgenin and /3-sitosterol, were observed to act as stimulants of the uterus.
In the rabbit charantin has been found to cause uterine haemorrhage and abortion
and in rats it inhibited foetal development (Jamwall and Anand, 1964). The
cucurbitacin-like triterpenes also found in the plant have been shown to possess a
potent cytotoxic activity (Weniger et al., 1982).
237
Recently, a Mexican plant, Montanoa tomentosa (Compositae) with a non-steroidal

fertility regulating substance (zoapatanol, an oxepane diterpene) for use by women
has attracted much attention. It was the subject of over thirty patents between 1971
and 1982 (Farnsworth et al.> 1983). Unfortunately, it is not found in tropical West
Arica. In India, the alkaloid vasicine from Adhatoda vasica (related species in
tropical West Africa) has been extensively tested for the termination of mid-trimester
pregnancy. Intra-amniotic instillation of 60 mg or more produces abortion within
48 h, with minimal side-effects (Atal, 1980). The presence of vasicine in African
species has not been reported so far.
Enzyme-inhibiting contraceptives and spermicides of plant origin

In order to find more selective sperm inhibitors, Farnsworth and Waller
(1982) have investigated sperm-specific enzyme inhibitors. Numerous enzyme
systems in viable sperm are susceptible to inhibition, for example those involving
glycolysis, energy production and myosin contraction. Investigations into the
biochemistry of fertilization have shown that the enzymes of major importance for
fertilization are acrosin and hyaluronidase and that 'plant derived acrosin inhibitors
are few, they include soybean and other trypsin inhibitors as well as a large number
of monosaccharides' (Farnsworth and Waller, 1982). These authors quote recent
publications by Kennedy et al. (1982) and van der Ven et al. (1982) reporting the
inhibition of acrosin by gossypol and another, by Lee and Mailing (1981), reporting
the selective inhibition of sperm-specific lactate dehydrogenase (LDH X ) by gos-
sypol. In addition they mention as a hyaluronidase inhibitor the essential oil of the
root of Curcuma domestica, a species also cultivated in West Africa.
Active spermicidal compounds encompass a number of chemical structures. A
majority of plant-derived spermicides are triterpene saponins and, more rarely,
some are steroid saponins. Since all saponins show surface-active properties, it has
been suggested that the most likely mechanism for their action is a disruption of the
sperm plasma cell membrane (David and Heftman, 1981). A currently marketed
spermicide, 'nonoxynol-9', has been based on this theory (Ad Elbary and Nour,
1979; Farnsworth and Waller, 1982).
In females using contraceptive steroids, changes have been reported in red blood
cell enzymes requiring B vitamins for their coenzymes and in steroid-metabolizing
enzymes of the uterus (Briggs and Briggs, 1981).
Plants with an action on menstruation

Plants used to treat dysmenorrhoea can act in different ways. Plants such
as Polygonum spp., which contain haemostatic flavonoids, are used for the treatment
of menorrhagia whereas other plants, such as Alchornea cordifolia and some members
of the Solanaceae, which contain atropine, papaverine and yohimbine, are used
because of the antispasmodic action of these alkaloids. Sometimes progesterone or
androgens are used.
In some forms of dysmenorrhoea and in amenorrhoea, plants such as Petroselinum
which contain essential oils (apiol) that produce contractions of the uterus and are
238
abortive in high doses are sometimes given (Paris and Moyse, II, 1967, p. 476).
Usually, however, oxytocic agents based on oestrogenic hormones are used. These
plants can act as abortifacients in high doses. In folkloric medicine their mechanism
of action is mostly unknown and the same lack of information as is evident for the
plant oestrogens also applies in this field. A number of these plants are described as
antifertility plants (Achyranthes aspera, Diospyros spp., Grewia spp. (Paris and
Theallet, 1961), Gossypium herbaceum and spp. and Withania somnifera, etc.). Some
of these plants which act as emmenagogues exert their hormonal action via the
hypothalamus and the pituitary. This property was reported as early as 1950 (Gupta
et al., 1950) for one West African plant (Pergularia daemia).
Pergulariadaemia(Forsk.)Chiov. syn. (P. extensaN.E. Br.,DaemiaextensaK. Br.)

ASCLEPIADACEAE
The plant is believed to have emmenagogic properties. In Ghana the leaves are given
to women immediately after childbirth. In Nigeria the latex or a poultice of the leaves
is applied to boils and abscesses, a use also known in India. The juice of the leaves is
also used to treat sore eyes (Dalziel, 1937, pp. 388-9).
The plant contains a bitter resin, two bitter principles and a glycoside (Chopra et al.,
1956, p. 188).
The glycoside has a physiological action on the uterus similar to that of the pituitary
gland.
Aloe barbadensis Mill. c. syn. vera L., A. vulgaris Lam., A. indica Royle)
LILIACEAE
In Nigeria the juice of the leaves of A. schweinfurthi Bak. is used in the treatment of
guinea worm infestation and in Ghana it is used for the treatment of vitiligo (Dalziel,
1937, p. 476). In India extracts of A. barbadensis are considered a tonic in small doses
and a purgative, emmenagogue and anthelmintic in larger doses. The dried juice is
cathartic and is used to relieve constipation. The pulp is used to reduce or prevent
menstruation (Chopra etal., 1956, p. 13).
The juice of the leaves contains anthraquinone derivatives (emodin, aloin, barbaloin,
isobarbaloin and resins (Chopra et al., 1956, p. 13; Shah and Mody, 1967). Whole
leaves, the rind and the pulp contain oxidases, catalases and sugars.
A. barbadensis powder has been widely used as a purgative and was found to have a
beneficial effect in the healing of thermal burns and of radiation therapy (Singh et al.,
1973). When given in doses of 60 mg/kg intragastrically to female rabbits this
powder increased not only the fertility rate but also the litter size of the animals
(Sharmaera/., 1972).
Aloe compound was reported to be very useful in cases of disturbed menstrual
function and functional sterility (Bhaduri et al., 1968; Garg et al., 1970). This was
confirmed by Gupta (1972), who found in 250 cases of sterility that Aloe powder
improved fertility in 85% of the cases and that menstrual functions improved in
44.6% of them. However, when plants were tested for interceptive action, it was
found that a 50% ethanol extract of the leaves, in contrast to all other extracts tested,
239
had a strong interceptive action when given in high doses (100-200 mg/kg) on Days
1-7 post coitum (Casey, 1960; Gupta et aL, 1971).
Plants with an action on lactation

Plants with latex, such as Euphorbia hirta and other Euphorbia spp., and
Alstonia scholaris, often have the folkloric reputation of acting as galactogogues.
These properties are still reported by reviewers today. Although the constituents
and pharmacological properties of these plants have been studied in more detail in
the last few years, a scientific confirmation of their galactogogue action has not been
reported.
It has long been known that prolactin, the lactation stimulating hormone of the
anterior pituitary can increase lactation. There is, however, often a certain reluctance
nowadays to manipulate the hypothalamus-pituitary axis because of the other
pharmacological effects produced.
Sarcostemma viminale R.Br. ASCLEPIADACEAE

In some South African tribes this plant is used as a galactogogue for both women and
cows (Watt and Breyer-Brandwijk, 1962).
The stems contain 2% of a mixture of five pregnane glycosides. One of two recently
reported genins contains a dihydroacetone group like cortisol but has different
stereochemistry at C-14 and C-17 (Schaub et aL, 1968; Stockel et aL, 1969).
Not only does this plant seem to act via the adrenal-pituitary axis but convulsions
similar to those produced by strychnine, which result in paralysis and death, have
been observed in cattle (sheep) after they have eaten the plant (Steyn, 1937).
Therefore this plant should not be considered for human or veterinary applications!
Vitex agnus castus L.c. VERBENACEAE

The fruit contains an essential oil, cineol, flavonoids and the glycoside aucubin and
its hydroxybenzoic ester agnuside. These melanin-forming glycosides are unstable
and polymerize to form black pigments when exposed to the air (Steinegger and
Hansel, 1968, p. 497; Paris and Moyse, 1971, Vol. Ill, p. 255).
V. agnus castus has been reported to have a luteinizing action as a result of inhibition
of the gonadotrophic action of the posterior lobe of the pituitary. Extracts of the
fruits have been on the market for the treatment of dysmenorrhoea and as a
galactogogue (Steinegger and Hansel, 1968, p. 497).
Other Verbenaceae like Verbena officinalis are also said to have galactogogue
properties. The active principle is aucubin (a glycoside of a lactonic monoterpene).
It has weak parasympathomimetic properties and causes contraction of the smooth
muscle of the uterus (Steinegger and Hansel, 1968, pp. 497-8). In mammals
V. officinalis produces a strong and prolonged milk secretion. The twigs, leaves and
flowers yield verbenalin (Mcllroy, 1951, p. 110).
Ipomoea mauritiana Jacq. syn. (/. digitata of F.T.A.) CONVOLVULACEAE

In Nigeria the whole root is used as a purgative and a galactogogue (Dalziel, 1937,
240
p. 438). The same uses are mentioned for the very closely related / . digitata L. syn.
(/. paniculata R.Br.) in India, which is also claimed to be an aphrodisiac (Chopra et
al., 1956, p. 142).
The roots of the Indian species contain 1.3% of fixed oil (glycerides of oleic, palmitic,
linoleic and linolenic acids). In addition /3-sitosterol and a heteroside, paniculatin,
which is soluble in water and thermostable, have been isolated (Matin et al., 1969).
The heteroside of the Indian species acts as a stimulant of the smooth muscles of the
myocardium, bronchi and bowel and is also oxytocic; when it is given intraperitone-
ally, the LD 50 in mice is 867.4 mg/kg (Mishra and Datta, 1962; Matin et al., 1969).
Kigelia africana (Lam.) Benth. syn. (K. pinnata (Jacq.) D C , (K. aethiopica Decne,
K. abyssinica Rich., K. elliotii Sprague, etc.) (16 synonyms!) BIGNONIACEAE
Sausage tree
In South Africa the fruits are used as a dressing for ulcers or to increase the flow of
milk in lactating women (Watt and Breyer-Brandwijk, 1962). In Ghana the fruit and
roots are boiled together with the 'tassels' of plantain flowers as a 'women's remedy'
(Dalziel, 1937). In Northern Nigeria the fruit is used in some districts as a purgative,
whereas in other regions it is used to treat dysentery (Dalziel, 1937, p. 443). In Cape
Verde the fruit is rubbed on the breast of young girls to enhance their development.
The fruit also has many superstitious uses. In Kenya a decoction of bark and leaves
is drunk as an abortifacient. The fruit is commonly added to beer and claimed to be
an aphrodisiac (Kokwaro, 1981). The unripe fruit is said to be very toxic.
From the fruits and leaves El Sayyad (1981) isolated and identified the flavonoids
6-hydroxyluteolin-7-O-glucoside, luteolin-7-O-glucoside, luteolin and quercitin.
From the roots Govindachari et al. (1971) have obtained dihydro-isocoumarins,
lapachol and sterols and Alamelu and Bhuwan (1974) have reported the presence of
iridoid glycosides.
Other plants growing in Nigeria that are reported to act as galactogogues are
Allophyllus africanus Beauv. (Sapindaceae) (the leaves are also used to treat piles)
and Alternanthera repens (L.) Link. (Amaranthaceae) (the leaves of which are also
used as an abortifacient). The presence of flavonoids and the absence of steroids,
terpenes, alkaloids, saponosides, tannins, quinones and cyanogenetic glucosides has
been reported for the bark of the Congolese specimen of Allophyllus africanus
(Bouquet, 1972). The chemistry of Alternanthera appears not to have been studied.
Trigonella foenum graecum L. (Fabaceae) is considered a galactogogue in the
Sudan (Ayoub and Svendsen, 1981).
Indirect stimulation of lactation has also been obtained with dried thyroid gland
or thyroxine via the pituitary gland (Robinson, 1947; Naish, 1954).
Jasminum sambac (L.) Ait. c. OLEACEAE

The flowers are used in India to stop the secretion of milk in women in the puerperal
state after childbirth (in cases of threatened abscess) by applying them unmoistened
to the breasts. The roots are claimed to be emmenagogic (Chopra et al., 1956, p. 144).
241
An iridoid glycoside as well as jasminin, quercetrin, isoquercetrin, rutin, quercetin-

3-dirhamnoglycoside, kaempferol-3-rhamnoglycoside, mannitol, a-amyrin, /3-
sitosterol and sucrose have been reported to be present in the leaves of this plant
(Ross et al., 1982). The flowers contain an essential oil.
(c) Male sex hormones (androgens)

The main androgen is testosterone. It is secreted by the interstitial cells of
the testis under the influence of luteinizing hormone and is required for sper-
matogenesis. In fact both androgen secretion and spermatogenesis are controlled by
the hypothalamic-pituitary axis. In the liver a large proportion of the testosterone is
degradated into androsterone and etiocholanone. These two substances and testo-
sterone glucoronide are eliminated by the kidneys. The androgens are also secreted
from the adrenal cortex and the ovaries. They cause retention of water and of
nitrogen, sodium, calcium, chloride, sulphate and phosphorus ions and also increase
protein metabolism (Burgen and Mitchell, 1972; Lechat et al., 1978).
Testosterone can only be administered by injection as it is absorbed by the
digestive mucous membranes and immediately inactivated by the liver when given
perorally. Dissolving testosterone in oil and making chemical substitutions in the
molecule can to a certain extent slow down the hepatic catabolism.
Exogenous oestrogen produces an anti-testosterone effect, mainly owing to its
action on the hypothalamus and pituitary (Lechat et al., 1978, pp. 548-51). The
need to administer the hormone parenterally explains the dearth of published
reports and indications in folkloric medicine of the use of plant androgens.
Aphrodisiacs seem to be the main indication mentioned. The use of a leaf decoction
of Lonchocarpus cyanescens for the treatment of venereal disease and semen insuf-
ficiency has, however, been reported (Ainslie, 1937).
Apart from being given in replacement therapy when normal secretions are
reduced or absent, androgens are used to stimulate anabolic activity, encouraging
protein anabolism, in the treatment of osteoporosis and sometimes to inhibit the
growth of breast carcinoma. For their use as anabolic agents the difficulty lies in
obtaining compounds with high anabolic and low androgenic activity, as in female
patients there is the danger of masculinization (Burgen and Mitchell, 1972). A West
African plant used in the treatment of osteoporosis is Cissus quadrangularis (see
Chapter 3).
II Thyroid hormones
The thyroid gland plays an important part in the organism as it stimulates
metabolic activity and also controls growth. The two hormones secreted by the gland
are thyroxine and triiodotyronine, and they are present in a proportion of 50:1; they
are both iodine-containing amino acids and are synthesized in the gland itself, which
takes up iodine from the blood (Burgen and Mitchell, 1972).
Hypoactivity of the thyroid gland causes myxoedema and a 20-30% decrease in
basal metabolism. Lack of iodine is often the basis of this insufficiency and treatment
242
is usually effected by administration of thyroxine or thyrotrophin (anterior pituitary

hormone) or of components rich in organic or inorganic iodine, for example algae
like Fucus vesiculosis L., which contains 0.03-0.1% iodine (Chesney and Webster,
1928; Steinegger and Hansel, 1968). Hyperactivity of the thyroid function, e.g. in
patients with Basedow's disease, can be inhibited by drugs which inhibit the uptake
of iodine by the gland. Thiocyanates inhibit this uptake and have a weak inhibitory
action on iodide binding (Burgen and Mitchell, 1972, p. 148). Temporary treatment
is obtained with iodine as it causes retention of thyroxine in the gland and so it is not
released into the blood. (This effect is used in preparing hyperthyroid patients for
thyroidectomy.) Other drugs which inhibit, by substrate competition, the
peroxidase enzyme which releases iodine from circulating iodides and, in addition,
inhibit the enzymes responsible for iodination of tyrosine and coupling of the
iodinated derivatives are imidazoles and thiouracils (Turner and Richens, 1978, p.
168; Kagihara, 1980).
Other substances which reduce hyperactivity are extracts of Brassica oleraceae
L. and other Brassica spp. as had already been observed in 1928. In 1949 an active
'goitrogenic' principle was isolated from the turnip, B. napa; it was called goitrine
and was found to be a glucoside of l,5-vinyl-2-thio-oxazolidone (Astwood et al.,
1949). Subsequently it was shown that the seeds, roots and aerial parts of many
Brassica spp. contain progoitrine. Through hydrolysis by enzymes such as
myrosinase, a common enzyme in the Cruciferae, but also under the influence of
bacteria present in the digestive tracts of animals, progoitrine liberates the
isothiocyanate of 2-hydroxy-3-butenyl. Cyclization of this leads to the active
principle, goitrine (Virtanen, 1961). The mechanism of action of goitrine is believed
to be based on its intervention in the biosynthesis of thyroxine and not on the
accumulation of iodine in the thyroid gland (Murti etal., 1964).
Diverse poly phenols are also capable of fixing iodine and of removing this element
from the thyroid gland. The goitrogenic effect of Glycine soya is thought to be related
to the presence of phytoagglutinins, which prevent normal intestinal absorption of
thyroxine. Other plants which contain phenols of the flavonoid type such as
quercetin, rutin and catechin also have an action on the thyroid gland (Steinegger
and Hansel, 1968).
An indirect inhibitory effect on thyroid secretion by Lithospermum ruderale and L.
officinale (not in W. Africa) has been reported (Train et al., 1941; Kemper and
Loeser, 1957); they act via the thyrotrophic (and also gonadotrophic) hormone of
the pituitary gland.
In West Africa it is mainly Arachis hypogeae which provides the goitrogenic
principle although some Capparidaceae and Carica papaya seeds are likely to have a
similar effect.
Arachis hypogeae L. FAB ACE AE

Groundnut, peanut
(See also Chapter 2.) A goitrogenic and an oestrogenic factor have been isolated from
the seeds of this species.
The goitrogenic principle was found to be insoluble in oil and thermostable as it is
243
retained in the oil-cake and in the roasted seeds (Greer and Astwood, 1948; Buxton
et al., 1954; Busson, 1965; Adrian and Jacquot, 1968). If the normal diet of the rat
is supplemented by 20% with the oil-cake, the weight of the thyroid gland is
increased from 9 to 24 mg whilst its content of mineral iodine goes up from 5 to
20.5%. Addition of 1 g of water per day per animal completely re-establishes the
thyroid metabolism. The goitrogenic factor is believed to be located in the
chromogenic tegument of the nut. Arachoside and glycosides isolated from the nuts
inhibit the formation of inorganic iodine and thyroxine and result in a major increase
in the urinary secretion of iodine and phenols (Mudgal et al., 1957, 1958).
The oestrogenic factor is soluble in oil and is retained after refining. Introduction
of refined peanut oil to form 10% of the food ration of immature mice increases
uterine weight from 9.5 to 15.9 mg (refined olive oil produces an increase to 16.7 mg)
(Booth et al., 1960). A substance antagonistic to aldosterone which modified sodium
reabsorption and urinary secretion of sodium and potassium could also be detected
in arachis oil; 0.05 ml of the oil largely antagonized the action of 10 fig aldosterone
(Kumar tf al., 1962).
Kumar et al. (1962) noticed in earlier investigations that the effects of desoxycorti-
costerone acetate on the urinary secretion of sodium and potassium ions in adrenalec-
tomized animals were abolished when the 'deoxycortone' was dissolved in arachis
oil. They therefore undertook a systematic investigation of the aldosterone-
antagonistic action of various vegetable oils. Consistent and marked antagonism was
seen only with arachis oil at all doses. The potent aldosterone antagonist is believed
to be contained in the unsaponifiable portion of the oil (Kumar et al., 1962).
Manihot esculenta Crantz. syn. (M. utilissima Pohl.) EUPHORBIACEAE

Cassava, manioc
In West Africa this species occurs mainly as the bitter cassava (dark root) but a sweet
variety is cultivated in the northern parts of West Africa. Cassava is a major
foodplant which requires cooking as it contains a thiocyanate which is rendered inert
by heat. Many varieties exist. The meal is called fufu. Gari is a coarse powder
obtained by dry methods of scraping, pounding, etc. A poultice, often used as a
substitute for linseed meal, is put on burns, ulcers, etc. (Dalziel, 1937, pp. 150-4).
Cassava is rich in starch and poor in nitrogen: there is 39% starch, 1.3% protein and
0.5% fat in Ghanaian cassava root after cooking. Linamarin is the source of the
thiocyanate found in manioc meal.
Antithyroid effects of cassava and the thiocyanate were observed in rats. In some
areas of Zaire endemic goitre and cretinism was attributed to endogenous formation
of thiocyanate resulting from ingestion of manioc; this aggravated iodine deficiency
in these areas (Ermans, 1979). In Nigeria a degenerative ataxic neuropathy
(polyneuritis of variable location) with deafness and bilateral optic atrophia in 320
patients could be traced to a chronic intoxication by hydrocyanic acid. The acid
resulted from hydrolysis of cyanogenetic glycosides contained in manioc, which is a
basic food in the country (Osuntokun et al., 1969,1970). Thus chronic intoxications
can result from regular ingestion over long periods from boiled manioc. It had been
observed that increasing thiocyanate in the blood of humans and rats aggravated the
244
loss of iodine from the thyroid. Renal elimination of thiocyanate becomes apparent
when the blood level exceeds 10-15 /xg/ml, 'which was not adequate for prevention
of thyroid anomalies' (Ermans, 1979; Ermans el al., 1980). Ermans et al. (1980)
recommend, in endemic goitre studies, completion of the iodine level examination
by determination of thiocyanate levels in the blood and urine and checking of the
intake of manioc.
Oral hypoglycaemic action
Insulin, a hormone secreted by the /3-cells of the Islets of Langerhans in the

pancreas, is of utmost importance for the correct metabolism of carbohydrates and
fats. It induces the oxidative breakdown of glucose, has a stimulating effect on the
synthesis of liver glycogen from glucose and inhibits the formation of liver glycogen
from protein and fat.
Diabetes, a condition characterized by hyperglycaemia, is caused by insufficient
secretion of insulin or to insufficiency of its peripheral efficacy. Excess of insulin
leads to hypoglycaemia; this is easily counteracted if dextrose or a few lumps of sugar
are taken at once.
Modern investigations into the biochemistry of diabetes show that its causes and
the sites of intervention in the biochemical processes are diverse. Somatostatin, the
pituitary and sex hormones, corticosteroids, prostaglandins and vascular modifi-
cations of the pancreas can all be involved, together with a straightforward inad-
equacy in insulin production (Randle el al., 1963; Gupta et al., 1966; Burkhard etal.,
1968).
A number of plants have constituents which have antidiabetic properties when
taken orally (Oliver-Bever and Zahnd, 1979). There is great diversity in the nature
and action of these constituents, but a number of them do seem to belong to certain
chemical groups, such as sitosterol glycosides, alkaloids, sulphur oils andflavonoids,
and in this chapter I have assembled the plants described into a few groups based on
their possible active chemical constituents while at the same time taking into
consideration their relation to, or identity with, hypoglycaemic plant constituents
found elsewhere. Some of the plants appear to have several constituents, each of a
different chemical group, which may all contribute to their activity.
In each chemical group some details are given on one or a few plants only and the
others are listed in Tables 7.1-7.6. Since a major hypoglycaemic action has been
found in several currently cultivated, introduced plants, which are often foodcrops,
these have also been included.
In an extensive comparative evaluation of Indian antidiabetic plants, including
246
clinical trials, Chaudhury and Vohora (1966) recommended further tests, in order of
prioiity on Momordica charantia, Gymnema sylvestre, Syzygium cumini and Coccinia
indica. These plants and Syzygium guineense varieties (Fig. 7.1) figure also amongst
the plants with possible hypoglycaemic action selected on the basis of the literature
for West Africa and they will be treated in more detail hereunder.
I Plants containing hypoglycaemic phytosterin glycosides

(See Table 7.1.)
The active constituent from the rootbark of hypoglycaemic Ficus species (Ficus
glomerata and F. religiosa) was found in India to be /3-sitosterol D-glycoside; this had
a peroral hypoglycaemic effect in fasting and alloxan-diabetic rabbits and in
Fig. 7.1. Syzygium guineenses. var. littorale Keay.

247
pituitary-diabetic rats comparable to the effect of tolbutamide (Modak and Rajarama

Rao, 1966; Ambike and Rajarama Rao, 1967; Vohora, 1970).
Momordica charantia L. CUCURBITACEAE

African cucumber or balsam pear
The African cucumber, M. charantia, and the allied M. foetida are used in many
countries in folk medicine as a remedy for diabetes.
A hypoglycaemic principle could be isolated from M. charantia fruit and was called
charantin. It appeared to be a phytosterolin (Rivera, 1941, 1942). Sucrow (1965)
found that charantin is a mixture in equal parts of /3-sitosterol-/3D-glucoside and
A5-25 stigmastadien 3/3-ol. 5-Hydroxytryptamine and a-amino-butyric acid have also
been reported to be present in the fruit (Dhalla et al., 1961). The fruit of M. foetida
contains foetidin, which has been isolated and characterized as a chromato-
graphically homogeneous product consisting also of /3-sitosterol-/3D-glucoside and
A5 25-stigmastadien 3/3-ol-glucoside in equal parts and was thus shown to be identical
with charantin (Olaniji, 1975; Olaniji and Marquis, 1975). Recently, a polypeptide
has been isolated from the fruit, seeds and tissue of M. charantia. It has been called
p-insulin and amino-acid analysis has revealed that it has 166 residues composed of
17 different amino acids and a molecular weight of approximately 11000.
Methionine was the only amino acid not also found in bovine insulin (Khanna et al.,
1981). Immunoassays did not, however, indicate any cross-reaction between p-insu-
lin and bovine insulin (Weniger et al., 1982).
Extensive investigations have shown that an extract of the dried fruits of M. charan-
tia has marked hypoglycaemic properties, giving good results in clinical trials (Vad,
1960). Charantin has a more potent hypoglycaemic action than tolbutamide in
equivalent doses. The action is less pronounced in depancreatized cats but seems to
subsit nervetheless, indicating the existence of a slight extra-pancreatic as well as a
pancreatic action. Doses of 400 mg/kg given intraperitoneally are not lethal in mice.
Charantin probably does not account for all the properties of the fruit as the
favourable results obtained from 50-60 ml of fresh juice consumed daily could not
be attributed only to the few mg of charantin the juice contained (Lotlikar and
Rajarama Rao, 1960, 1966; Kulkarni and Gaitonde, 1962). A consistent hypo-
glycaemic effect was produced when 0.5 g of dried powdered fruit of M. charantia
per kg of body weight was given at 10-h intervals to normal and alloxan diabetic
rabbits (Athar, 1979; Akhtar etal., 1981).
Subcutaneous administration of the polypeptide p-insulin isolated from the fruit
produced hypoglycaemic activity in diabetic gerbils, langurs and humans. In
juvenile diabetic patients the peak effect was observed after 4-8 h as compared to 2 h
for bovine insulin (Khanna et al., 1981).
Foetidin from M. foetida has been shown to lower the blood glucose level in
normal rats but, contrary to results published earlier, Marquis et al. (1977) noticed
no significant effect in diabetic animals.
Phytosterin glycosides are found together with an alkaloid in Syzygium cumini
(also containing tannins) and with sulphur compounds in Phaseolus vulgaris.
248 249
Table 7 . 1 . Plants containing hypoglycaemic phytosterin glycosides
Plant Possible active

Family Part used constituent(s) Observed activity References
Hygrophila auriculata Whole The root contains Oral hypoglycaemic action in cats and rabbits; McMillan (1954)
(Schum.) Heine syn. plant 0.25-0.33% lupeol(= through decoction of whole plant, BasuandRakhit(1957)
(H. spinosa And., hygrosterol) and an it is mainly diuretic Chatter jee and Shrimani (1957)
Asteracantha longifolia essential oil. The seeds Govindachari el ah (1957)
Nees, Barleria auriculata contain 4 steroid gluco- Martindale(1958)
Schum., B. longifolia L.) sides (phytosterols), 2 Dhar«a/.(1968,p.365)
Acanthaceae water-soluble bases,
23% semi-drying oil and
enzymes (diastase,
lipase and portease).
The leaves contain the
alkaloid vasicine (=
peganine)
Monwrdica charantia L. Fruit Phytosterin glycosides: 50 mg/kg doses of charantin reduce hyper- Lotlikar and Rajarama Rao (1960,
M.foetida Schum. & charantin, momordicin, glycaemia by 42% in rabbits. Charantin 1966)
Thonn. foetidin. (Foetidin = possesses pancreatic and extrapancreatic action Kulkarni and Gaitonde (1962)
(African cucumber, /3sitosterol,/3D- and is more active than tolbutamide. It has Chatterjee(1963)
Bitter gourd) glucoside plus A5*25 slight antispasmodic and anticholinergic Gupta (1963a)
Cucurbitaceae stigmastadiene-3/8-ol- effects and controls but does not heal diabetic Sucrow(1965)
glucoside patients (160 cases) Olaniji(1975)
Olaniji and Marquis (1975)
Marquis«a/.(1977)
Athar(1979)
Akhtare!a/.(1981)
Pkaseolus vulgaris L. Bean-husks Hypoglycaemic principle An aqueous infusion reduces hyperglycaemia in Hartleb(1932)
Kidney or haricot bean in aqueous infusion mild diabetics and restores carbohydrate Lyass and Vovski (1932)
P. multiflorescens called phaseolan, balance Sachser(1961)
Papilionaceae stigmasterin,
querceturon (glycoside:
quercetin + glucuronic
acid), sulphur
compound, indole acetic
acid oxidase inhibitor
Syzygium cumini (L.) Skeels Seeds Hypoglycaemic principle, In cats and rabbits the alcoholic extract has oral Mercier and Bonnafous (1940)
syn. (S. jambolanum DC., antimellin (glycoside). hypoglycaemic action comparable to that of Venkateswarlu(1952)
Eugenia jambolana Lam., Known constituents in toibutamide. In alloxan-diabetic rats the SepahaandBose(1956)
E. cumini Merr.) seeds: phytosterin, purified principle abolishes hyperglycaemia Nair and Subramanian (1962)
(Jambul, Java plum) jambosine (alkaloid), and glycosuria within seven days. A single dose Mukherjee«a/. (1963)
Myrtaceae jambolan, essential oil, of an aqueous extract of the seeds reduces blood Shrotri<?(a/.(1963)
galli and ellagi-tannins. sugar by 15-2 5% in 4-5 h Sengupta and Das (1965)
Constituent in flowers Sicognau-Jagodzinski el al. 1966)
and fruits: cyanidine-2- Jain and Sharma( 1967)
rhamnoglucoside Laroche Navaron (1968)
250
II Plants containing hypoglycaemic alkaloids

(See Table 7.2)
Catharanthus roseus (L.) Don (Fig. 7.3) APOCYNACEAE

Madagascar periwinkle
In the folk medicine of several countries, such as the Philippines, Jamaica, South
Africa, India and Australia, an infusion of the leaves is given in the treatment of
diabetes.
American research workers, anxious to study the hypoglycaemic properties of this
plant, lost a great many rats which had been given an extract of the leaves through
Fig. 7.2. Securinega virosa (Roxb. ex Willd.) Baill.

251
Pseudomonas infection. Investigation revealed that the rats had forfeited their
resistance to a severe fall in the number of their lymphocytes. This discovery led to
research into the treatment of leukemia by Catharanthus alkaloids (Noble et at.,
1958).
Research on the hypoglycaemic effect was not abandoned, however, and the
different Catharanthus alkaloids were administered in doses of 100 mg/kg to rats with
fasting hyperglycaemia. Three of the alkaloids, leurosine, vindoline and vindolinine,
proved more potent than tolbutamide at equivalent doses, whilst three other
alkaloids had a less pronounced effect (see Table 7.2). Leurosine alone had a slight
effect on cell division. Before possible use in diabetes the hypoglycaemic alkaloids
will have to be completely isolated from the others as many of these are cytotoxic
(Svoboda etal, 1964).
Fig. 7.3. Catharanthus roseus (L.) Don.

252 253
Table 7.2. Plants containing hypoglycaemic alkaloids or amino acids
Plant
Family Part used Constituents Observed activity References
Catharanthusrosem Leaves Hypoglycaemic alkaloids: The action of (4), (5) and (6) is stronger than that Noble«a/.(1958)
G. Don syn. (Lochnera catharanthine(HCl)(l), of tolbutamide at equivalent doses. 1-3 had a Mukherjeeera/. (1963)
rosea (L.)Reichb., lochnerine (2), tetra- less pronounced action. The hypoglycaemic Shrothri era/. (1963)
Vincaroseah.) hydroalstonine (3), effect starts slowly and is relatively long lasting Svoboda era/. (1964)
(Madagascar periwinkle) leurosine sulphate (4), Svoboda(1969)
Apocynaceae vindoline(HCl)(5),
vindolinine(2HCl)(6)
Anthocyanins in the leaves
Lupinus lassilicus Maire Seeds Sparteine and lupanine in Alkaloids are moderately hypoglycaemic in Shani era/. (1974)
syn. (L. termis Forsk.) hypoglycaemic fraction alloxan-diabetic but not in normal rats. Short
Fabaceae (quinolizidine alkaloids) lasting effect
Securinega virosa (Roxb. ex Seeds Hypoglycaemic fraction: In doses of 0.5 mg/kg both extracts produce in cats KjaerandFriis(1962)
Willd.)Baill.syn. alcoholic and aqueous and rabbits a decrease of blood sugar level Satoda(1962)
(Fluggea virosa (Roxb. ex extracts of seeds lasting for about 4 h Iketobosin and Mathieson (1963)
Willd.)Baill.,F.m!cro- Known constituents: Hericz era/. (1964)
carpa Blume, S. micro- numerous alkaloids in Saitoera/.(1964a,b)
carpa Pax and Hoffm., this and allied spp. Chatter jee and Roy (1965)
Phyllanthus virosus Roxb. (fluggeine, securinine,
exWilld.)(Fig.7.2) norsecurinine, virosine,
etc.)
Euphorbiaceae
7>tt>masrans(L.)H.B.K. Leaves Alkaloids: tecomine and Tecomine (citrate) and tecostanine (hydro- Garcia and Colin(1926)
Bignoniaceae tecostanine chloride) given perorally (both in doses of Guerra(1946)
20 mg/kg, calculated on the free base) to Hammouda and Motawi (1959)
alloxan-diabetic rabbits seems rather untoxic Hammouda era/. (1963,1964)
but do not act in total absence of active /3 cells Jones era/. (1963)
of the pancreas Hammouda and Amer (1966)
Hammouda and Khallafallah(1971)
TrigonellafoenumgraecumL. Seeds Alkaloid: trigonelline Used in Israel as an oral insulin substitute. In rats Sulman and Menczel (1962)
Fabaceae (N-methylnicotinic trigonelline counteracts the hyperglycaemic Menczel era/. (1965)
acid). effect of cortisone given 2 h before or simul- Mishinsky era/. (1967)
Also coumarin and taneously. It produces a variable effect in Varsneyand Sharma(1968)
nicotinicacid alloxan-diabetic rats and in diabetic patients. Hardman and Fazli (1972)
Nicotinic acid has a stronger hypoglycaemic Shani era/. (1974)
action but of shorter duration whilst the effect
of coumarin in diabetic rats persists for 24 h
Hordeum vulgareh. syn. Germinating Hypoglycaemic principle Hypoglycaemic, reduces blood sugar level in DonardandLabbe(1933)
(H. sativum Pers.) seeds has to be freed from fasting rabbits by 37.9% and in diabetic Labbe(1936)
(Barley) (radicle) hyperglycaemic patients by 25%. Produces strong reduction Dhare(a/.(1968)
Gramineae fraction (sugars and in elimination of acetone and oxybutyric acid,
hordenine) and which occurs in diabetic patients, and improves
vitamin B. general condition. Is also diuretic and emollient
Known constituents.
alkaloids; hordenine,
gramme; others:
amylase, vitamins of
groupB,glucides,
protides, lipids
Blighia sapida Koenig Fruit aril Hypoglycin A = aamino- Hypoglycins active in most animals; act also in Holtera/. (1956,1966)
(Akee apple) and seeds 2-methylene-L-cyclo- depancreatized and adrenalectomized rats. Goldner(1958)
Sapindaceae propylpropionic acid The hypoglycins block oxidation of long-chain Ucciani era/. (1964)
Seeds only Hypoglycin B = y- fatty acids leading to loss of energy production Sherrat era/. (1970)
glutamyl-hypoglycin A for the organism, which reacts by increasing Ashurst(1971)
oxidation of glucose. Hypoglycin B produces Persaud(1972)
congenital malformations
254
Hypoglycaemic alkaloids are also reported in Tecoma stans (sometimes cultivated in

West Africa). A hypoglycaemic betain was isolated from Trigonella foenum-graecum
and called trigonelline; it is a methylbetaine of nicotinic acid and was considered to
be the active constituent of fenugreek until 1974. Shani etal. (1974) then found that
coumarin and nicotinic acid seemed to be the main hypoglycaemic constituents of all
components isolated from the active fraction of the seeds. Trigonelline was found to
be less effective but more persistent in its action. The seeds also contain sterols.
Many other hypoglycaemic plants contain alkaloids but it has not been shown that
these are the active constituents (e.g. Hordeum vulgare).
Some active plant constituents contain amino nitrogen, e.g. hypoglycins in
Blighia sapida. They are, unfortunately, too poisonous for clinical use. Their
interest lies in the knowledge acquired about the ways in which they act.
Blighia sapida Koenig (Fig. 7.4) SAPINDACEAE

Akee apple
The ripe fruit is edible and tastes much like a chestnut, but is poisonous if immature
or decaying (ichthyotoxic in Africa). In Jamaica there used to be annual epidemics
of 'vomiting sickness', which were marked by vomiting, prostration, convulsions
and finally coma. This condition was eventually traced to the ingestion of unripe
akees, and in particular to the ingestion of two constituents, hypoglycin A and
hypoglycin B. These substances have strong hypoglycaemic and emetic action in
most animals and Man. Hypoglycin A has proved to be twice as active as hypoglycin
B. However, the livers of animals treated by these substances show fatty degener-
Fig. 7.4. Blighia sapida Koenig.

255
ation and reduced glycogen content. Hypoglycins appear to act through inhibition
of the /3-oxidase enzymes, thereby blocking the oxidation of long-chain fatty acids;
this causes accumulation of unmetabolized fatty acids and makes them unavailable
for energy production. The organism reacts by oxidizing glucose in large quantities,
thus causing a decrease in liver glycogen and a drop in blood glucose to hypo-
glycaemic levels (Tanaka et al., 1972).
Ill Plants containing hypoglycaemic organic sulphur compounds

(See Table 7.3.)
Allium cepa LILIACEAE

Onion
(See also Chapters 2 and 4). Already in 1923 Collip noticed that a totally (?)
depancreatized dog could be kept alive for 66 days on three injections of crude onion
extract. Later, a number of research workers confirmed that the onion and its
extracts have a distinct, slowly developing hypoglycaemic action and that the effect
is also obtained when the extract is given by mouth (Hermann, 1956, 1958; Jain and
Vyas, 1974).
The action of a petroleum ether extract of sliced dried onion was equivalent to 62%
of that of a standard dose (0.5 g) of tolbutamide and further purification led to an
extract equivalent to 76.6% of this standard) (Brahmachari and Augusti, 1962).
Later, two active disulphides were isolated from fresh onions by steam distillation
and solvent extraction. They were allyl propyl disulphide (APDS) and allicin (diallyl
disulphide oxide) (Augusti and Benaim, 1974; Augusti, 1975, 1976a, b; Augusti et
al., 1975).
With APDS, blood glucose and glycosuria were significantly decreased in alloxan-
diabetic rabbits and glucose tolerance was also improved. In a 4-h test in fasting
human subjects APDS caused a marked fall of blood sugar (hourly controls) plus an
increase of serum insulin levels, whilst the free fatty acid levels remained the same.
In a control trial there was no fall of blood glucose, but the serum insulin levels
decreased and the free fatty acid levels increased considerably.
The authors (Augusti and Benaim, 1974; Augusti, 1976a, b) explain these results
as follows. Insulin is a disulphide protein and its inactivation by compounds and
albumins rich in SH groups has been established. APDS probably removes insulin-
inactivating compounds by competing with insulin for the SH group(s) in these
compounds, thus producing an insulin-sparing effect and preventing the increase of
free fatty acids on fasting.
In clinical trials, 100 mg allicin per kg body weight produced a significant drop in
fasting blood glucose levels with a concomitant rise in serum insulin levels. In 12
subjects the action lasted for about 12 h. Long-term feeding to normal rats of 100 mg
of allicin per kg of body weight produced a large reduction in the lipid constituents
of the blood and liver and in this respect allicin might have an advantage over
tolbutamide (Augusti and Benaim, 1974). Cyanidin- and paeonidin-glycosides are
also present in onion bulbs, and could well be partly responsible for the effect of the
crude extract.
Table 7.3. Plants containing hypoglycaemic organic sulphur compounds

Family Part used constituents Observed activity References
AlliumcepaL. Bulbs Allyl propyl disulphide In fasting humans, APDS in doses of 0.125 g/ Bhandahari and Mukerje (1959)
(Onion) (APDS),allicin(diallyl 50 kg produced a significant fall of hyper- Brahmachari and Augusti (1961a, b,
Liliaceae disulphide oxide), glycaemia, a rise in serum insulin levels and no 1962a)
methylalliin in fresh change in free fatty acid levels. APDS is Jain and Sharma (1967)
juice (latter also believed to remove insulin-inactivating Augusti and Benaim (1974)
bacteriostatic) compounds by competing with insulin for the Jain and Vyas( 1974)
Also in bulbs: flavon SH group, thus having an insulin sparing Augusti (1975,1976a, 1976b)
glycosides; kaempferol, effect. Augustiâl. (1975)
quercetin- and The activities of petroleum ether and ethyl ether Matthew and Augusti (1975)
phloroglucin- extracts of sliced dried onion were equivalent
derivatives to 62 and 76% of that of a tolbutamide standard
respectively. APDS does not act in totally
depancreatized rabbits
Allium sativum L. Dried flower Organic sulphur The activity of an ethyl ether extract of dried A.
(Garlic) heads compounds sativum heads is 58% of that of a tolbutamide
Liliaceae standard
Brassica oleraceaeh. var. Leaves Hypoglycaemic fraction, Hypoglycaemic principle tied to a hyper- MacDonaldand Wislicki, (1938)
capitataL,. called vegulin, loses glycaemic fraction from which it can be Lewis (1950)
(Cabbage) activityinl month. separated Johnsons al. (1971)
Cruciferae Thioglycosides (methyl Vohora etal. (1973)
and ethyl propyldi-
sulphides and goitro-
genic indole-myrosin
glycoside (neo-gluco-
brassicin)
257
Garlic (Allium sativum) (Brahmachari and Augusti, 1962b), Brassica oleraceae and
Phaseolus vulgaris also contain organic sulphur compounds.
Allium cepa,A. saliva, Brassica oleraceae, Phaseolus vulgaris and some non-African
plants contain, in addition to a hypoglycaemic factor, a hyperglycaemic factor; this
has to be eliminated before the hypoglycaemic effect can be estimated. This
simultaneous presence of the two antagonistic factors could explain the discrepancy
in results obtained in older publications.
IV Hypoglycaemic plants containing anthocyanins, catechols or
flavonoids, or their glycosides and/or tannins (See Table 7.4)
In diabetic patients the basal membrane of the small blood vessels, which has an
important metabolic function, is thickened (by an accumulation of glycoproteins),
thus causing a disturbance of metabolic exchange. Also, the capillary wall becomes
permeable (diabetic angiopathy). It has been shown that Vaccinium anthocyanosides
can inhibit or slow down this evolution of the capillary walls particularly at the onset
of the diabetic disease process. Treatment over 6 months (a starting dose of 600 mg
per day) reduces the number of affected capillaries from 34 to 24% and the average
surface of glycoprotein accumulation from 14 to 8 jitm (Pourrat, 1977; Pourrat etal.,
1977, 1978).
The active constituent of Euopean Vaccinium myrtillus berries has proved to be a
glycoside of 7-methyl-delphinidin and the traditional use of the berries in the
treatment of diabetes in Europe has been justified by pharmacological and clinical
trials which have shown that the effect of a single dose can last up to two weeks and
more. The active principle allowed a gradual decrease in the use of insulin in a
number of patients (Allen, 1927).
In West Africa several antidiabetic plants with similar constituents have been
reported. Thus leucodelphinidin and leucocyanidin are found in the flowers and also
in other parts of banana plants and Musa sapientum pigment contains deoxyxanthin
cyanidin.
In evaluating the hypoglycaemic effect of extracts or products of 56 Indian plants
reputed to be antidiabetic in native medicine, by their reduction of the normal
fasting blood-sugar level in rabbits, Jain and Sharma (1967) found that an extract of
the flowers of a variety of M. sapientum (Ney Poo van) was second in order of efficacy
(Allium cepa being first).
A solution of 10 mg/kg of the dried residue of this extract produced a
hyperglycaemia of 15-24 mg, compared to one of 20-30 mg for Allium cepa, one of
12-23 mg for Syzygium cumini, one of 13-21 mg for Ficus glomerata and one of
10-18 mg for both Momordica charantia and Gymnema sylvestre.
Saponifiable and mainly non-saponifiable fractions of the extract of the flowers of
Musa sapientum var. Ney Poovan have hypoglycaemic properties.
The leaves of Morus alba contain cyanidin and delphinidin glucosides in addition
to phytosterol glycosides. Similarly, in the fruits and seeds of Syzygium cumini
(Table 7.1), which are used as antidiabetics, cyanidin rhamnoglucosides and galli-
and ellagi tannins, respectively, are found, as well as phytosterol glycosides (Ven-
kateswarlu, 1952).
258 259
Table 7.4. Hypoglycaemic plants containing anthocyanins, catechols orflavonoids, or their glycosides and/or tannins

Family Part used constituents Observed activity References
Anacardium occidenlalel*. Leaves Quercetin and kaempferol The glycoside fraction normalizes glycaemia Dhar etal. (1968)
Anarcardiaceae glycosides Laurens and Paris (1976)
Brideliaferruginea Benth. Bark, roots, Tannins, flavonoids and Injection of water and methanol extracts of leaves Githens(1949)
Euphorbiaceae leaves biflavonoids based on lowers hyperglycaemia in fasting rats, but only Iwu (1980,1983)
apogeninand protects alloxan-diabetic rats when given 1 h
kaempferol moieties before alloxan. In clinical trials 8 out of 10
patients saw their blood sugar reduced from
230 mg% to under 120 mg% when taking a
decoction or maceration of the leaves perorally
Ceiba pentandra (L.) Juice, roots, Quercetol and kaempferol The glycosides are reported to be antidiabetic in Currie and Timell (1959)
Gaertn. syn. (Eriodendron bark glucosides, traces of India, needs checking
anfractuosum DC.) gossypiol, methylglucu-
(Silk cotton tree) ronoxylan. In the seeds,
Bombacaceae ySsitosterol
Centaurea perrottetti DC. Inflorescence Centaurea spp. contain The peptide fraction reduces glycaemia in rabbits LaboandPuig(1953)
syn.(C. asperaL., glycosides of flavones by 28-42 mg/24h Viguera and Casabuena (1965)
C. cakitrapa Chev., (apigenin, baicalein, Centaurin has antibiotic properties, mainly Ahmed«a/.(1971)
C. alexandrinaL.) luteolin, etc.) and/or of towards Brucella Monya and Racz (1974)
Compositae flavonols (centaureidin, Masso«a/.(1979)
jadein, quercetin). They
also contain /3-sito-
sterin, /3-amyrin,
peptides,cnicin(=
centaurin (sesquiter-
penic lactone) and an
alkaloid, stizolphine
CocciniagrandisL. Voigt Tuberous There is a hypoglycaemic Hypoglycaemic effect of alcoholic extract in Chopra etal. (1956)
syn. (C.indicaW& A., roots fraction in alcoholic rabbits = 58.9% of that of tolbutamide. Effect Currie and Timell (1959)
Cephalandra indica and aqueous extracts of in alloxan-diabetic rabbits is comparable to that Brahmachari and Augusti (1963)
Naud.,C. cordifolia(L.) roots. Known constitu- of tolbutamide De and Mukher jee (1963)
Cogn.) ents of roots: caffeic Trivedi(1963)
Cucurbitaceae acid, quercetin, Jain and Sharma (1967)
kaempferol, /3-sitosterol MukerjeeandGhosh(1972)
Morusalbah.. Leaves Hypoglycaemic fraction = Leaf extracts are hypoglycaemic in tests in rats Leclerc(1934)
M. nigrah.. alcoholic and aqueous with experimental diabetes and in the fasting Sharaf and Mansour (1964)
(White and black extract of leaves. animal, increases glycosuria. Has also slight, Talyshinski(1967)
mulberry) Known constituents: antispasmodic and hypotensive action. Deshpande(1968)
Moraceae cyanidin and delphin- Naito(1968)
idin glucosides, rutin, Nomora and Fukai (1981)
moracetin (= quercetin
triglycoside), /3sito-
sterin,sitosteryl-
carpate and palmitate
Musa paradisiaca L. var. Juice of Liquid extract of flowers, The extract of the flowers is hypoglycaemic in Hood and Lowburry (1954)
sapientum (L.) Kuntze flowers mainly 3rd fraction of tests on fasting rabbits (reduction of 15-24 mg Simmonds(1954)
syn. (M. sapientum (L.)) non-saponifiable in blood sugar) Sinha«a/.(1962)
(Banana) portion, is hypo- Jain (1968)
Musaceae glycaemic. In bracts, Jain (1969)
anthocyanidins; in
fruits, hydroxytryp-
tamine,glucides
Phyllanthus niruri L. Leaves Flavonoids (phyllanthin Antidiabetic in India, needs checking Vila (1940)
Euphorbiaceae and hypophyllanthin), Krishnamurti and Seshadri (1946)
lignanes, quercetoside Jain and Sharma (1967)
4 alkaloids (norsecuri- Stanislas etal. (1967)
nine isomers). In the Dhar el al. (1968)
barkrlupeol Rouffiac and Perello (1969)
Nara«a/.(1977)
Rhizophora racemosa Mey. Bark, roots Tannins and catechins A decoction is hypoglycaemic in diabetes in India McMillan (1954)
and spp. (15-42%) Chopra <« a*. (1956,p.212)
(Mangrove) Jain and Sharma (1967)
Rhizophoraceae
Sclerocarya birrea (Rich.) Leaves Tannins and flavonoids A decoction or maceration of the leaves is Busson(1965)
Hochst. syn. (Spondias distinctly hypoglycaemic when administered Gueye(1973)
birrea Rich., Poupartia by mouth or intraperitoneally. Low toxicity
birrea (Rich.)Aubrev.) in rats
Anacardiaceae
Scoparia dulcis L. Whole plant Hypoglycaemic bitter Reduces hyperglycaemia and glycosuria in human Nath(1943)
(Sweet broom weed) principle named diabetics. When chewed, plant tastes bitter, Nath and Bannerjee (1943)
Scrophulariaceae amellin. Known then sweet Nath and Chowdurry( 1943,1945)
constituents: scoparol Nathrta/. (1943,1945)
(=3'O-methyl- Whittacker(1948)
luteolin), Scoparoside
(=8glycosyl-scopanol)
260
In France a hypoglycaemic drug based on Syzgium has been put on the market:
14 g of active substance are obtained from 100 g of dried seeds by triple extraction
using 95% alcohol or boiling water. (It is used in doses of 1-2.5 g/day; the LD 50 in
mice is 4 g/kg). Hypoglycaemic action, possibly through flavonoids and tannins, has
been found in the bark and roots of Bridelia ferruginea and Rhizophora mucronata and
in the leaves of Sclerocarya birrea.
Bridelia ferruginea Benth. EUPHORBIACEAE

The bark, leaves and roots of this tree are ingredients of the Yoruba agbo infusion
and are used in the preparation of a popular mouthwash and as a remedy for thrush
in children. The roots are used as a chewstick and in Togo externally for the
treatment of skin diseases and eruptions. In Northern Nigeria it is also used as an
antidote to arrow poison (Dalziel, 1937, p. 137). In the Congo the bark is used as an
anthelmintic for roundworm and is given in the treatment of cystitis (Githens, 1949).
Tannins have been reported to be present in the bark (Githens, 1949) and roots of
both B. ferruginea and Rhizophora mucronata. Flavonoids and biflavonoids based on
apigenin and kaempferol moieties were isolated together with their glycosides from
the methanolic extract of this plant. 'It is however not clear which of these
compounds is responsible for the antidiabetic properties of this plant' (Iwu, 1983).
An ethyl acetate-insoluble fraction yielded coumestans (Iwu, 1983).
One hour after intraperitoneal injection or oral administration of leaf extracts to
12-h-fasted albino rats there was a significant reduction in fasting blood sugar but the
animals were not protected against alloxan-induced diabetes. There was, however,
a significant reduction in the expected hyperglycaemia in alloxan-diabetic rats when
administration took place 1 h before alloxan injection. (The extracts were water and
methanol extracts.) Clinical evaluation at a herbal home has revealed that eight out
of ten patients benefited from Bridelia therapy. Their blood sugar was reduced from
230 mg% to less than 120 mg% and remained at this level for 8 weeks after they had
taken daily a decoction or maceration of the leaves perorally (Iwu, 1980).
Sclerocary a birrea (Rich.) Hochst. syn. (Spondias birrea Rich., Poupartia birrea
(Rich.) Aubrev.) (Fig. 7.5) ANACARDIACEAE
Locally a fermented beverage like cider is prepared from the expressed juice of the
fruit. The tree is mainly found in Northern Nigeria, Ghana and Gambia, and the
Hausas use a cold infusion of the bark along with native natron as a remedy for
dysentery. The leafy branches are cut for fodder during periods of drought (Dalziel,
1937). In Senegal the leaves and rootbark are used together with Securidaca
longepedunculata, sometimes mixed with other plants as well, as a plaster against
venoms, e.g. those in snake bites (Kerharo and Adam, 1974).
Analysis of the leaves revealed the presence of tannins and flavonoids. No alkaloids,
steroids or triterpenoids were detected (Gueye, 1973). The fruit is rich in vitamin C,
but the juice is rather toxic. The seeds are rich in oil, mostly oleic acid (64%) but also
myristic and stearic acids. They also contain amino acids with a predominance of
glutamic acid and arginine (Busson, 1965).
261
A decoction or maceration of the leaves of the tree has a distinct hypoglycaemic

action when administered by mouth or intraperitoneally. The extracts show low
toxicity in rats. The leaf extract is believed to have a direct action on the glycaemia-
regulating system as well as a stimulating action on the peripheral assimilation of
glucose, in particular by the muscular tissues (Gueye, 1973).
Some plants contain quercetin-, kaempferol- and/or luteolin-glycosides as active
constituents. Examples are Anacardium occidentale, Ceiba pentandra, Centaurea
perrottetti, Coccinia grandis, Phyllanthus niruri and Scoparia dulcis. The activity of two
of these plants reputed to be antidiabetic in Indian folk medicine, Ceiba pentandra
and Phyllanthus niruri, needs scientific confirmation according to Jain and Sharma
(1967).
Fig. 7.5. Sclerocarya birrea (Rich.) Hochst.
m -
262 263
Table 7.5. Hypoglycaemic plants containing other active constituents
Plant
Family Part used Known constituents Observed activity References
Azadirachta indica Juss. Leaves Acetylnimbin, nimbolid Fresh leaf extract is hypoglycaemic in dogs with Luscombe and Taha (1974)
Meliaceae (lactone) adrenaline- or glucose-hyperglycaemia when See also Chapter 4
given by intravenous injection
Corchorus olitorius L. Leaves A hypoglycaemic extract An aqueous extract decreases hyperglycaemia in Uzan and Dziri( 1952)
(Jute) free from pectins, sugars mice, guinea-pigs and rabbits. It does not act in Frere jacque and Durgat (1954)
Tiliaceae and fats, contains traces the absence of the pancreas; it promotes the Peters(1957)
of elemental sulphur degradation of glucose in vitro Goldner(1958)
and zinc. There are Samilova and Lagodich (1977)
cardiac glycosides in the
seeds (corcherosides A
and B, their genin is
strophanthidin
olitoriside)
Lagerstroemia spectosa (L.) Old leaves Thermostable hypo- A decoction of 20 g of dried leaves has an activity Garcia(1941)
Pers. syn. (L.flosregina and ripe glycaemic principle. equivalent to 6-7.7 units of insulin. Even high
Retz.) fruit Terpenes and saponins doses are not toxic
Lythraceae in the leaves
Muc una pruriens (L.) DC. Seeds A powder of the decoated When the powder formed 96.5% of the diet (+ salt MajumdarandZalani(1953)
var. pruriens syn. (Dolichos seeds contains 27% and vitamins), it produced a lowering of 39% Dhar«la/.(1968)
pruriens\,.) protein ,8.3% lipids, of the blood sugar, as compared to standard Pamela/. (1968)
(Cow-itch) 47.8% carbohydrates, diet, in fasted rats and a lowering of 61 % of the Ghosalela/.(1971)
Fabaceae two alkaloids (mucunine cholesterol level
and mucunadine) and
two soluble bases
(prurienine and
prurienivrine)
Vigna unguiculata (L.) Walp. Seeds A powder of the decoated When the powder formed 96.5% of the diet, it Pamela/. (1968)
syn. (Dolichos unguicu- seeds contains 19% produced a lowering of 42% of the blood sugar Kerharo and Adam (1974,
latusL.,D. biflorusL.,D. protein, 2% lipids, of fasted rats and a lowering of 26.7% of their pp. 480-1)
sinensisL., V. sinensis(h.) 53.18% carbohydrates; cholesterol level Telia and Ojihomon (1980)
Savi & Hask) the 'mineral content' is
Fabaceae 0.1-0.2% calcium,
0.37% phosphorus and
traces of iron and
vitamins
264
V Hypoglycaemic plants containing other active constituents

(See Table 7.5).
Among these we find Azadirachta indica and Gymnema sylvestre. The hypoglycaemic
effect in dogs with adrenaline- or glucose-induced hyperglycaemia of the intravenous
injection of a fresh-leaf extract of A. indica has been reported by Luscombe and Taha
(1974). However, the need exists mainly for oral antidiabetics. The leaves contain
acetylnimbin and a lactone, nimbolid.
The leaves of Gymnema sylvestre, which are chewed in India to reduce glycosuria,
normalize the blood sugar in diabetic subjects in about 3-4 weeks, but when they
were used in combination with insulin a prompt response was observed where
insulin alone in that particular dose had failed (Gupta, 1961). The active principle
has been called gymnemic acid and consists of a complex mixture of heterosides of
diverse organic acids. Administration of the dried leaf powder regulates the blood
sugar levels also in alloxan-diabetic rabbits and increases the activities of the
enzymes commanding the utilization of glucose by insulin-dependent pathways.
Thus control of phosphorylase levels, gluconeogenic enzymes and sorbitol dehydro-
genase has been observed. G. sylvestre appears to correct the metabolic derangements
in the diabetic liver, kidneys and muscles (Shanmugasundaram et at., 1983).
G. sylvestre and Scoparia dulcis are taste-modifiers, a property which is also found
in sweetening agents. The latter are a useful contribution to the diet of diabetics and
are discussed briefly below. The powdered seeds of two Fabaceae, Mucuna pruriens
and Vigna unguiculata, have been shown to lower the level of cholesterol as well as
that of the blood sugar.
VI Mechanism of action of hypoglycaemic plants

The plant constituents which have a hypoglycaemic action act in various
ways. We have seen that plants rich in organic sulphides seem to remove insulin-inac-
tivating compounds through their SH groups by competing with insulin, which is a
disulphide protein, for the SH groups in these inactivating compounds. Similarly,
nicotinic acid is known to be an insulinase inhibitor (Ben David et al., 1963).
We have also seen that anthocyanosides appear to act by improving the vasculariz-
ation of the pancreas. Insulin is fixed on proteins at the surface of the cells, thus
cellular membranes play an important part in diabetes. Vascular troubles develop
gradually during the course of the disease, entailing a thickening of the basal
membrane of the walls of the small blood vessels and an increase of their permeability
(Osuntokun, 1975). Anthocyanosides have been found to inhibit or slow down these
changes in the capillary walls, especially in the early stages of the disease. Thus the
improvement in a patient's condition that is obtained thanks to some plants rich in
anthocyanosides might possibly be due to recovery of the vascularization of the
pancreas. Other plant flavonoids, which also appear to act on the capillaries, could
have a similar effect.
In a number of cases the plants seem to intervene in oxido-reduction phenomena.
We have seen that hypoglycins appear to act through inhibition of the /3-oxidase
265
enzymes. Galegine, like synthetic biguanides, acts in blocking oxidative enzymes of

the Krebs cycle (succinic dehydrogenase and cytochrome oxidase), thus increasing
anaerobic glycolysis and decreasing gluconeogenesis, and entailing an increased rate
of transfer of glucose from the blood to tissues (see also Oliver-Bever and Zahnd,
1979).
The action of other plants seems to be related to the quantities of metal ions or
plant-growth regulators they contain (see Oliver-Bever and Zahnd, 1979).
It thus seems that hyperglycaemic patients can be treated by a variety of plants
which are active at different points in the glucose-metabolism cycle; the success of
the treatment may well be governed by the particular abnormalities of the individual
case.
The majority of the plants mentioned are moderate in their effects and can be
useful in mild cases of diabetes; their use might perhaps be combined with a diet that
is poor in glucides. In some instances their prolonged administration might delay the
establishment of a more serious diabetic condition. In more severe cases of diabetes,
these plants might constitute a form of secondary therapy, with the resul1: that the
frequency or dosage of insulin (or other orthodox drugs) could be reduced.
Several of these plants depend for their efficacy on the presence of insulin, be it
exogenous or endogenous.
VII Sweetening agents
Abrus precatorius L. PAPILIONACEAE

This slender climber is rendered conspicuous by its red seeds, which are black at the
base and visible among clusters of ripe, burst beans. These seeds are used locally as
beads and in the manufacture of masks and shields and are so similar in size and
weight that they were employed in Ashanti (Ghana) and in India as standard weights
by goldsmiths.
Only the leaves (but to some extent also the roots) can be used as sweetening
agents, which is what concerns us here. The dried leaves contain 6-10% of
glycyrrhizin; the dried roots contain 1.5%. This saponoside, first found in the roots
and rhizomes of liquorice, is a diglycuronide of glycyrrhetic acid. The substance is
widely used as a sweetening agent, being sixty times sweeter than saccharose (Milhet
et al., 1978). It also has anti-inflammatory, expectorant, antitussive and antibiotic
properties. During prolonged intake glycyrrhetic acid produces oedema through
water retention with retention of sodium and chloride ions (Na + and Cl") and
increased elimination of potassium ions, (K + ), an effect similar to that produced by
cortisone.
In France the cultivation and propagation of Abrus in greenhouses as a source of
extraction of glycyrrhizin was studied by Milhet and coworkers in 1978.
The seeds contain a highly toxic protein, abrin, and have been used to treat
trachoma and certain forms of cancer (Dupaigne, 1974).
266
Dioscoreophyllum cumminsii (Stapf) Diels MENISPERMACEAE

The most potent sweetening agent known today seems to be the protein isolated
from the berries of Dioscoreophyllum. This is a high forest climber found from Guinea
to the Cameroons. The red berries of this tree have been called 'serendipity berries'
as their intensely sweet taste was discovered fortuitously. The active principle, first
reported by Inglett and May (1968, 1969) was isolated by van der Wei (1972) but is
as yet difficult to obtain in any great quantity. It is a basic protein with a net positive
charge at neutral pH; it has been called monellin and has a sweetness relative to
sucrose on a weight basis of 3000 and on a molecular weight basis of about 9000.
Monellin loses its sweetening ability above pH 10 and below pH 2 and the tertiary
structure is important with regard to this sweetening property, as has been shown by
denaturation of the protein (van der Wei, 1972).
Preliminary trials have shown that monellin is a useful adjunct in the preparation
of drinks poor in calories and in non-glucidic diets. Being required in low concentra-
tions only, it is likely to prove completely inoffensive.
Synsepalum dulcificum (Schum. & Thonn.) Daniell. syn. (Richardella dulcifica)

SAPOTACEAE
The small, red, single-seeded fruits of this small tree are commonly called 'miracul-
ous berries'. Their pulp is used locally to sweeten palm wine and imparts a sweet
taste to anything eaten soon afterwards. The sweetening agent is a glycoprotein
which was named miraculin by Brouver et al. (1968). Miraculin has a molecular
weight of 44000 and the constituent sugars are arabinose and xylose. It causes sour
substances and acids to taste sweet for up to several hours after a 2.3 x 10~ 6 M
solution of it is held in the mouth for 5 min. After this time the sensitivity to acid
taste is recovered. Salt and bitter tastes are not affecied (Brouver et al., 1968;
Kurihari and Beidler, 1968). Miraculin is also said to be an appetite depressant and
a patent has been issued for its use as an anorexic agent.
Miraculin is thought to modify the taste receptors of the tongue, which take a
certain time, varying with the individual, to recover their acid taste sensation
(Kurihari and Beidler, 1968, 1969; Morris and Juscy, 1976).
Thaumatococcus daniellii (Benn.) Benth. MARANTHACEAE

Miraculous fruit
This is a herb which grows up to ten feet tall and has papery leaves that are commonly
used to wrap kola or food. In the crimson, underground fruits, an intensely sweet
substance, which is used locally to sweeten palm wine or acid fruits; is formed. It is
found in the jelly-like aril surrounding the hard black seed and has been called
thaumatin (Inglett and May, 1968). Van der Wei and Loeve (1972) found that the
sweet substance consisted of two proteins with almost identical amino acid compo-
sition; and molecular weights of 21000 and 20 000. Thaumatin loses sweetness below
pH 2.5 and upon heating, reduction of disulphide bonds or when digested by
proteolytic enzymes. It is somewhat similar to liquorice in taste and is said to be 1600
267
times sweeter than saccharose by some and 4000 times sweeter than saccharose by
others. Adesina and Harborne (1978) identified the polyphenols occurring with the
protein sweetener and found flavonol and flavones, apparently absent in the fruits,
in other parts of the plant.
A possible connection between electrostatic charge and taste activity might be
explored as the three taste-active proteins, monellin, miraculin and thaumatin, all
have isoelectric points in the alkaline region (Morris and Juscy, 1976).
NOTES
Chapter 2: The cardiovascular system

1 Arrow poisons were prepared by rubbing certain seeds between two stones until they formed a
paste to which were added saliva and the juice of different toxic plants. A vesicant latex, for
example from Euphorbia, was often used as this damaged the skin, thus facilitating penetration
and absorption (Dalziel, 1937).
2 In trials by ordeal (e.g. trial of Lander in Badagry in 1827) a man suspected of evil influence or
action was forced with much ceremony to swallow a dose of poison. If he survived it was the
wish of the tribal gods and he was considered innocent. If he died this was evidence of guilt
(Dalziel, 1937).
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Chapter 4: Anti-infective activity ofhigher plants

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BOTANICAL AND GENERAL INDEX
Main entries are italicized, synonyms are not italicized.
Species Common name Family Page
Abrus precatorius L. Crab's eye, lucky Fabaceae 224,230,265

bean
Acacia farnesiana (L.) Willd. c. Cassie flower Mimosaceae 174
Acacia nilotica (L.) Willd. ex Del. var. Mimosaceae 167,174,184
nilotica
Acalyphawilkesiana M.ul\. Arg. c. Acalypha Euphorbiaceae 142
Acanthospermum hispidum DC. Star bur Compositae 144
(A. humileChev.)
Achyranthes aspera L. Amaranthaceae 45,72,144,224,
A. repens L. (see Alternanthera) 235
Adansonia digitata L. Baobab, Monkey Bombacaceae 49
bread
AdenantheratetrapteraSchum. &
Thonn. (see Tetrapleura)
Adenia cissampeloides (Planch, ex Benth.) Passifloraceae 45
Harms
Adeniumhonghel DC. (see
A. obesum)
Adeniumobesum (Forsk.)Kocm. & Liar tree Apocynaceae 14,20
Schult.
Adhatoda diffusa Benth.
(see Justicia insularis)
Aegle barteri Hook, f. (see Afraegle
paniculata)
Aeschynomene indica L. Fabaceae 226
Afraegle paniculata (Schum. & Thonn.) Rutaceae 206
Engl.
Afrormosia laxiflora (Benth. ex Bak.) False Dalbergia Fabaceae 70,184
Harms
Ageratum conyzoides L. Goat weed Compositae 132
Agialida senegalensis v. Tiegh, A.
barteria v. Tiegh (see Balanites)
Agialida tombouctensis v. Tiegh.
Alafia multiflora (Stapf) Stapf Apocynaceae 144
Albizia lebbeck (L.) Benth. Women's tongue Fabaceae 167,174,223,226
Albizia flavovirens (see Samanea

saman)
Alchornea cordata Benth. see:
Alchornea cordifolia (Schum. & Thonn.) Christmas bush Euphorbiaceae 115,167
Mull. Arg.
AlchorneafloribundaMull. Arg. Niando Euphorbiaceae 115
Allamanda cathartica L. Apocynaceae 13,158
AlliumsativumL. Garlic Liliaceae 44,135,211,256
AlliumcepaL,. Onion Liliaceae 135,255,256
Allophyllus africanus Beauv. Sapindaceae 240
356
Aloe barbadensis Mill. (A. vera L., Liliaceae 238

A. vulgaris Lam., Aloe indica Royle)
Alpinia speciosa (Wendl.) Schum. c. Zingiberaceae 150,174
Alstonia booneidt Wild. (A. congensis Stool wood, Apocynaceae 12,89,167,211
Chev. &Aubrev.) pattern wood
Alternanthera repens (L.) Link. Amaranthaceae 240
(A.echinataSm.)
Anacardium occidentale L. Cashew nut tree Anacardiaceae 43,91,127,258
Anagallis arvensis L. Primulaceae 158,226
Ananas comosus (L.) Merrill (A. sativa Pineapple Bromeliaceae 144,224
Schult.)
Anchusa asperrima Del. (see Arnebia)
Andira inermis (Wright) DC. Dog almond, Fabaceae 86,174
wormbark
Annona aethiopica Dun. (see Xylopia
aethiopica)
Annona muricata L. Sour sop Annonaceae 112,182
Annona reticulata L. Custard apple, Annonaceae 112,182
bullock's heart
Annona senegalensis Pers. Annonaceae 182
Annona squamosa L. Sweet sop Annonaceae 183
Anogeissusleiocarpus(DC.)Guill. & Combretaceae 87,133,174
Perr. (A. schimperi Hochst ex
Hutch. & Dalz., A. leiocarpus var.
schimperi (Hochst ex. Hutch. &
Dalz.)Aubrev.)
Anthocleista djalonensis Chev. Loganiaceae 109
(A. kerstingii Gilg ex Volkens,
A. procera Chev.)
Anthocleista nobilis Don (A. parviflora Loganiaceae 109
Bak.)
Anthocleista procera Lepr. ex Bureau Loganiaceae 109,211
(A. frezoulsii Chev., A. nobilis
Lepr.)
Anthocleista vogelii Planch. Cabbage tree Loganiaceae 66
(A. kalbreyeri Bak., A. talbotti
Wern., A. nobilis FTA)
Antiaris africana Engl. (A. kerstingii Bark cloth tree Moraceae 26
Engl., Antiaris toxicaria (Rumph.
ex Pers) Lesch. var. africana)
Arachis hypogaea L. Groundnut Fabaceae 51,217,242
Argemone mexicana L. Prickly or Papaveraceae 31,84,144,150,
Mexican poppy 167
Arnebia hispidissima (Sieber & Lehm) Boraginaceae 206
DC.
A. asperrima (Del.) Hutch. & Dalz.,
Anchusa asperrima Del.
(see A. hispidissima)
Asclepias curassavica L. Swallow wort, Asclepiadaceae 19,22
A. daemiaForsk. (see Pergularia wild ipecacuanha
daemia)
357
A. lineolata (Decne.) Schltr.

(see Pachycarpus lineolatus)
Asteracantha longifolia (L.) Nees
(see Hygrophila auriculata)
Atractylis aristata Battandier Compositae 211
Azadirachta indica Juss. Neem, margosa Meliaceae 140,211,226,262
tree
BaissealeonensisBenth. (B. brachyantha Apocynaceae 14,48

Stapf)
Balanites aegyptiaca (L.) Del. (B. Soap berry tree, Zygophyllaceae 54,184
zizyphoides Mldbr. & Schltr.) thorn tree, desert
date
Balsamocitruspaniculata(Schum. &
Thonn.) Swingle (see Afraegle)
Balsamodendron africanum (Rich.)
Arn. (see Commiphora africana)
Barleria auriculata Schum.,
B. longifolia L. (see Hygrophyla
auriculata)
Bauhinia benzoin Kotschy, B.
reticulata DC. (see Piliostigma
reticulatum)
Bauhinia purpurea L. c. St Thomas tree Caesalpiniaceae 47
Bauhinia tomentosa L. c. Caesalpiniaceae 47
Bauhinia variegata L. c. Caesalpiniaceae 47
Bidenspibsa L. (B. abortiva Schum. & Bur marigold Compositae 150,184
Thonn.)
Bignonia africana (see Kigelia)
Bixaorellana L. (subspontaneous) Anatto tree Bixaceae 167
Blighia sapida Koenig Akee apple Sapindaceae 226,253,254
Boerhaviadiffusa L. (partly B. repens Hog weed, Nyctaginaceae 106,211
var. diffusa (L.) Hook., partly B. punarnava
adscendens Willd.)
Bombax buonopozense Beauv. (B. Silk cotton tree Bombacaceae 144
flammeum Ulbr., B. buesgeni Ulbr.)
Bombax pentandrum L. (see Ceiba
pentandra)
Borreria vertidllata (L.) Mey. Green borreria Rubiaceae 62,121,139
Brassica oleraceae L. Cabbage Cruciferae 242,256
Brideliaferruginea Benth. Euphorbiaceae 258,260
Bruceaantidysenterica Lam. (B. salutaris Simaroubaceae 167
Chev.)
Brucea guineensis Don (B. macrophylla 167
Oliv.)
Brugmansia Candida Pers. (see Datura
Candida)
Bryonia grandis L. (see Coccinia
grandis)
Bryophyllumpinnatum (Lam.) Oken Never-die Crassulaceae 129
(B. calycinum Salisb.)
358
Butyrospermum paradoxum subsp. parkii Shea butter tree Sapotaceae 144

(Don) Hepper
Caesalpinia bonduc (L.) Roxb. Bonduc or physic Caesalpiniaceae 155,158

(C. crista L., C. bonducella (L.) (nicker) nut
Flem.)
Caesalpinia pulcherrima (L.) Sw. c. Pride of Barbados Caesalpiniaceae 158
Cajanus cajan (L.) Millsp. Pigeon pea Fabaceae 221
Callichilia barteri (Hook.) Stapf
(see Hedranthera barteri)
Callichilia monopodialis (Schum.) Stapf Apocynaceae 12
Caloncoba echinata (Oliv.) Gilg Gorli Flacourtiaceae 130
Caloncobaglauca (P. Beauv.) Gilg Flacourtiaceae 130
Caloncoba welwitschii (Oliv.) Gilg Flacourtiaceae 130
Calophyllum inophyllum L. c. Guttiferae 207
Calotropisprocera (Ait.) Ait. Mudar, sodom Asclepiadaceae 18,24,144,226
apple, swallow
wort
Calyptranthes guineensis Willd. (see
Syzgium guineense var. guineense)
Camellia thea Link Tea plant Ternstroemaceae 51
Canavallia ensiformis (L.) DC. Sword or horse Fabaceae 53,158
bean
Cannabis sativa L. var. indica Lam. Indian hemp Cannabinaceae 78,144,212
Canscora decussata (Roxb.) Roem. & Gentianaceae 134,212
Schult.
Capparis decidua (Forsk.) Edgew. Capparidaceae 136,212
(C. aphylla Hayne ex Roth.)
Capsicum annuum L. Capsicum Solanaceae 144,204
Capsicum frutescens L. African pepper Solanaceae 204
Carapaprocera DC. (C. guineensis Sweet Crabwood, Meliaceae 164
ex Juss., C. touloucouna Guill. & monkey cola
Perr., C. gummiflua DC., C.
velutina DC., C. microcarpa
Chev.)
Cardiospermum halicacabum L. (C. Balloon vine Sapindaceae 122,145
micro-carpum Kunth)
Carica papaya L. Pawpaw, papaya Caricaceae 42,138,145,150,
167,174,212,224,
227,242
Carissa edulis Vahl (edulis forma Apocynaceae 11,174
pubescens (DC.) Pichon,
C.pubescensDC.)
Carpodinus umbellatus Schum.
(see Hunteria umbellata)
Cassia absush. Four-leaved senna Fabaceae 93,145
Cassia alata L. c. and nat. Ringworm bush Fabaceae 148
CassiafistulaL,. Indian laburnum Fabaceae 154
Cassia occidentalis L. Coffee senna, Fabaceae 148
stinkweed
359
Cassia toraL. Foetid cassia Fabaceae 148

Catharanthus roseus (L.) Don Madagascar Apocynaceae 12,159,227,250,
Cedrela kotschyi Schweinf. (see periwinkle 252
Pseudocedrela kotschyi (Schweinf.)
Harms)
Ceiba pentandra L. Gaertn. (C. Silk cotton tree Bombacaceae 258
thonningiiChev.)
Centaurea perrotteti DC. (C. asperal L., Compositae 258
C. calcitrapa Chev., C.
alexandrinaL.)
Centella asiatica (L.) Urb. Indian pennywort Umbelliferae 67,145,227
Cephalandra indica Naud (see
Coccinia grandis)
Cerbera thevetia L., C. peruviana
Pers. (see Thevetia neriifolia)
Charia chevalieri DC., C. indeniensis
Chev. (see Ekebergia senegalensis)
Chasmanthera dependens Hochst. Menispermaceae 60,161,167
Chenopodium ambrosioides L. c. American Chenopodiaceae 170
wormweed
Chlorophora excelsa (Welw.) Benth, African oak, iroko Moraceae 150
(C. alba Chev.)
Cicca discoidea Baill. (see Phyllanthus
discoideus)
Cinchona spp. Quinine bark Rubiaceae 33,62,162
Cissampelos dinklagei Engl. (see
Stephania dinklagei)
Cissampelos mucronata A. Rich. Menispermaceae 59,96
(C. pareiraof F.T.A.)
Cissampelos owariensis Beauv. ex DC. Pareira brava Menispermaceae 59,96
(C. pareira L. var. owariensis
Beauv. ex DC.) Oliv., C. robertsonii
Excell.)
Cissus quadrangularis L. Vitaceae 118
Citrus limonum, C. aurantium, Lemon, orange, Rutaceae 47,174
C.decumana, etc. grapefruit, etc.
Citrus nobilis Lour Rutaceae 212
Citrus paniculata Schum. & Thonn.
(see Afraegle)
Cleome gynandra L. (see
Gynandropsis)
Cnestisferruginea DC. (C. oblongifolia Connaraceae 145
Bak.
Coccinia grandis (L.) J. & O. Voigt Cucurbitaceae 258
Cocculus bakis Rich, (see Tinospora
bakis)
Cocculus leaba (Del.) DC. (see C.
pendulus)
Cocculus pendulus (J. & G. Forst.) Menispermaceae 59,98,159
Diels
Cocos nucifera L. Coco nut Palmae 150
360
CoffeaarabicaL. Coffee Rubiaceae 62

Cola acuminata (Beauv.) Schott & Endl. Kola nut tree Sterculiaceae 65
(C. pseudoacuminataEngl.)
Cola nitida (Vent.) Schott & Endl. (Cola Sterculiaceae 64
acuminata Engl.)
CombretumfloribundumEngl. &
DielSjC.altumPerr.)
Combretum micranthum Don (C. altum Kinkeliba Combretaceae 132
Perr.)
Combretum racemosum Beauv. Combretaceae 133
Combretum rhodanthum Engl. & Diels Combretaceae 134
Commiphora africana (Rich.) Engl. African Myrrh Burseraceae 197
Conocarpusleiocarpus DC. (see
Anogeissus leiocarpus)
Conopharyngia durissima (Stapf)
Stapf,C. crassaBenth. Stapf (see
Tabernaemontana crassa)
Conopharyngia pachysiphon (Stapf)
Stapf (see Tabernaemontana
pachysiphon)
Conyza cinerea L. (see Vernonia
cinerea(L.)Less-)
Conyza pauciflora Willd. (see
Vernonia pauciflora)
Corchorus olitorius L. Jute Tiliaceae 25,262
Corynanthe johimbe Schum. (see
Pausinystalia johimbe)
Corynanthe pachyceras Schum. Rubiaceae 40,62,95
Costus afer Ker-Gawl., C. obliterans Ginger lily Zingiberaceae 198
Schum.
Costus anomocalyx Schum., C.
insularis Chev., C. lucanusciamis
Chev.
Cotyledon pinnata Lam. (see
Bryophyllum pinnatum)
Cracca purpurea L. (see Tephrosia
purpurea)
CratevareligiosaForst. (C. adansonii Capparidaceae 121,145,212
Oliv.)
Crossopteryxfebrifuga (Afzel. exG. Don) Rubiaceae 62,165
Benth. (C. kotschyana Fenzl)
Croton macrostachyusHochst. ex Del. Euphorbiaceae 189
(Croton guerzesiensis Beille)
Croton oppositifolius Geisel (see
Mallotus oppositifolius)
Cryptolepis sanguinolenta (Lindl.) Schltr. Asclepiadaceae 18,41,131,205
(C. triangularis N. E. Br.)
Cryptostegia grandiflora (Roxb.) R.Br. Asclepiadaceae 18,21,22
ex Lindley
Cucurbita maxima Duchesne Squash gourd Cucurbitaceae 170
CucurbitapepoL. Pumpkin Cucurbitaceae 170
361
Curcuma domestica Val. (C. longa L.) Turmeric Zingiberaceae 161,208,224

Cynanchum pyrotechnicum Forsk.
(see Leptadeniapyrotechnica)
Cynanchum hastatum Pers. (see
Leptadenia hastata)
CyperusrotundusL. Nut grass Cyperaceae 145,200,217
Daemia extensa R.Br. (see Pergularia

daemia)
Dalbergia sissoo Roxb. Fabaceae 212,216
Datura Candida (Pers.) Safford (D. Solanaceae 80
arborea Ruiz & Pavon)
Datura innoxia Mill. (D. metel Chev. Solanaceae 80
Berh.ofF.T.A.)
Datura metel L. (D. fastuosa L. var. alba Thornapple, Solanaceae 80
(Nees))C.B.Cl. devil's trumpet
Datura stramonium L. incl. D. tatula L. Solanaceae 80
Datura suaveolens Humb. & Bonpl. Solanaceae 80
exWilld.c.
Denis microphylla (Miq.) Jacks. c. Fabaceae 177
Desmodiumgangeticum L. DC. var. Tick trefoil Fabaceae 102,151,159,213
gangeticum
Dichrostachys glomerata (Forsk.) Chiov. Mimosaceae 184
(D. platycarpa Welw. ex Oliv.)
Dioscorea dumetorum (Kunth.) Pax (D. Bitter yam, Dioscoreaceae 70
buchholziana Engl.) cluster yam
Dioscorea pruriens L. (see Mucuna
pruriens)
Dioscoreophyllum cumminsii (Stapf) Diels Menispermaceae 266
Diospyros canaliculata de Wild. 53
(D. xanthochlamys)
Diospyros mespiliformis Hochst. ex DC. Swamp ebony, Ebenaceae 53,145,174
(D. senegalensis Perr. ex DC.) monkey guava
Diospyros tricolor {Schum. &Thonn.) Ebenaceae 54,174
Hiern
Dolichos unguiculatus L., D.
biflorus L., D. sinensis (L.) Savi &
Hask (see Vigna unguiculata)
Dolichos pruriens L. (see Mucuna
pruriens)
Dracaena mannii Baker Asparagus tree Agavaceae 145
Drosera indica L. Droseraceae 129
Duranta repens L.c. (Duranta plumieri) Pigeon berry Verbenaceae 184
Ecliptaprostrata (L.) L. (E. alba (L.) Compositae 143

Hassk.)
Ekebergia senegalensis Juss. (E. chevalieri Meliaceae 138,145
(DC.) Harms E. indeniensis (Chev.)
Harms, E. dahomensis Chev.)
362
Elaeocarpus sphaericus Schum. (E. Tiliaceae

ganitrusRoxb.)
Elaeis guineensis Jacq. Oil palm Palmae 216
Elcaja roka Forsk. (see Trichilia roka)
EmbeliaschimperiVatke (E. abyssinica Myrsinaceae 172
Bak.)
Enantia chlorantha Oliv. African Yellow- Annonaceae 111
wood
Enantiapolycarpa (DC.) Engl. & Diels Annonaceae 111
EntadaafricanaGuill. &Perr. (E. Mimosaceae 178
sudanica Schweinf., E. ubanguiensis
de Wild., Entadopsis sudanica
(Schweinf.) Gilb. & Boutique)
Epibaterium pendulum J. &G. Forst.,
Epibaterium leaeba (Del.) DC. (see
Cocculus pendulus)
Epinetrum cordifolium Mangenot & Miege Menispermaceae 59,100
Eriodendron anfractuosum DC.
(see Ceiba pentandra)
Erythrina excelsaBak. (E. seretideWild.) Fabaceae 100
Erythrina mildbraedii Harms (E. altissima Fabaceae 100
Chev.)
Erythrinas senegalensis DC. Coral flower, Fabaceae 100
parrot tree
Erythrina sigmoidea Hua (E. dybowski 100
Hua, E. eryotricha Harms)
Erythrina vogeliiHook. f. Fabaceae 100
ErythrophleumguineenseG. Don Sassy bark, ordeal Caesalpiniaceae 28,72
tree
Erythrophleum ivorense Chev. (E. Caesalpiniaceae 28
micranthum Harms.)
Erythrophleum suaveolens (Guill. & Perr.) Caesalpiniaceae 29
Brenam
Erythroxylum coca Lam. Erythroxylaceae 92
Eucalyptus globulus Labill. c. Blue gum tree Myrtaceae 145
Eugenia jambolana Lam. (see
Syzygium cumini)
Eupatorium coloratum Willd. (see
Vernonia colorata)
Euphorbia hirta L. (E. pilulifera Chev.) Asthma herb Euphorbiaceae 113,167,184
Euphorbia prostrata Ait. Euphorbiaceae 149
Euphorbia thymifolia L. (E. burmannia Euphorbiaceae 149
Gay partly; E. aegyptiaca Soiss.;
E. scordifolia Jacq. of F.T.A.
partly)
Euphorbia tirucalli L. Euphorbiaceae 162
Fagara leprieuri(Guill. & Perr.) Engl. Rutaceae 33

FagaramacrophyllaEngl. (see
Zanthoxylum gilletii (de Wild.)
Watson)
363
Fagara rubescens (Planch, ex Hook, f.

Engl.) (see Zanthoxylum rubescens
Planch, ex Hook, f.) Watson
Fagara zanthoxyloides Lam. (F.
senegalensis (DC.) Chev. (see
Zanthoxylum zanthoxyloides
(Lam.) Watson)
Feretia apodanthera Del. (F. canthioides Rubiaceae 62
Hiern)
Fluggea klaineana Pierre ex Chev. (see
Phyllanthus discoideus)
Fluggea microcarpa Blume (see
Securinega virosa)
Fluggea obovata var. luxurians Beille
(see Phyllanthus discoideus)
Fluggea virosa (Roxb. ex Willd.) Baill.
(see Securinega virosa)
Funtumia africana (Benth.) Stapf, F. False rubber tree Apocynaceae 13,193,218
latifolia(Stapf) Schlechter
Funtumia elastica (Preuss) Stapf West African Apocynaceae 193
rubber tree
Gabunia glandulosa Stapf (see

Tabernaemontana glandulosa)
Glossopholis dinklagei (Engl.) Stapf
(see Tiliacora dinklagei)
Gnidia kraussiana Meisn. (see
Lasiosiphon kraussianus)
Gongronema latifolium Benth. Asclepiadaceae 23
Gossampinus buonopozensis (Beauv.)
Bak. (see Bombax buonopozense)
Gossypium herbaceum L., G. hirsutum L., Cotton plant Malvaceae 156,227,232
G. barbadenseL,.
Grewia bicolor Juss. (G. salvifolia Heyne Tiliaceae 116
ex Roth)
Grewia carpinifolia Juss. Tiliaceae 116
Grewia lasiodiscus Schum. (G. kerstingii Tiliaceae 116
Burrett)
Groutia celtidifolia Guill. & Perr. (see
Opilia celtidifolia)
Guiera senegalensis Gmell. Combretaceae 89,146
Guillandina bonduc L. (see Caesalpinia
bonduc)
Gynandropsisgynandra (L.) Briq. (G. Cat's whiskers Capparidaceae 175,213
pentaphylla DC.)
Gymnema sylvestre (Retz.) Schultes Asclepiadaceae 23,213,262
Gymnosporia senegalensis (Lam.)
Loes. (see Maytenus senegalensis)
HaematoxylumcampechianumL.c. Logwood Caesalpiniaceae 151,213

364
Harrisonia abyssinica Oliv. (H. Simaroubaceae 173

occidentalis Engl.)
Hedranthera barteri (Hook, f.) Pichon Apocynaceae 12
Hedysarum gangeticum L. (see
Desmodium gangeticum)
Helmia dumetorum Kunth. (see
Dioscorea dumetorum)
Heptacyclum Engl. (seePenianthus
zenkeri)
Heudelotia africana Rich, (see
Commiphora africana)
Hibiscus rosa-sinensis L. Malvaceae 224,227,233
Hibiscus vitifolius L. Malvaceae 213
Holarrhenafloribunda (Don) Dur. & Conessi or kurchi Apocynaceae 13,38,72,84,163,
Schinz. var.floribunda(H. africana bark 193,218
DC., H. wulfsbergii Stapf)
Holalafia multiflora Stapf (see Alafia
multiflora)
Hordeum vulgare L. Barley Gramineae 253
Hunteria eburnea Pichon Apocynaceae 11,39
Hunteria elliotii (Stapf) Pichon Apocynaceae 39
Hunteria umbeilata (Schum.) Hallier Erin tree Apocynaceae 39,175
Hydrocotyle asiatica L. (see Centella
asiatka(L.)Urb.)
Hygtophyla auriculata (Schum.) Heine Acanthaceae 151,248
(H. spinosa Anders.)
Hylacium owariense Beauv. (see
Rauvoffia vomitoria)
Hymenocallis littoralis Salisb. Spider lily Amaryllidaceae 151,159
Hymenocardia acida Tul. Euphorbiaceae 184
Hyptis suavolens (L.) Poit. Bush tea-bush Labiatae 225
Ipomoeamauritiana Jacq. (I. digitataof Convolvulaceae 239

F.T.A.)
Ipomoeapes-caprae (L.) Sweet Goats foot Convolvulaceae 209
(I. pes-caprae Roth) Convolvulus
Ipomoea purpurea (L.) Roth Convolvulaceae 209
Isokmacampanulata Engl. & Diels Annonaceae 111
(I. leonensis Sprague & Hutch.,
I. soubreanaChev. ex Hutch. &
Dalz.)
Jasminum sambac (L.) Ait Oleaceae 240

Jateorhizatnacrantha (Hook, f.) Exell. & Menispermaceae 60,84
Mendonâ (J. strigosa Miers)
Jatwpha curcas L. Physic nut, Euphorbiaceae 54,190
Barbados nut
Jatmpkagossypifolia L. Wild cassada Euphorbiaceae 190
Jatr&phapodagrica Hook. Euphorbiaceae 94
365
Justiciainsularis Anders. (J. galeopsis Acanthaceae 76

Anders.)
Kalanchoe pinnata (Lam.) Pers.

(see Bryophyllum pinnatum)
Karlea berchemoides Pierre (see
Maesopsis eminii Engl.)
Khaya senegalensis (Desv.) Juss. Dry zone Meliaceae 85,146,168
mahogany cail
cedrat
Kigelia africana (Lam.) Benth. Sausage tree Bignoniaceae 240
(K. pinnata (Jacq.) DC., K.
aethiopica Decne., K. eliottii
Sprague (16 synonyms))
Kolobopetalum auriculatum Engl. (K. Menispermaceae 60,84
veitchianum Diels)
Kickxia africana, K. latifolia, K.
zenkeri and K. elastica (see
Funtumia)
Lagerstroemia speciosa (L.) Pers. (L. flos Lythraceae 263

reginaRetz.)
Lantana camara L. (L. antidotalis Wild sage, Verbenaceae 118
Thonn.) Bahama tea
Lasiosiphon kraussianus (Meisn.) Thymelaceae 146
Burtt-Davy (L. kraussi Meisn., L.
kerstingii Pearson, L. guineensis
Chev.)
Lawsonia inermis L. (L. alba Lam.) Henna, Egyptian Lythraceae 53,146
privet
Lepidium sativum L. c. and nat. Common cress Cruciferae 151
Leptactina densiflora Hook, f. Rubiaceae 62
Leptactina senegambica Hook, f. Rubiaceae 62
Leptadenia hastata (Pers.) Decne. (L. Asclepiadaceae 23
lancifolia (Schum. & Thonn.)
Decne)
Leptadenia pyrotechnica (Forsk.) Decne. Asclepiadaceae 213
(L. spartium Wight & Arn.)
Leucena glauca (L.) Benth. Wild or horse Mimosaceae 227
tamarind
Limonia Warnecki Engl. (see Afraegle
paniculata)
Lithospermum hispidissimum Sieber
ex Lehm (see Arnebia hispidissima)
LochneraroseaReichb. (see
Catharanthus roseus)
Lonchocarpus cyanescens (Schum. & Indigo vine Fabaceae 202
Thonn.) Benth.
Lonchocarpus laxiflorus Guill. & Perr. Fabaceae 202
366
Lonchocarpus sericeus (Poir.) H. B. & K. Fabaceae 178

Lupinus tassilicus Maire (L. termis Forsk.) Fabaceae 216,227,252
MaesopsiseminiiEngl. (M. berchemoides Rhamnaceae 159

(Pierre) Chev.)
Mallotus oppositifolius (Geisel.) Mull. Kamala Euphorbiaceae 175
Arg.(M.beilleiChev.)
Mallotus philippinensisc. Euphorbiaceae 175
Malouetia heudelotii DC. Apocynaceae 14
Mangifera indica L. Mango tree Anacardiaceae 50,146
Manihot esculenta Crantz (M. utilissima Cassava, manioc Euphorbiaceae 243
Pohl.)
Mansonia altissima (Chev.) Chev. var. Sterculiaceae 26
altissima
Marsdenia latifolia (Benth.) Schum.
(see Gongronema latifolium)
Massularia acuminata (Don) Bullock ex Rubiaceae 131
Holye
Medicago sativa L. c. Fabaceae 217
Melia azadirachta L., Melia indica
(Juss.) Brandis (see Azadirachta
indica)
Melia azedarach L. Persian lilac, Meliaceae 180
bead tree
Mesuaferrea L. c. Guttifereae 207
Milletia aboensis CHook.) Bak. Fabaceae 184
(M. macrophyllavar. aboensis
Hook, f.)
Milletia barteri (Benth.) Dunn Fabaceae 159
Mimosa farnesiana L. (see Acacia
farnesiana)
Mimosa glauca L. (see Leucena glauca)
Mimosa glomerata Forsk., M. nutans
Pers. (see Dichrostachys
glomerata)
Mimosa lebbeck L. (see Albizia
lebbeck)
Mimosa nilotica L. (see Acacia nilotica
var. nilotica)
Mimusops elengi L. Sapotaceae 227
Mitragyna ciliata Aubrev. & Pellegr. Rubiaceae 41
Mitragyna inermis (Willd.) Ktze. (M. Rubiaceae 40,62,168
africana(Willd.)Korth.)
Mitragyna stipulosa (DC.) Ktze. African linden Rubiaceae 40,62,95,168
(M. macrophylla Hiern)
Modecca cissampeloides Planch, ex
Benth. (see Adenia cissampeloides)
Momordica charantia L. African cucumber, Cucurbitaceae 146,184,228,236,
balsam pear 247,248
367
Montanoa tomentosa (not in West Africa) Compositae

Morinda longiflora G. Don. Rubiaceae 63
Morinda lucida Benth. (M. citrifolia Brimstone tree Rubiaceae 44,63
Chev.)
Morinda geminata DC. Rubiaceae 62,175
Moringa oleifera Lam. (M. pterygo- Horseradish tree Moringaceae 46,136,146,214
spermaGaertn.)
Morus alba L., Morus nigra L. Mulberry Moraceae 257,259
Morus excelsa Welw. (seeChlorophora
excelsa)
Mostuea hirsuta (Anders, ex Benth.) Loganiaceae 44,72
Baill.exBak.
Mucunapruriens(L.) DC. var. pruriens Cowhage, Cow- Fabaceae 102,263
itch
Munduleasericea (Willd.) Chev. (M. Fabaceae 178
suberosa (DC.) Benth.)
Musa sapientum L. (Musa paradisiaca Banana Musaceae 46,257,259
var. sapientum Ktze.)
Myristicafragrans Houtt. Nutmeg Myristicaceae 79
Nauclea africana Willd. (see Mitragyna

inermis)
Nauclea diderrichii (de Wild. & Dur.) Rubiaceae 63,76
Merrill
Nauclea latifolia Sm. (N. esculenta Afz. African or Guinea Rubiaceae 63,75
ex. Sab. Merrill)
Nauclea pobeguinii (Pob. ex Pellegr.) Rubiaceae 63
Petit
Nauclea stipulosa DC. (see Mitragyna
stipulosa)
Nerium obesum Forsk (see Adenium
obesum)
Nerium oleander L. Oleander Apocynaceae 14,17
Newbouldia laevis (Beauv.) Seem, ex Bignoniaceae 117,168
Bureau.
Nicotiana tabacum L. Tobacco plant Solanaceae 185
Nymphaea lotus and spp. (N. liberiensis Water lily Nymphaceae 87,168
Chev.)
Ocimum basilicum L. (O. americanum Basil Labiatae 66,146,185

L., O. lanceolatum Schum. &
Thonn., O. dichotomum Hochst
ex Benth., O. menthaefolium
Chev.)
Ocimum canum Sims (O. hispidum Labiatae 66,146,185
Schum. & Thonn.)
Ocimum gratissimum L. (O. viride Labiatae 66
Willd., O. guineenseSchum. &
Thonn.)
368
Olax latifolia Engl. Olacaceae 159

Oldenlandia affinis DC. Rubiaceae 225
Omphalogonus nigritans N. E. Br. (see
Parquetina nigrescens)
Oncoba echinata Oliv. (see Caloncoba
echinata)
Oncoba glauca (P. Beauv.)Hook. f.
(see Caloncoba glauca)
Ophiocaulon cissampeloides (Planch,
ex Benth.) Mast, (see Adenia
cissampeloides)
Opilia celtidifolia (GuiU. & Perr.) Endl. Opiliaceae 171
ex Walp. (O. amentaceaeChev.)
Ormosia laxiflora Benth. ex Bak. (see
Afrormosia laxiflora)
Oryzasativah. Gramineae 217
Pachycarpus lineolata (Decne.) Bullock Asclepiadaceae 22

(Asclepias lineolata (Decne)
Schlechler partly)
PachypodanthiumstaudtiiEngl. & Diels Annonaceae 113
Parquetina nigrescens (Afzel.) Bullock Silk vine Apocynaceae 18,21
Passiflora edulis Sims. Passion fruit Passifloraceae 88
Passiflorafoetida L. Stinking passion Passifloraceae 88
flower
Paulliniapinnata L. Sapindaceae 27,165,168
Pauridiantha viridiflora (Schweinf. Rubiaceae 63,74,168
ex Hiern) Hepper
Pausinystaliajohimbe (K. Schum.) Yohimbe tree Rubiaceae 39,62,95
Pierre ex Beille (P. macroceras
Kenn.)
Pausinystaliapachyceras Schum. de
Wild. (seeCorynanthepachyceras)
Penianthus zenkeri (Engl.) Diels Menispermaceae 60
Pentaclethra macrophylla Benth. Oil bean tree Mimosaceae 116,185
Pergularia daemia (Forsk.) Chiov. Asclepiadaceae 19,24,233
(P.extensaN.E.Br.)
Pergularia sanguinolenta Lindl. (see
Cryptolepis sanguinolenta)
Periploca nigrescens Afzel, P.
calophylla (Baill.) Roberty (see
Parquetina nigrescens)
Periploca sylvestre Retz. (see
Gymnema sylvestre)
Phaseolusvulgaris L. c. Vegetable bean Fabaceae 217,219
Philenopteracyanescens (Schum. &
Thonn.) Roberty (see Lonchocarpus
cyanescens)
Phoenix dactylifera L. Date palm Palmae 216
369
Phyllanthusdiscoideus (Baill.) Mull. Arg Euphorbiaceae 74

Phyllanthus niruri L. Euphorbiaceae 151,163,168,259
Phyllanthus virosus Roxb. ex Willd.
(see Securinega virosa)
Physalis somnifera L. (see Withania
somnifera)
Physostigma venenosum Balfour Calabar bean Fabaceae 41,72
Phytolacca dodecandra l'Herit Endod, soapberry Phytolaccaceae 188,204,228
(P. abyssinica Hoffm.)
Picralima elliotii Stapf (see Hunteria
elliotii)
Picralima gracilis Chev. (see Hunteria
eburnia)
Picralima nitida (Stapf) Th. & H. Dur. Apocynaceae 11,38,95
(P. macrocarpa Chev., P. klaineana
Pierre)
Picralima umbellata (Schum.) Stapf
(see Hunteria umbellata (Schum.)
Hallier)
Piliostigma reticulatum (DC.) Hochst. Caesalpiniaceae 47
Piperguineense Schum. & Thonn. (P. Black or Ashanti Piperaceae 91,146,185
leonense DC., P. famechonii DC.) pepper
Piper nigrum L. Black pepper Piperaceae 151
Pisum sativum L. Garden pea Fabaceae 221
Pithecellobum saman (Jacq.) Benth.
(see Samanea saman)
Pladera decussata Roxb. (see Canscora
decussata)
Pleioceras barteri Baill. Apocynaceae 13
PleomelemanniiBak. N.E.Br. (see
Dracaena mannii)
Plumbago zeylanica L. Ceylon leadwort Plumbaginaceae 128,225
Plumeria alba L. Apocynaceae 153
PlumeriarubraL. Frangipani Apocynaceae 13,153
Poinciana pulcherrima L. (see
Caesalpinia pulcherrima)
Polyadoa elliotii (see Hunteria
elliotii)
Polyadoa umbellata (Schum.) Stapf
(see Hunteria umbellata)
Polyalthia oliveri Engl. (P. acuminata Annonaceae 111
Oliv.)
Polygonum salicylifolium Brouss. Polygonaceae 147
ex Willd. (P. serrulatum Lag.,
P.barbatumChev.)
Polygonum senegalense Meisn. Polygonaceae 147,189
(P.glabrumofF.T.A.)
P. senegalense albotomentosum Polygonaceae 189
Porterandia cladantha (Schum.) Keay Rubiaceae 159
Poupartia birrea (Rich.) Aubrev (see
Sclerocarya birrea)
370
Species Common name Family
Pseudocedrela kotschyi (Schweinf.) Dry zone cedar Meliaceae 164,185

Harms (P. chevalieri DC.)
PseudocinchonaafricanaChev. ex
Perr. (see Corynanthe pachyceras)
Psidiumguajava L. c. Guava Myrtaceae 134
Pueraria thunbergiana (Sieb. & Zucc.) Fabaceae 216
Benth.
Punica granatum L. c. Pomegranate Rubiaceae 175
Quassia africana (Baill.) Baill. c. Simaroubaceae 185

Quisqualis indica L. Rangoon creeper Combretaceae 133,175
Randia cladantha Schum. (see

Porterandia cladantha)
Rauvolfia caffra Sond. (R. welwitschii Apocynaceae 37
Stapf)
Rauvolfia macrophylla Stapf Apocynaceae 37
Rauvolfia mannii Stapf (R. preussii Apocynaceae 37
Schum.)
Rauvolfia vomitoria Afzel. (R. Rauvolfia, Swizzle Apocynaceae 13,34,36,84
senegambiae DC.) stick
Rhigiocarya racemifera Miers (R. nervosa Menispermaceae 60,84
(Miers) Chev.)
Rhizophora racemosa Mey. Mangrove Rhizophoraceae 259
Rhoeo spathaceae (Sw.) Stearn (Rhoeo Commelinaceae 225
discolor (PHerit) Hance)
Ricinus communis L. Castor oil plant Euphorbiaceae 151
Ritchia longipedicilata Gilg Capparidaceae 172
Robinia cyanescens Schum. & Thonn.
(see Lonchocarpus)
Robinia sericeaPoir. (see
Lonchocarpus sericeus)
Rondeletia febrifuga Afzel. ex Don,
R. africana Winterb. (see
Crossopteryx febrifuga)
RondeletiafloribundaDon (see
Holarrhena floribunda)
Salvadora persica L. Salt bush, Salvadoraceae 147, 209

toothbrush tree
Samanea saman Jacq. & Merr. Mimosaceae 228
Santalum album L. c. Sandalwood Santalaceae 183
Sapindus trifoliatus L. Sapindaceae 44,225,228, 236
Sarcocephalus diderrichii de Wild.
& Dur. (see Nauclea diderrichii)
Sarcocephalus esculentus Afzel.
ex Sabine (see Nauclea latifolia)
Sarcocephalus pobeguini. Pobeg. ex
Pell, (see Nauclea pobeguinii)
371
Sarcocephalus russeggeri Kotschy ex

Schweinf. (see Nauclea latifolia)
Sarcocephalus sambucinus Schum.
(see Nauclea latifolia)
Sarcocephalus sassandrae Chev. (see
Nauclea latifolia)
SarcostemmaviminaleK.hr. Asclepiadaceae 23,239
Schmidelia africana (Beauv.) DC. (see
Allophyllus)
Schousboeacordifolia Schum. &
Thonn. (see Alchornea cordifolia)
Schwenkiaamericana L. (S. guineensis Solanaceae 27
Schum. & Thonn., S. hirta
Wright.)
Scilla indica Roxb. (see Urginea indica)
Sclerocarya birrea (Rich.) Hochst. Anacardiaceae 259,260
Scoparia dulcis L. Sweet broom weed Scrophulariaceae 259
Scyphostrychnos talbotii Moore, S.
psittaconyx Duvigne (see Strychnos
camptoneura)
SecuridacalongepedunculataFres. Violet tree, Polygalaceae 108,175,185,214
Senega-root tree
Securinega virosa (Roxb. ex Willd.) Euphorbiaceae 73,250,252
Baill. (S. microcarpa (Blume) Pax
&Hoffm.)exAubrev.)
Sesamumindicumh. Sesame, beniseed Pedaliaceae 185
Sida acuta Burm. (S. vogelii Hook., Malvaceae 147
S. carpinifolia oartlv")
Sida cordifolia L., S. hombifolia L. Malvaceae 120,147
Siphonoglossa macleodiae Moore (see
Justicia insularis)
Sodada decidua Forsk. (see Capparis
decidua)
Solarium nigrum L. (S.nodiflorumjacq., Solanaceae 104,147
S. guineense (L.) Lam.)
Solarium torvum Sw. incl. S. torvum var. Solanaceae 200
compactum Wright (S. mannii incl.
var. compactum Wright)
Sophora occidentalis L. (S. nitens Schum. Fabaceae 50,221
& Thonn., S. tomentosaof F.T.A.)
Spathodea laevis Beauv. (see
Newbouldia laevis)
Spermacoce verticillata L., S. globosa
Schum. & Thonn. (see Borreria)
SpigeliaanthelmiaL. Pink root, Loganiaceae 75
wormweed
SpilanthusuliginosaSw. (S.acmellaL., Para or bresil cress Compositae 180,185
S.oleraceajacq.)
Spondias birrea Rich, (see
Sclerocarya birrea)
372
Stephania dinklagei (Engl.) Diels Menispermaceae 59,101

Sterculia acuminata Beauv. (see Cola
acuminata).
Sterculia nitida Vent, (see Cola nitida)
Strophanthus gracilis Schum. & Pax Apocynaceae 14,15
Strophanthus gratus (Hook.) Franch. Strophanthus Apocynaceae 10,14
Strophanthus hispidus DC. Apocynaceae 14,15
Strophanthus sarmentosus DC. Apocynaceae 14,16
Strychnos afzelii Gilg (S. zizyphoides Loganiaceae 147
Bak., S. erythrocarpa Gilg)
Strychnos camptoneura Gilg & Busse Loganiaceae 68
Strychnos decussata Loganiaceae 69
Strychnos dinklagei Gilg Loganiaceae 69
Strychnos dolichothyrsa Gilg ex Onochi Loganiaceae 69
&Hepper
Strychnos spinosa Lam. (S. lokua Rich., Loganiaceae 69
S. laxa Solered., S. djalonensis
Chev., S. buettneri Gilg, S. spinosa
var. pubescens Bak.)
Strychnos usambarensis Gilg (S. micans Loganiaceae 68
Moore, S. cooperi Hutch. & Moss)
Swartzia madagascariensis Desv. Caesalpiniaceae 55,187
Swietenia senegalensis Desr. (see
Khaya senegalensis)
Synsepalum dulcificum (Schum. & Sapotaceae 266
Thonn.)Daniell
Syzygium cumini (L.) Skeels c. Jambolan Myrtaceae 249,257
Syzygiumguineense (Willd.) DC. var. Myrtaceae 159
guineense
Tabernaemontana crassa Benth. Apocynaceae 11,77

(T. durissima Stapf)
Tabernaemontana glandulosa (Stapf) Apocynaceae 147
Pichon
Tabernaemontana nitida Stapf (see
Picralima nitida)
Tabernaemontana pachysiphon Stapf Apocynaceae 12,77
var. pachysiphon
Teclea sudanica Chev. Rutaceae 51
Tecoma stans (L.)H.B.K.c. (ornam.) Bignoniaceae 252
Tephrosia purpurea (L.) Pers. Fish poison bean Fabaceae 51
(T. leptostachya DC.)
Tephrosia vogelii Hook. f. Fish poison bean Fabaceae 179
Terminalia avicennoides Guill. & Perr. Combretaceae 52,147
(T. lecardiiEngl. & Diels,
T. dictyoneura Diels)
Terminalia glaucescensPlanch, ex Combretaceae 147
Benth. (T. togoensis Engl. & Diels,
T. baumanniiEngl. & Diels,
T. passargeiEngl.)
373
Terminalia ivorensis Chev. Satin wood, Combretaceae 203

shingle wood
Terminalia laxiflora Engl. (T. elliotii Combretaceae 52
Engl. & Diels, T. sokodensis Engl.)
Terminalia macroptera Guill. & Perr. Combretaceae 52
(T. chevalieri Diels)
Tetrapleura tetraptera (Schum. & Mimosaceae 107,185,214
Thonn.)Taub. (T. thonningi
Benth.)
Thalictrum rhynchocarpum Dill. & Rich. Ranunculaceae 42
Thalictrum rugosum Ait Ranunculaceae 147
Thaumatococcus danielli (Benn.) Benth. Maranthaceae 266
Thea sinensis (see Camellia thea)
Thevetia neriifolia Juss. (T. peruviana Yellow oleander Apocynaceae 14,17,147,185
Pers.)
Tiliacora dinklagei Engl. Menispermaceae 58,99
Tiliacorafunifera (Miers) Oliv. Menispermaceae 58,99
Tiliacora subcordata Chev. (see
Triclisia subcordata)
Tiliacora tricantha Diels (see Triclisia
dictyophylla)
Tinospora bakis (A. Rich.) Miers Menispermaceae 60,85
T. roka (Forsk.) Chiov. (Trichilia Roka tree Meliaceae 164,168
emetica Vahl)
Trichilia prieuriana Juss. Meliaceae 165
Triclisia dictyophylla Diels (T. gilletii Menispermaceae 58,99
(deWild.)Staner)
Triclisia patens Oliv. Menispermaceae 58,99
Triclisia subcordata Oliv. Menispermaceae 58.99
Trifolium baccarinii Chiov. Fabaceae 216
Trigonellafoenum graecum L. Fenugreek Fabaceae 229,240,253
Triticumaestivum L. c. (Triticum Gramineae 217
sativumLam.)
Uncaria africana G. Don var. africana Rubiaceae 63,115

(U. talbotii Wernh. partly)
Uncaria africana var. angolensis (Havil.) Rubiaceae 63,115
Welw. ex Hutch. & Dalz.
Uncaria inermis Willd. (see Mitragyna
inermis)
Unona aethiopica Dunal (see Xylopia
aethiopica)
Unona macrocarpa Dunal (see Uvaria
chamae)
Urginea indica (Roxb.) Kunth. Indian squill Liliaceae 25,168
Urginea altissima (L.) Bak. Squill Liliaceae 26
Urophyllum viridiflorum Schweinf.
ex Hiern (see Pauridiantha
viridiflora)
374
Uvaria chamaeBeauv. (U. cylindrica Annonaceae 134

Schum. & Thonn., U. cristataR.Br.
ex Oliv., U. nigrescens Engl. &
Diels, U. echinataChev.)
Uvariopsis guineensis Keay Annonaceae 110
(U. spectabilis Chev. ex Hutch
&Dalz.)
Ventenatia glauca (see Caloncoba)

Verbena officinalis L. Verbenaceae 239
Verbesina prostata L. (see Eclipta
prostrata)
Vernonia amygdalina Del. Bitter leaf, iron Compositae 27
(V. senegalensis Chev.) weed
Vernonia cinerea (L.) Less. Compositae 27
Vernonia colorata (Willd.) Drake Compositae 28,214
(V. senegalensis Less.)
Vernonia conferta Benth. Compositae 27
Vernonia guineensis Benth. var. Compositae 27
guineensis
Vernonia nigritiana Oliv. & Hiern Compositae 27
(V. baoulensisChev.)
Vernonia pauciflora (Willd.) Less. Compositae 185
Vigna unguiculata (L.) Walp (V. sinensis Fabaceae 263
T \
L..)
Vinca rosea L. (see Catharanthus
roseus)
Vinticena carpinifolia (Juss.) Burret
(see Grewia carpinifolia)
Vinticena lasiodiscus (Schum.) Burret,
V. kerstingii (Burret) Burret
(see Grewia lasiodiscus)
Vitex agnus castus L. Verbenaceae 239
Vitis quadrangularis (L.) Wall, ex
Wight & Arn. (see Cissus
quadrangularis)
Voacanga africana Stapf (V. glabra Apocynaceae 12,29,95
Schum., V. magnifolia Wernh., V.
eketensis Wernh., V. glaberrima
Wernh., V. Schweinfurtii var.
parviflora Schum., V. africana var.
glabra (Schum.) Pichon)
Voacanga bracteata Stapf Apocynaceae 12
Voacanga thouarsii(Roem. & Schult.) Apocynaceae 29
Walteria indica L. (W. americana L.) Sterculiaceae 89

Withania somnifera Dunal Winter cherry Solanaceae 105,147,201,229
Wrightia parviflora Stapf (see
Pleioceras barteri)
375
Ximenia aegyptiaca (see Balanites

aegyptiaca)
Xylopia aethiopica (Dunal) Rich Ethiopian pepper Annonaceae 140,214
(X. eminiChev.)
Xysmalobium heudelotianum Decne. Asclepiadaceae 19,25
Zanthoxylum gilletii (de Wild.) Watson Rutaceae 33

Zanthoxylum guineense Stapf (see
Harrisonia abyssinica)
Zanthoxylum rubescens (Planch, ex Rutaceae 33
Hook, f.) Watson
Zanthoxylum zanthoxyloides (Lam.) Prickly ash, Rutaceae 32,131,205
Watson (Zanthoxylum senegalense candlewood,
(DC.) Che v., Z. polyganum tooth-ache
Schum.) bark

Medicinal Plants in Tropical West Africa (PDFDrive)

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Medicinal plants in tropical West Africa

WITH ILLUSTRATIONS BY THE AUTHOR

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CAMBRIDGE UNIVERSITY PRESS

Cambridge University Press

The Edinburgh Building, Cambridge CB2 8RU, UK

This publication is in copyright. Subject to statutory exception

First published 1986

This digitally printed version 2009

Library of Congress Catalogue Card Number: 85-5952

Foreword ProfessorG.B.MariniBettolo vii

In 1975 I began to be interested in the study of the active principles of African

Professor G. B. Marini Bettolo

Chairman, Scientific Committee, WHO Coordinating Centre

I want to thank Dr Lambo, Deputy Director of the World Health Organization in

Early traditional medicine

Practical therapeutic indications and mechanisms of action of the drugs

Fig. 1.1. Action and sites of action on the ANS.

other macromolecules. Blocking at different peripheral levels leads to more or less

I Plants in tropical West Africa with an action on the

Stimulation of the preganglionic nerve fibres to the ganglia results in liberation of

Group A: Plants containing cardiotonic steroid heterosides

Strophanthus gratus (Hook.) Franch. APOCYNACEAE

Strophanthus hispidus DC. APOCYNACEAE

Strophanthus gracilis Schum. & Pax APOCYNACEAE

Strophanthus sarmentosus DC. (Fig. 2.1) APOCYNACEAE

Fig. 2.1. Strophanthus sarmentosus D C .

Nerium oleander L. APOCYNACEAE

Fig. 2.2. Adenium obesum (Forsk.) Roem. & Schult.

ASCLEPIADACEAE AND PERIPLOCACEAE. Cardenolides and allocardenolides (in the

Parquetina nigrescens (Afzel.) Bullock syn. (Periploca nigrescens Afzel.,

Cryptostegia grandiflora (Roxb.) R.Br. ex. Lindley (Fig. 2.3) PERIPLOCACEAE

Fig. 2.3. Cryptostegia grandiflora (Roxb.) R. Br. ex. Lindley.

1967). A parallel appears to exist between cytotoxicity towards KB cells, a heart

Asclepias curassavica L. ASCLEPIADACEAE

Fig. 2.4. Calotropisprocera (Ait.) Ait.

Calotropis procera (Ait.) Ait. (Fig. 2.4) ASCLEPIADACEAE

Xysmalobium heudelotianum Decne. ASCLEPIADACEAE

PLANTS BELONGING TO OTHER BOTANICAL FAMILIES. Cardenolides related to those

Corchorus olitorius L. TILIACEAE

with experimental myocarditis and myocardiosclerosis, and in dogs with acute

Urginea indica (Roxb.) Kunth. syn. (Scilla indica Roxb.) LILIACEAE

Mansonia altissima (Chev.) Chev. var. altissima STERCULIACEAE

Paullinia pinnata L. SAPINDACEAE

Vernonia colorata (Willd.) Drake syn. (Eupatorium coloratumWiWd., V. senegalensis

Group B: Plants containing cardiotonic alkaloids

Erythrophleum guineense G. Don CAESALPINIACEAE

Fig. 2.5. Voacanga africana Stapf.

eliminated without any cumulative effect. Voacamine, voacangine and voacorine

(b) Cardiac depressants: anti-arrhythmic agents

Argemone mexicana L. (naturalized) (Fig. 2.6) PAPAVERACEAE

Fig. 2.6. Argemone mexicana L.

Zanthoxylum zanthoxyloides (Lam.) Watson syn. (Fagara zanthoxyloides Lam.,

Cinchona spp. (cultivated in the Cameroons and Guinea) RUBIACEAE

Rauvolfia vomitoria Afzel. syn. (R. senegambiae D C , Hylacium owariense P.

Fig. 2.7. Rauvolfia vomitoria Afzel.

(c) Vascular agents

Group Aj: hypotensives

Plants containing hypotensive alkaloids. Amongst these many indole and

Rauvolfia vomitoria Afzel. (for synonyms see above) APOCYNACEAE

containing up to 1.7% of reserpine (which has to be separated from accompanying

Fig. 2.8(a). Holarrhenine.

Fig. 2.8(b). 5/3-pregnane.