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Phytopharmacology 2013, 4(3), 598-637 Touqeer et al. 

A Review on the Phytochemistry and Pharmacology of Genus 

Tephrosia 

Saad Touqeer 1,* , Muhammad Asad Saeed 1 , Muhammad Ajaib 2 

1 Department of Pharmacy, The University of Lahore, Lahore, Pakistan. 

2 Department of Botany, GC University, Lahore, Pakistan. 

* Corresponding author: saadtouqeer@gmail.com; Tel: +92-322-4899048 

Received: 2 March 2013, Revised: 2 May 2013, Accepted: 9 May 2013 

Abstract 

Introduction 

The plants of genus Tephrosia of family Leguminosae are widely distributed in 

many tropical and subtropical countries of the world and have been used in folk 

medicine for the treatment of large number of diseases. The importance of this genus 

is similar to that of other therapeutically renowned genera. This review includes 

the chemical studies on different species mainly the isolation and identification of 

flavonoids, rotenoids and study of activity of some isolated compounds and also 

includes diffe-rent pharmacological activities like antioxidant, antimicrobial, anticancer, 

antiplas-modial, anti-inflammatory, larvicidal and toxicity studies of extracts 

and fractions. 

Keywords: Tephrosia; Flavonoids; Rotenoids; Phytochemistry; Pharmacology; 

Acivity. 

Plants have been used for the treatment of diseases from centuries. Natural product 

chemistry, especially phytochemistry, has become a topic of interest for most of the researchhers 

due to the advantages of the plant derived medicinal compounds over the traditional 

ways of using herbal plants. Ethnopharmacology plays an important role in the discovery of 

new biologically active compounds. The process usually starts with searching of useful 

plants from different records to the development of methods for the industrial production of 

drugs (Rout et al., 2009; Farnsworth et al., 1985; Koehn and Carter, 2005). According to 

World Health Organization (WHO) more than 80% of the world’s population uses plants for 

the treatment of their diseases (Calixto et al., 1998; Duraipandiyan et al., 2006). 

The genus Tephrosia belongs to the family Leguminosae and subfamily Papilionaceae. 

There are approximately 400 species included in this genus. The plants in this genus are 

widely distributed in tropical, sub-tropical and arid regions of the world (Willis, 1973; Al- 

598 

© 2013 Inforesights Publishing UK


Zahrani, 2007). The plants are prostate or erect herbs or in the form of soft or woody shrubs 

(Hacker, 1990). The base chromosome number of this genus is X=11 and are placed in the 

tribe Galegeae of the family Leguminosae (Atchison, 1951; Agarwal and Gupta 1983). Many 

plants from this genus have been used traditionally for the treatment of diseases like rheumatic 

pains, syphilis, dropsy, stomach ache, diarrhea, asthma, abortifacient, respiratory disorderrs, 

laxative, diuretic, and inflammation etc (Qureshi et al., 2010; Dzenda et al., 2007). Tephrosia 

purpurea, an important plnt of the genus is used as tonic, laxative, antivenom, antiulcer, 

antidiarhheal, and in leprosy (Virupanagouda et al., 2011). 

The main purpose of this review is to provide a comprehensive and up-to-date knowledge 

of the pharmacological and phytochemical research work performed on the genus Tephrosia. 

The plants of this genus have a large potential for study of its activities and chemical 

constituents for important leads. 

Chemical constituents from plants of genus Tephrosia 

A great variety of plants belonging to genus Tephrosia have been studied for their 

chemical constituents and pharmacological activities. The number of species studied phytochemically 

are much more than those studied pharmacologically. Different classes of organic 

compounds have been isolated of which some have been tested for their biological activities 

and some still unknown for their effect. The main classes of compounds include flavonoids, 

rotenoids, terpenoids, and sterols. It should be noted that flavonoids are the most abundantly 

isolated and identified compounds in the genus. Similarly in case of essential oil and fixed 

oil, we can see that very little work has been done by the scientists. Tephrosia purpurea, Tephrosia 

toxicaria, Tephrosia candida, Tephrosia elata, and Tephrosia villosa have been the 

plants of interest for the scientists. The readers will also find some work on the stereochemistry 

of compounds. Praecansone A, flavonoid from Tephrosia pumila for example, exists 

in the form of two isomers (Dagne et al., 2012). 

Table 1 briefly describes all the chemical work done on genus Tephrosia. Readers will 

see some novel compounds as well some compounds repeating in many species. Some 

chemicals in the table would be familiar to us as they have been isolated from other genera as 

well 

Table 1. Chemical constituents from plants of genus Tephrosia. 

Species Class Compound Reference 

Tephrosia abbottiae Flavonoid abbotin Gómez-Garibay et al., 

1986 

tephrobotin 

Tephrosia aequilata Flavonoid obovatin methyl ether Muiva, 2012 

(E)-praecansone A 

demethylpraecansone B 

3,4:8,9-dimethylenedioxypterocarpan Tarus et al., 2002 

Tephrosia apollinea Flavonoid (−)-semiglabrin Waterman and Khalid, 

1980 

(−)-pseudosemiglabrin 

(+)-glabratephrin 

(+)-glabratephrinol 

appollinine (7-methoxy-8-[3″-(2″,5″dihydro-5″,5″-dimethyl-2″-oxofuryl)]flavone 

599 



lanceolatin-A 

(+)-apollineanin Hisham et al., 2006 

(−)-semiglabrin 

(−)-semiglabrinol 

Tephrosia barbigera Flavonoid isopongaflavone Vilain, 1983 

barbigerone Vilain, 1980 

Tephrosia bidwilli Flavonoid (-)-6aR; 11aR-maackiain Ingham and Markham, 

1980 

(-)-6aS; 11aS-pisatin 

(-)-6aR; 11aR-4-methoxy- maackiain 

tephrocarpin 

Tephrosia 

bracteolata 

acanthocarpan 

Flavonoid isopongaflavone Khalid and Waterman, 

1981 

trans-tephrostachin 

trans-anhydrotephrostachin 

obovatin 

Tephrosia calophylla Coumestan tephcalostan Hari Kishore et al., 2003 

Flavonoid 7-O-methylglabranin 

kaempferol 3-O-β-D-glucopyranoside 

(2S)-5-hydroxy-7,4'-di-O-(gamma, gamma- 

dimethylallyl) flavanone 

600 

Reddy et al., 2009 

6-hydroxy-E-3-(2,5-dimethoxy 

benzylidine)-2',5'-dimethoxyflavanone 

tephrowatsin C 

afrormosin 

kaempferol 3-O- β -D-glucopyranoside 

Benzil calophione A Ganapaty et al., 2009b 

1-(6′-Hydroxy-1′,3′-benzodioxol-5′-yl)-2- 

(6″-hydroxy-2″-isopropenyl-2″,3″-dihydrobenzofuran-5″-yl)-ethane-1,2-dione 

Coumestan tephcalostan B 

tephcalostan C 

tephcalostan D 

Tephrosia candida Flavonoid candidol Dutt and Chibber, 1983 

candidone Roy et al., 1986 

ovalichalcone 

dehydrorotenone 

candidin Parmar et al., 1988 

pongachin 

flemichapparin-B Roy et al., 1987 

Sterol β -sitsterol Parmar et al., 1988 

Acid caffeic acid 

Rotenoid 12a-hydroxyrotenone Parmar et al., 1988 

tephrosin 

amorpholone Kole et al., 1992 

6a,12,-dehydodeguelin Parmar et al., 1988 

12a-hydroxy-β-toxicarol Andrei et al., 1997 

deguelin 

α-toxicarol 

6a,12a-dehydrodeguelin 

12a-hydroxy-α-toxicarol, 6a 

12a-dehydro-α-toxicarol 

6a,12a-dehydro-β-toxicarol 

dehydrodihydrorotenone Roy et al., 1987 

tephrospirolactone Andrei et al., 2002 

tephrospiroketone 1 

Tephrosia cinerea Flavonoids and 

Phenolics 

tephrospiroketone II 

demethylapollinin 7-O-β-Dglucopyranoside 

apollinin 

glabatephrin 

semiglabrin 

Maldini et al., 2011 



Sesquiterpene 

pseudosemiglabrin 

3′-O-methyl- methylquercetin 

3,7-di-O-rhamnopyranoside 

kaempferol 3,7-di-O-rhamnopyranoside 

quercetin 3,7-di-O-rhamnopyranoside 

3-O-β-glucopyranosylquercetin 7-O-αrhamnopyranoside 

3-O-β-xylopyranosylquercetin 7-O-αrhamnopyranoside 

3-O-α-arabinopyranosylquercetin 7-O-αrhamnopyranoside 

5-O-methylgenistein 7-O-β-Dglucopyranoside 

quercetin 3-O-β-glucopyronoside 

quercetin 3-O-α-rhamnopyranoside 

kaempferol 

7-O-methylquercetin 

cineroside A 

caryophyllene oxide 

teclenone B 

(1β,7R*)-opposit-4(15)-ene-1,7-diol 

Arriaga et al., 2008 

Lignan pinoresinol 

Tephrosia crassifolia Flavonoid crassifolin 

crassichalcone 

Gómez-Garibay et al., 

1999 

Tephrosia egreria Terpenoid geijerene 

pregeijerene 

Arriaga et al., 2005 

Rotenoid Dehydrorotenone. Arriaga et al., 2009b 

Tephrosia elata Flavonoid isopongaflavone 

tephrosin 

Bentley et al., 1987 

8-(3,3-dimethylallyl)-5,7- dimethoxy Lwande et al., 1985a 

flavanone 

obovatin methyl ether 

warangalone 

elatadihydrochalcone Muiva, 2012 

obovatachalcone 

(S)-elatadihydrochalcone Muiva et al., 2009 

obovatachalcone 

obovatin Muiva et al., 2009; Muiva, 

2012 

obovatin methyl ether Muiva et al., 2009; Muiva, 

2012 

Pterocarpan (+)-pisatin Lwande et al., 1985a 

(-)- maackiain 

Rotenoid deguelin Muiva et al., 2009; Muiva, 

2012 

rotenone Muiva, 2012 

Tephrosia elongata Flavonoid elongatin Smalberger et al., 1975 

Tephrosia emoroides Flavonoid emoroidenone Machocho et al., 1995 

emoroidone 

emoroidocarpan 

5-methoxyisolonchocarpin 

Flavene hildegardtene 

Tephrosia falciformis Flavonoid falciformin Khan et al., 1986 

7-hydroxy-8-(γ,γ-dimethylallyl)flavanone 

Alcohol triacontanol Khan et al., 1984 

Tephrosia fulvinervis Flavonoid fulvinervin C Venkataratnam et al., 

1986 

fulvinervin A Venkataratnam et al., 

1986; Venkata et al., 

1985b 

fulvinervin B Venkata et al., 1985b 

Rotenoid α-toxicarol Dagne et al., 1989 

601 



deguelin 

munduserone 

cis-12a-hydroxymunduserone 

Pterocarpan (-)-maackiain 

Tephrosia hamiltonii Flavonoid 5, 7-dimethoxy-8-(2, 3-epoxy-3- 

Tephrosia 

hildebrandtii 

Tephrosia 

hookeriana 

methylbutyl)-flavanone 

602 

Falak and Shoeb 1987 

pongamol 

flemichapparin-B 

flemichapparin-C 

Rajani and Sarma, 1988 

Coumestone 2-methoxy-3,9-dihydroxy coumestone 

Pterocarpan hildecarpidin Lwande et al., 1987 

hildecarpin Lwande et al., 1985b 

Flavonoid trans-tephrostachin Lwande et al., 1986 

trans-anhydrotephrostachin 

Flavonoid hookerianin Prabhakar et al., 1996; 

Vanangamudi et al., 

1997b 

(−)semiglabrin 

lanceolatin A. 

tephrorianin Vanangamudi et al., 

1997b 

rutin 

Tephrosia lanceolata Flavonoid rutin Rangaswami and Rao, 

1955 

Tephrosia leiocarpa Flavonoid tephroleocarpin A Quijano and Rios, 1991 

tephroleocarpin B 

Tephrosia lupinifolia Flavonoid lupinifolin Smalberger et al., 1974 

lupinifolinol 

Tephrosia madrensis Flavonoid 5,7-dimethoxy-8-prenylflavan Gómez et al., 1983 

Tephrosia major Flavonoid 2',6'-dihydroxy-3'-prenyl-4'-methoxy-β- Gomez-Garibay et al., 

hydroxychalcone 

quercetin 

2002 

Sterol β-sitosterol 

stigmasterol 

Triterpene lupeol 

Tephrosia maxima Flavonoid maxima flavanone A Venkata et al., 1994 

maxima isoflavone A Rao et al., 1984a 

maxima isoflavone B Venkata and Sree Rama, 

1985a 

maxima isoflavone C 

maxima isoflavone D 

maxima isoflavone E 

maxima isoflavone F 

maxima isoflavone G 

Rao et al., 1984a 

maxima isoflavone H Venkata and Sree Rama, 

1985a 

maxima isoflavone J Murthy and Rao, 1985; 

Venkata et al., 1994 

maxima isoflavone T Venkata et al., 1994 

Tephrosia multijuga Flavonoid multijuginol 

multijugin 

Vleggaar et al., 1975 

Tephrosia nubica Flavonoidal 

glycoside 

kaemferol 3,7-dirhamnoside 

quercetin 3-galactoside 7-rhamnoside 

quercetin 3,7-dirhamnoside 

Sharaby and Ammar, 1997 

Flavonoid semiglabrin 


apollinine 

lanceolatin A 

Rotenoid rotenones 

deguelin 

Tephrosia Rotenoid dihydrostemonal Dagne et al., 1989 



pentaphylla 

Flavonoid 

9-demethyldihydrostemonal 

6-acetoxydihydrostemonal 

villosin 

sumatrol 

rotenone 

cis-12a-hydroxyrotenone 

6-hydroxyrotenone 

α-toxicarol 

obovatin 

Tephrosia polyphylla Flavonoid 4′-demethyltoxicarol isoflavone 

toxicarol isoflavone 

7-methylglabranin 

Dagne et al., 1992 

Tephrosia 

Rotenoid rotenone Venkataratnam et al., 

procumbens 

sumatrol 

1987 

β -diketone praecansone A 

praecansone B 

Flavonoid obovatin 

7-ethoxy-3,3′,4′-trihydroxyflavone; fisetin 

7-ethyl ether 

7,4′-dihydroxy-3′-methoxyisoflavone 

Tephrosia pumila Flavonoid pumilaisoflavones A 

pumilaisoflavones B 

pumilaisoflavones C 

pumilaisoflavones D 

Yenesew et al., 1989 

pumilanol 

tephrinone 

Ganapaty et al., 2008b 

β-hydroxychalcone 

Praecansone-A. 

Dagne et al., 1988 

Rotenoid rotenone Ganapaty et al., 2008b 

Triterpene lupeol 

Sterol stigmasterol 

Tephrosia purpurea Flavonoid tephrosin 

pongaglabol 

semiglabrin 

Ahmad et al., 1999 

purpuritenin 

purpureamethide 

pongamol 

karanjin 

Sinha et al., 1982 

lanceolatin B Sinha et al., 1982; Chang 

et al., 1997 

(+)-tephrorins A 

(+)-tephrorins B 

(+)-tephrosone 

Chang et al., 2000 

purpurenone Rao and Raju, 1984b 

(+)-purpurin 

(−)purpurin 

dehydroisoderricin 

(−)-maackiain 


(−)-semiglabrin 

Rao and Raju, 1984b; 


terpurinflavone Juma et al., 2011 

pongamol Parmar et al., 1989; Chang 

et al., 1997 

(-)-isolonchocarpin Rao and Raju, 1979 

7,4‘-dihydroxy-3‘,5‘-dimethoxyisoflavone 

(+)-tephropurpurin 

(−)-3-hydroxy-4-methoxy-8,9methylenedioxypterocarpan 

(−)-medicarpin 

3‘-methoxydaidzein 


603 



desmoxyphyllin B 

3,9-dihydroxy-8-methoxycoumestan 

isoglabratephrin 

tephropurpulin A 

Hegazy et al., 2009 

quercitin 

rutin 

Jain et al., 2009 

Ester stigmast-5, 22-dien-34, 21diol-34, 21dihexadecanoate 

Sharma et al., 2008 

Neoflavonoid serratin 7-O-[β-D-glucopyranosyl-(1→4)- Saxena and Choubey, 

glycoside 

O-β-D-galoctopyranoside 

1997 


spinasterol-α 

Chang et al., 1997; Parmar 

et al., 1989 

Acid ursolic acid 

Tephrosia 

Flavonoid quercetols A Gómez-Garibay et al., 

quercetorum 

quercetols B 

quercetols C 

1988 

Tephrosia semiglabra Flavonoid glabratephrin Vleggaar et al., 1978 

semiglabrinol 

semiglabrin 

Smalberger et al., 1973 

Tephrosia sinapou Flavonoid toxicarine 

7-O-methylglabranine 

tephrowatsin A 

quercetol B 

flamichapparin B 

Martinez et al., 2012 

Coumarin 2,3-dihydro-p-coumaric acid 

Rotenoid tephrosin 

rotenolone 

deguelin 

6-oxo-6a,12a-dehydrodeguelin 

6-oxo-6a,12a-dehydro-α-toxicarol 

6a,12a-dehydrorotenone 

rotenonone 

villosone 

Tephrosia spinosa Flavonoid spinochalcone C 

spinoflavanones A 

spinoflavanones B 

fulvinervin A 

Rao and Prasad, 1992 

3′,5′-diisopentenyl-2′,4′-dihydroxychalcone 

tephrospinosin 

Sharma and Rao, 1992 

spinochalcones A 

spinochalcones B 

flemistrictin A 

Rao and Prasad, 1992 

Flavonol glycoside eupalitin 3-O-b-D-galactopyranoside Vanangamudi et al., 

1997a; Chakradhar et al., 

2005 

Tephrosia tepicana Flavonoid tepicanol A Gómez-Garibay et al., 

1997 

Tephrosia tinctoria Flavonoid 5,7-di-O-prenylbiochanin A 

7-O-methylglabranin 


flemichapparin B 

Khalivulla et al., 2008 

2-hydroxy tephrosin 

tephrinone 

Ganapaty et al., 2009 

lupinifolin 

7-O-methyl glabranin 

Ganapaty et al., 2010 

Rotenoid rotenone 

dehydrodeguelin 


Acid betulinic acid 

Tephrosia toxicaria Flavonoid iso-obovatin Vasconcelos et al., 2009 

obovatin Vasconcelos et al., 2009; 

604 



Jang et al., 2003 

6a,12a-dehydro-β-toxicarol 

6a,12a-dehydro-α-toxicarol 

α-toxicarol 

toxicarol Clark, 1930 

(2S)-5-hydroxy-7-methoxy-8-[(E)-3-oxo-1- Jang et al., 2003 

butenyl]flavanone 

Rotenoid 

isoliquiritigenin 

genistein 

chrysoeriol 

sumatrol 

4‘,5‘-dihydro-11,5‘-dihydroxy-4‘methoxytephrosin 

11-hydroxytephrosin 

Coumarin marmesin 

Triterpene lupenone 

Ester benzyl benzoate 

benzyl trans-cinnamate 

Tephrosia tunicata Flavonoid tunicatachalcone Andrei et al., 2000 

Tephrosia uniflora Flavonoid elongatin Abreu and Luis, 1996 

Rotenoid 12a-hydroxyrotenone 


stigmasterol 

Tephrosia viciodes Flavonoid enantiomultijugin Gómez-Garibay et al., 

1992 

Tephrosia villosa Flavonoid (2S)-5,4′-dihydroxy-7-O-[(E)-3,7-dimethyl- Madhusudhana et al., 

2,6-octadienyl]flavanone 

(2S)-5,4′-dihydroxy-7-O-[(E)-3,7-dimethyl- 

2,6-octa-dienyl]-8-C-[(E)-3,7-dimethyl-2,6octadienyl]flavanone 

7-O-methylglabranin 

tephcalostan 

12a-dehydro-6-hydroxysumatrol 

2010 

7-methylglabranin Jayaraman et al., 1980 

villosin 

villosone 

villol 

villinol 

David Krupadanam et al., 

1997 

tephrinone Rao and Srimanarayana, 

1981 

Triterpenoid lupenone Prashant and Krupadanam 

1993 

Triterpene lupeol Ganapaty et al., 2008a 


Rotenoid 12a-dehydro-6-hydroxysumatrol Prashant and Krupadanam 

1993 

rotenone 

dehydrorotenone 

Ganapaty et al., 2008a 

6a,12a-dehydro,2,3,6- trimethoxy-8-(3’,3’- Prashant and 

dimethylallyl)-9,11dihydroxy rotenone 

12a-hydroxy toxicarol 

Krupadanam, 1993 

Tephrosia viridiflora Flavonoids viridiflorin Gómez et al., 1985 

Tephrosia vogelii Sesquiterpene (1β,6α,10α)-guai-4(15)-ene-6,7,10-triol Wei et al., 2009 

Lignan (+)-lariciresinol 9′-stearate 

Rotenoid deguelin Kalume et al., 2012; 

Delfel et al., 1970; Gills, 

1992 

tephrosin 

toxiconol 

tephrosal 

Gills, 1992 

Flavonoid quercitin 

Tephrosia Flavonoid tephrowatsin A Gómez et al., 1985 

605 



watsoniana 

Tephrosia woodii Flavonoid 

tephrowatsin B 


tephrowatsin D 

tephrowatsin E 

oaxacacin 

mixtecacin 

Dominguez et al., 1983 

606 



607 



608 



O 

O 

O OMe 

O 

O 

H 

O 

Enantiomultijugin 

O 

O 

O 

Flemichapparin C 

O 

O 

H 

OMe 

609 

HO 

OH 

OMe 

O 

O 

Emoroidone 

O O 

O 

Fulvinervin B 

OH 



610 



611 



612 



613 



HO 

O O 

OH 

Quercetol A 

OMe 

614 

O 

HO 

Spinochalcone C 

O 



O 

O 

HO 

O 

O 

Tephrocarpin 

OMe 

OH 

615 

HO 

H 

H H 

Stigmasterol 

H 

H 

H 



MeO 

OMe 

O 

616 

O 

Tephrowatsin B 

O 

O O 

Tephrospiroketone 1 

MeO 

OH 

O 

OMe 

OMe 

OMe 

© 2013 Inforesights Publishing UK 

O 

O 

Trans tephrostachin


MeO 

OMe 

617 

O 

5 7 dimethoxy 8 prenylflavan 



618 

O 

HO 

C 

CH 

HC OH 

Caffeic acid 

OH 



619 

O 

O 

O 

O 

O 

Fulvinervin A 

OH 

O 

Maxima isoflavone A 

O 

© 2013 Inforesights Publishing UK 

O 

O


620 



Some of the compounds isolated have been studied for their pharmacological actions (see 

table 2). The activities reported include anticancer, antiplasmodial, larvicidal, and others. There 

are many compounds in Table 1 whose activities are not studied under the genus Tephrosia 

but if we look into the literature, we find their presence in other genera and their activities 

determined for example Pseudosemiglabrin, Flemichapparin, Caryophyllene oxide, deguelin, 

pongamol, lupeol, possess platelet aggregation antagonism, antifungal, antifungal, anticancer, 

anticonvusant, and antiinflammatory respectively (Pirrung and Lee, 1995; Gahlot et al., 

2012; Yang et al., 2000; Udeani et al., 1997; Basu et al., 1994; Geetha and Varalakshmi, 

2001). Caffeic acid and rutin, which are also found in Phyllanthus sellowianus have analgesic 

activity (Calixto et al., 1998). 

Table 2. Pharmacological actions of isolated compounds from genus Tephrosia. 

Species Compound Activity Reference 

Tephrosia calophylla calophione A Cytotoxic Ganapaty et al., 2009 

Tephrosia candida candidone Cytotoxic Ganapaty et al., 2009; 

Roy et al., 1986 

pongachin Ganapaty et al., 2009; 

Parmar et al., 1988 

candidachalcone Estrogenic activity Hegazy et al., 2011 

Tephrosia elata tephrosin 

isopongaflavone 

Antifeedant Bentley et al., 1987 

rotenone Larvicidal, antifeedant Muiva, 2012; Bentley et 

al., 1987 

(S)-elatadihydrochalcone Antiplasmodial Muiva, 2012 

obovatin methyl ether 

praecansone 

Muiva, 2012 

Tephrosia emoroides emoroidenone Antifeedant Machocho et al., 1995 

Tephrosia ergeria dehydrorotenone Antioxidant, larivcidal Arriaga et al., 2009a 

Tephrosia hildebrandtii hildecarpin Insect antifeedant 

Antifungal 

Lwande et al., 1985 

Tephrosia pulcherrima pulcherrimin Cytotoxic Ganapaty et al., 2009 

Tephrosia pumila pumilanol Antiprotozoal Ganapaty et al., 2008 

Tephrosia purpurea (+)-tephrorin A Cancer chemopreventive 

activity 


621 



(+)-tephrorin B 

(+)-tephrosone 

7,4‘-dihydroxy-3‘,5‘- 

dimethoxyisoflavone 

622 


(+)-tephropurpurin 

(+)-purpurin 

pongamol 

lanceolatin B 

(−)-maackiain 

(−)-3-hydroxy-4-methoxy - 

8, 9- methylenedioxy 

pterocarpan 

(−)-medicarpin 

terpurinflavone Antiplasmodial Juma et al., 2011 

Tephrosia spinosa eupalitin-3-O-β-D-glucoside Anti-inflammatory Chakradhar et al., 2005 

Tephrosia tinctoria 2-hydroxy tephrosin Antiplasmodial Ganapaty et al., 2009 

tephrinone 

Tephrosia toxicaria (2S)-5-hydroxy-7-methoxy- 

8-[(E)-3-oxo-1- 

butenyl]flavanone 

Cancer chemopreventive 

activity 

Jang et al., 2003 

4‘,5‘-dihydro-11,5‘dihydroxy-4‘methoxytephrosin 

isoliquiritigenin 

genistein 

chrysoeriol 

obovatin Antioxidant Vasconcelos et al., 2009 

toxicarol Fish poison Clark, 1930 

α-toxicarol Larvicidal Vasconcelos et al., 2009 

Tephrosia vogelii deguelin Larvicidal Muiva, 2012; Kalume et 

al., 2012 

It can be concluded from the above discussion that if, for example, any species of 

genus Tephrosia having rutin or caffeic acid as its major component, is not reported for analgesic 

activity, may possess it. So in this way this methodology can give us a hint or base, which 

study to be carried on plant. 

Pharmacological profile of plants from genus Tephrosia 

Several plants of the genus have studied for their medicinal and therapeutic potential. 

A brief description of the work done so far is given below: 

Antioxidant activity 

Only a few species of Genus Tephrosia have been studied for their antioxidant activity. 

In 2007, G.P. Choudhary studied the ethanolic extract of Tephrosia purpurea for its antioxidant 

activity (Choudhary, 2007). The aqueous extract of the whole plant of Tephrosia 

purpurea also showed free radical scavenging activity in DPPH test (Gunjegaonkar et al., 

2010). From Tephrosia egregia the ethyl acetate and methanol extracts showed high antioxidant 

activities (Arriaga et al., 2009a). Obovatin, a flavonoid present in Tephrosia toxicaria 

showed significant antioxidant acivity of IC50 3.370 μg/mL. It was also seen that the methanol 

fraction of the ethanol extract from roots had the highest antioxidant activity (Vasconcelos 

et al., 2009). Tephrosia villosa also possess antioxidant activity due to the presence of 

20(29)-lupen-3-one, a compound also identified in Daedaleopsis tricolor where it inhibited 

lipid peroxidation by 6.4% (Prashant and Krupadanam 1993; Kim et al., 2001). The ethanol 



ether extract of Tephrosia vogelii seeds also showed antioxidant and free radical scavenging 

activity (Li et al., 2010). 

Antibacterial activity 

The species from Genus Tephrosia have also been studied for their antibacterial activity. 

Tephrosia vogelii was found to possess antimicrobial activity (Wanga et al., 2007). The 

dichloromethane extract from the roots and leaves was tested against S. aureus, E. coli and F. 

phoseolida. Hu et al., in 2011 also studied the antimicrobial and bactereostatic activity of 

ethanol and aqueous extract from Tephrosia vogelii seeds on E. coli, S. aureus and S. paratyphi 

B. and proved the antibacterial efficacy of the plant to be significant at high doses (Hu et 

al., 2011). The root extract of Tephrosia villosa showed moderate antibacterial and anti 

fungal activity (Ganapaty et al., 2008a). In another study on Tephrosia villosa the fruit, leaf, 

and root extract showed activity against C.neoformans, E.coli and B.anthracis respectively. 

The ethanolic twig extract was most active against C.neoformans and S.typhi (Nondo et al., 

2011). In case of Tephrosia purpurea, studies have been made on the antimicrobial activity 

of methanolic extract of Tephrosia purpurea roots on B. subtilis, S. aureus, M. luteus, the 

gram positive bacteria and the gram negative including E. coli, P. aeruginosa, and S. typhimurium 

(Gupta et al., 2008). In another study on Tephrosia purpurea, the roots showed antimicrobial 

activity against P. aeruginosa and no activity against S. aureus and E.coli (BNLD 

Rangama et al., 2009). Chinniah et al., in 2009 and Annalakshmi et al., in 2009 proved 

Tephrosia purpurea to have marked activity against H. pylori, an agent responsible for GIT 

ulcers (Chinniah et al., 2009; Annalakshmi et al., 2009). The methanolic leaf extract from 

Tephrosia tinctoria showed activity against B. subtilis, S. marceseans, and low activity for B. 

cereus and P. aeuriginosa (Ganapaty et al., 2010). Tephrosia deflexa and its isolated compounds 

were studied for antibacterial activity (Kare et al., 2006). The antibacterial activity of 

Tephrosia linearis has also been reported (Ratsimamanga et al., 1994). 

Antifungal activity 

In our literature survey, we found less work on antifungal activity of species from Genus 

Tephrosia. Only three species are known to possess antifungal potential. The methanolic 

extract of Tephrosia purpurea showed significant activity against A. niger and C. albicans 

(Gupta et al., 2008). Tephrosia hildebrandtii showed antifungal activity against C.cucumerinum. 

The activity was found to be related to a chemical compound isolated from its roots 

(see table 2) (Lwande et al., 1985b). Tephrosia tinctoria also showed activity against A. 

niger, C. albicans. The methanolic extract was found to be more active against the aforementioned 

organisms. However the methanolic extract showed no activity against S. cerevisiae 

(Ganapaty et al., 2010). 

Antiprotozoal and anti plasmodial activity 

Extract from the seed pods of Tephrosia elata showed antiplasmodial activity (Muiva 

et al., 2009; Muiva, 2012). Flavonoid extracted from the roots of Tephrosia pumila also showed 

activity against L. donovani, T. b. rhodesiense and T. cruzi (Ganapaty et al., 2008b). 

Isolated flavonoids from the root of Tephrosia tinctoria were studied for antiprotozoal and 

623 



antiplasmodial activities against T. b. rhodesiense, T. cruzi, L. donovani, and P. falciparum 

(Ganapaty et al., 2009a). Ganapaty, also studied the antiprotozoal activity of three Tephrosia 

species, namely, T. pulcherrima, T. pumila, and T. calophylla on Leishmania, Trypanosoma 

and Plasmodium parasites (Ganapaty et al., 2009c). Chloroquine sensitive and chloroquine 

resistant strains of P. falciparum were inhibited by the extracts from the stem of Tephrosia 

purpurea with IC50 values of 10.47 ± 2.22 μg/ml and 12.06 ± 2.54 μg/ml, respectively (Juma 

et al., 2011). Tephrosia purpurea has also been studied for antileishmanial activity in hamsters 

and Indian langular monkeys infected by L. donovani (Sharma et al., 2003). 

Anti pyretic and Anti inflammatory activity 

In 2010, Sandhya et al., studied the anti inflammatory activity of two species of Tephrosia 

namely Tephrosia maxima and Tephrosia purpurea by HRBC membrane stabilizing 

method. Both plants showed almost equal activity at doses of 500ug/ml. Tephrosia maxima 

giving 79.49% and Tephrosia purpurea giving 79.01% protection (Sandhya et al., 2010). 

Another study on Tephrosia purpurea root extracts showed its antipyretic and anti inflammatory 

activity (Valli et al., 2011). The methanolic extract of Tephrosia vogelii showed significant 

analgesic and anti-inflammatory activity in mice and rats using hot plate method and egg 

albumin induced oedema respectively (Adaudi et al., 2009). The root extract of Tephrosia 

sinapou showed to possess significant anti-inflammatory activity. The extract reduced inflammatory 

leukocyte recruitment, oxidative stress and other parameters involved directly or 

indirectly to the process of inflammation (Martinez et al., 2012). Tephrosia spinosa also showed 

anti inflammatory activity in an experimental model of carrageenin induced paw edema. 

The standard drug used was indomethacin (Chakradhar et al., 2005). The antipyretic activity 

of Tephrosia bracteolata has also been reported (Onaolapo et al., 2009). 

Anticancer and cytotoxic activity 

Cytotoxicity of some chemical compounds found in Tephrosia calophylla and Tephrosia 

candida have been studied using different cell lines (Ganapaty et al., 2009a; Ganapaty et 

al., 2009b; Roy et al., 1986; Parmar et al., 1988). The cytotoxicity of Tephrosia pulcherrima 

and Tephrosia pumila has also been studied by Ganapaty et al., in 2009 using HT-29 and 

RAW cell lines (Ganapaty et al., 2009c). In 2011 Kishore et al., mentioned Tephrosia purpurea 

containing an important chemical, B-sitosteol having anticancer and cancer protective 

activities against prostatic, breast and colonic carcinomas. In addition to the aforementioned 

activities of B-sitosterol, it is also an antioxidant and has significant effect on hypercholesterolemia 

and BPH (Kishore and Roy, 2011). In another study the anticarcinogenic activity 

of Tephrosia purpurea extract was tested in an experimental model of hepatocarcinoma in 

rats. The extract showed significant cancer chemoprevention (Hussain et al., 2012). Shanmugapriya 

et al., also studied the anticarcinogenic potential of Tephrosia purpurea in HELA 

cervical cancerous cell line. Different extracts were tested out of which ethyl acetate 

produced the most potent effect (Shanmugapriya et al., 2011). In a study by Subhadra, three 

species namely, Tephrosia calophylla, Tephrosia maxima and Tephrosia purpurea showed 

significant cytotoxic activity out of which Tephrosia calophylla showed the maximum activity 

(Subhadra et al., 2011). The ethanolic fruit and root extract of Tephrosia villosa showed 

toxicity to brine shrimp whereas the extract from leaves and twigs was found to be non toxic 

(Nondo et al., 2011). The ethyl acetate extract from stems of Tephrosia toxicaria possess 

624 



flavonoids having cancer chemopreventive activities (Jang et al., 2003). The flavonoids extracted 

from Tephrosia tinctoria possess cytotoxic activity tested in Cell line L-6 (Rat skeletal 

muscle myoblasts) (Ganapaty et al., 2009a). Tephrosia calophylla was also found to possess 

anticancer activity. The root extract inhibited growth and induced apoptosis in the human breast 

carcinoma (Adinarayana et al., 2009). Tephrosia vogelii root and leaf extract was found 

to be toxic to brine shrimps at doses of LC50: 0.960; 0.958 μg/ml, respectively (Wanga et al., 

2007). 

Hepatoprotective activity 

In 2011, Shah et al., studied the hepatoprotective effect of Tephrosia purpurea in 

CCl4 induced hepatotoxicity in rats. The ethyl acetate fraction at doses of 50mg/kg was found 

to be effective and comparable to silymarin (Rajal Shah et al., 2011). The hepatoprotective 

effect of Tephrosia calophylla has also been reported (Adinarayana et al., 2011). 

Animal feed 

In an effort to find new and cheap sources of food for animals, several species of genus 

Tephrosia have been studied. The nutritive value of three species of Tephrosia, namely, 

Tephrosia candida, Tephrosia bracteolata, and Tephrosia linearis have been studied (Babayemi 

et al., 2003). According to Babayemi and Bamikole, a mixture of Tephrosia candida 

leaves and guinea grass can serve as a good animal feed. The mixture has an additional benefit 

of low methane production upon fermentation (Babayemi and Bamikole. 2006b). Tephrosia 

bracteolata can serve as a good diet in laying hens both from nutritive and economic 

aspect (Akande et al., 2008). Tephrosia vogelii, Tephrosia candida, and Tephrosia purpurea 

can also be a good addition in the diet of ruminants (Mbomi et al., 2011). The use of Tephrosia 

candida and Tephrosia bracteolata in goats has also been established (Babayemi and 

Bamikole 2006a). A study on Tephrosia candida seeds has also been reported (Babayemi and 

Bamikole 2007). 

Larvicidal, insecticidal and antifeedant activity 

Different species from the genus have been studied for larvicidal, insecticidal, and 

antifeedant activities. There is an extensive work on the study of Tephrosia as an agent to 

control the population of insects harmful to animals and plants. 

The hexane extract from Tephrosia egregia showed potent larvicidal activity against 

aedes aegypti (Arriaga et al., 2009a). The whole plant extract of Tephrosia purpurea was tested 

for its larvicidal activity against the larvae of Culex quinquefasiciatus. The extract showed 

100% mortality in very small doses suggesting its beneficial use in controlling the mosquito 

reproduction (Deepak Kumar et al., 2012). The extracts of Tephrosia vogelii also possess 

larvicidal activity and therefore can be used to control mosquitoes (Matovu and Olila. 2007). 

The ethanolic extract of roots, leaves, fruit and twigs of Tephrosia villosa showed significant 

activity against C. quinquefasciatus larvae (Nondo et al., 2011). The ethanol extract from 

roots, stems, leaves, and pods and some fractions of Tephrosia toxicaria were tested for lavicidal 

activity with the larvae of Aedes aegypti. The ethanolic root extract, hexane and chlor- 

625 



oform fractions had (LC50 47.86 ppm) (LC50 23.99 ppm) and (LC50 13.80 ppm) respectively 

(Vasconcelos et al., 2009). Tephrosia nyikensis have been reported to possess larvicidal 

activity on Anopheles mosquito’s larvae (Wanjala et al., 2006). The oil obtained from Tephrosia 

cinerea showed larvicidal activity against Aedes aegypti larvae (Arriaga et al., 2008). 

The chloroform and methanol extracts of Tephrosia nubica were tested against Spodoptera 

littoralis and Agrotis ipsilon. The population of the pests was reduced due to the effect of the 

extract on all the stages of growth (Sharaby and Ammar, 1997). Tephrosia vogelii leaf extract 

was found to be effective in controlling ticks, an important insect and ectoparasite (Gadzirayi 

et al., 2010). Tephrosia magropoda is also reported to have insecticidal properties (Tatteksfield 

and Gimingham, 1932). In 2012, Kalume et al., reported the acaricidal activity of leaf 

extracts of Tephrosia vogelii on tick Rhipicephalus appendiculatus and mentioned its advantage 

of being economical than synthetic compounds (Kalume et al., 2012). The insecticidal 

property of Tephrosia purpurea whole plant was tested against Callosobruchus maculates, 

the pest on Phaseolus mungo (Diwan and Saxena, 2010). In 1992, Kole et al., isolated a 

rotenoid, amorpholone from Tephrosia candida having potent insecticidal properties (Kole et 

al., 1992). Tephrosia elata showed significant antifeedant activity against M. testulalis, S. 

exempta and E. sacchariana. The antifeedant activity is attributed to the presence of rotenoid 

compounds (Bentley et al., 1987). The larvicidal activity from seed pods of Tephrosia elata 

and Tephrosia aequilata has also been studied by Muiva, against the larvae of Aedes aegypti 

(Muiva, 2012). Antifeedant activity of flavonoids from Tephrosia emoroides was tested 

against Chilo partellus, a very destructive pest of maize. Emoroidenone, a flavonoid isolated 

showed strong feeding deterrence of 66.1% against the larvae at a dose of 100 μg (Machocho 

et al., 1995). The roots of Tephrosia hidebrandtii also possess antifeedant activity against the 

pest, Maruca testulalis (Lwande et al., 1985). 

Antidiabetic activity 

The aqueous seed extract of Tephrosia purpurea showed significant antihyperglycemic 

activity in streptozotocin induced diabetic rats (Pavana et al., 2009). The ethanolic extract 

of from Tephrosia villosa leaves showed reduction in glucose level and pancreatic cell 

regeneration in alloxan induced diabetes in rats (Ahmad et al., 2009). Balakrishnan et al., 

also repoted antidiabetic activity of extract from root of Tephrosia villosa (Balakrishnan et 

al., 2007). 

GIT activity 

Tephrosia vogelii leaf extract exerted a stimulant effect on the GIT smooth muscles. 

This was demonstrated by the contraction of the ileum isolated from guinea pig hence showing 

the purgative property of the plant (Dzenda et al., 2008b). Aqueous extract of Tephrosia 

purpurea root showed gastric ulcer healing and cytoprotective activities (Deshpande and 

Shah 2008). The extract of Tephrosia calophylla leaves showed significant antiulcer and cytoprotective 

activity at doses of 50mg/kg and 100mg/kg (Divya, et al., 2011). 

Antihyperlipidemic effect 

The antihyperlipidemic effect of Tephrosia calophylla has been studied in wistar albino 

rats (Mohan, 2011). The leaf extract of Tephrosia purpurea showed antihyperlipi-demic 

626 



activity in an experimental model of diabetic rats (Pavana et al., 2007). Akhtar et al., also 

studied Tephrosia purpurea for the same purpose and found a significant reduction in all the 

parameters (Akthar et al., 2011). 

Toxicity 

Tephrosia purpurea extract was evaluated by Talib et al., in 2012 for its toxicity in 

rodents. A dose up to 2000mg/kg was well tolerated in the acute toxicity studies whereas in 

sub acute toxicity studies, a dose 200mr/kg and 400 mg/kg showed no significant change in 

any of the parameters thus concluding that the plant is safe for use in treatment of different 

diseases (Talib Hussain et al., 2012). Tephrosia toxicaria used as a fish poison was studied 

by Clark in 1930. A compound, Toxicarol was identified as the major component (Clark, 

1930). The toxicity of Tephrosia vogelii was reported on mice. The signs were similar to 

those associated with the toxicity from rotenone. The LD50 of leaf extract calculated was 

134.16 mg/kg (Dzenda et al., 2008a). The chloroform extract of Tephrosia tinctoria leaves 

exhibited significant piscicidal activity compared to methanolic extract in gold fish (Ganapaty 

et al., 2010). Toxic hepatopathy was reported in sheep grazing on Tephrosia cinerea. The 

disease was also experimentally induced in the sheep in order to confirm the results (Santos 

et al., 2007). Tephrosia apollinea was also found to be toxic in a study on goats (Suliman et 

al., 1982). The toxicity of Tephrosia bracteolata has also been studied (Onaolapo et al., 

2009). In a study on mice Cai et al., found Tephrosia candida to be safe and no significant 

signs of toxicity were observed (Cai et al., 2010). 

Miscellaneous activities 

The root extract of Tephrosia purpurea showed xanthine oxidase inhibitory activity 

compare with standard, Allopurinol (Nile and Khobragade, 2011). Patel et al., studied the effect 

of Tephrosia purpuria on polycystic ovary syndrome (PCOS) in rats. (PCOS) was induced 

by the administration of Letrozole. The dried seed powder given orally showed normalization 

in the estrous cycle and reduction in the weight of the reproductive system as well as 

of the ovary (Patel and Thakor, 2012). Kumar et al., found Tephrosia purpuria to be effective 

anxiolytic agent and comparable to the standard drug, Diazepam. The hydroalcoholic extract 

at a dose of 200mg/kg and 400mg/kg orally was administered to mice in different maze models 

in the study (Kumar, et al., 2011). The acetylcholinesterase inhibitory activity of Tephrosia 

purpurea and neurobehavioral studies were made on zebra fish, a model for the study of 

neurodegenerative activities (Kannan and Vincent, 2012). Tephrosia purpurea has also been 

proved for its antiepileptic effect (Asuntha et al., 2010). Lodhi et al., studied the flavonoidal 

extract of Tephrosia purpurea and proved its potential for healing burn wounds. This activity 

is supposed to be due to its free radical scavenging property (Lodhi et al., 2010). The anti 

allergic effect of Tephrosia purpurea has been reported (Gokhale and Saraf 2000). The 

extract of Tephrosia purpurea stabilized mast cells significantly showing its usefulness in the 

treatment and management of asthma (Gajera Paresh Lallubhai and Dalal Mittal, 2011). In 

another study Tephrosia purpurea showed spasmolytic activity in the trachea of guinea pigs 

thus strengthening the view of its use in asthma (Soni et al., 2004). Tephrosia purpurea has 

also been studied for its immunomodulatory effect (Damre et al., 2003). Ashokkumar et al., 

studied the diuretic activity of methanol extract of Tephrosia purpurea (Ashokkumar et al., 

2012). The aqueous extract from roots of Tephrosia purpurea also posses antilithiatic activity 

627 



(Swathi et al., 2008). Still another study was made on the Tephrosia purpurea leaves for its 

protective and curative ability for renal injury in rats (Jain and Singhai, 2009). Study on 

chemical constituents of Tephrosia candida revealed a sesquiterpene having significant estrogenic 

activtity (Hegazy et al., 2011). The chloroform and methanolic extract of Tephrosia 

spinosa showed significant ant helmintic activity against earth worms (Pheretima posthuma) 

(Ilango et al., 2011). The leaf extract of Tephrosia vogelii was found to possess significant 

anthelmintic activity against Ascaridia galli, a parasite in chicken (Siamba et al., 2007). The 

methanol extract of Tephrosia vogelii produced significant reduction in the blood pressure of 

cats (Adaudi et al., 2009). 

Conclusion and discussion 

The plants of genus Tephrosia are of high therapeutic importance. We can see that a 

large number of species are studied for their chemical constituents but the number of isolated 

compounds from individual specie is very few with some exceptions. Mostly studied compounds 

include flavonoids and rotenoids. Studies on oil composition are very less. The genus 

has significant anticancer and larvicidal potential. 

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