Antimalarial activity of some plants traditionally used in treatment of malaria in Msambweni district of Kenya J.M.Nguta a *, J.M.Mbaria a, D.W.Gakuya.

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1 Antimalarial activity of some plants traditionally used in treatment of malaria in Msambweni district of Kenya J.M.Nguta a *, J.M.Mbaria a, D.W.Gakuya b, P.K.Gathumbi c, J.D.Kabasa d, S.G.Kiama e

2 Natural products from plants as drug sources The material culture of every civilization throughout the world is based more on plants than on animals. People of the earth have depended for along time on plants as a source of food, clothing, shelter, transportation, medicines, rituals and traditions The plant kingdom met the health needs of humans when no synthetic drugs were available and no concept of surgical management existed (Sharing innovative experiences)

3 Cont. The world has witnessed growing scientific and commercial interests in medicinal plants, mainly due to their immense economic potential and the widespread cultural acceptability of plant based products. An inventory of medicinal plants compiled by WHO lists 21,000 species of medicinal plants. According to WHO, 80% of the 5 billion people in the dev. World rely on herbal remedies for their basic health care needs.

4 Cont. The dev. world is rich in natural resourses, including floral resources However, the south's floral wealth has not been utilized for the benefit of its people.

5 Ethnopharmacology to modern medicine Drug/ChemicalActionPlant Source AcetyldigoxinCardiotonicDigitalis lanata (Grecian foxglove, woolly foxglove) AdonisideCardiotonicAdonis vernalis (pheasant's eye, red chamomile) AescinAntiinflammatoryAesculus hippocastanum (horse chestnut) AesculetinAntidysenteryFrazinus rhychophylla AgrimopholAnthelminticAgrimonia supatoria AjmalicineTreatment for circulatory disordersRauvolfia sepentina AllantoinVulnerarySeveral plants Allyl isothiocyanateRubefacientBrassica nigra (black mustard) AnabesineSkeletal muscle relaxantAnabasis sphylla AndrographolideTreatment for baccillary dysenteryAndrographis paniculata AnisodamineAnticholinergicAnisodus tanguticus AnisodineAnticholinergicAnisodus tanguticus ArecolineAnthelminticAreca catechu (betel nut palm) AsiaticosideVulneraryCentella asiatica (gotu cola)

6 Ethnopharmacology to modern medicine (Cont.) Drug/ChemicalActionPlant Source AtropineAnticholinergicAtropa belladonna (deadly nightshade) Benzyl benzoateScabicideSeveral plants BerberineTreatment for bacillary dysenteryBerberis vulgaris (common barberry) BergeninAntitussiveArdisia japonica (marlberry) Betulinic acidAnticancerousBetula alba (common birch) HyoscyamineAnticholinergicHyoscyamus niger (black henbane, stinking nightshade, henpin) IrinotecanAnticancer, antitumor agentCamptotheca acuminata Kaibic acudAscaricideDigenea simplex (wireweed) KawainTranquilizerPiper methysticum (kava kava) KheltinBronchodilatorAmmi visaga Lanatosides A, B, CCardiotonicDigitalis lanata (Grecian foxglove, woolly foxglove) LapacholAnticancer, antitumorTabebuia species (trumpet tree) a-LobelineSmoking deterrant, respiratory stimulantLobelia inflata (Indian tobacco) MentholRubefacientMentha species (mint)

7 Ethnopharmacology to modern medicine (Cont.) Drug/ChemicalActionPlant Source MonocrotalineTopical antitumor agentCrotalaria sessiliflora MorphineAnalgesicPapaver somniferum (poppy) NeoandrographolideTreatment of dysenteryAndrographis paniculata NicotineInsecticideNicotiana tabacum (tobacco) Nordihydroguaiaretic acidAntioxidantLarrea divaricata (creosote bush) NoscapineAntitussivePapaver somniferum (poppy) OuabainCardiotonicStrophanthus gratus (ouabain tree) PachycarpineOxytocicSophora pschycarpa PalmatineAntipyretic, detoxicantCoptis japonica (Chinese goldenthread, goldthread, Huang-Lia) PapainProteolytic, mucolyticCarica papaya (papaya) PapavarineSmooth muscle relaxantPapaver somniferum (opium poppy, common poppy) PhyllodulcinSweetenerHydrangea macrophylla (bigleaf hydrangea, French hydrangea) PhysostigmineCholinesterase inhibitorPhysostigma venenosum (Calabar bean) PicrotoxinAnalepticAnamirta cocculus (fish berry) PilocarpineParasympathomimeticPilocarpus jaborandi (jaborandi, Indian hemp)

8 Ethnopharmacology to modern medicine (Cont.) Drug/ChemicalActionPlant Source PodophyllotoxinAntitumor, anticancer agentPodophyllum peltatum (mayapple) Protoveratrines A, BAntihypertensivesVeratrum album (white false hellebore) PseudoephredrineSympathomimeticEphedra sinica (ephedra, ma huang) nor-pseudoephedrineSympathomimeticEphedra sinica (ephedra, ma huang) QuinidineAntiarrhythmicCinchona ledgeriana (quinine tree) QuinineAntimalarial, antipyreticCinchona ledgeriana (quinine tree) Qulsqualic acidAnthelminticQuisqualis indica (Rangoon creeper, drunken sailor) RescinnamineAntihypertensive, tranquilizerRauvolfia serpentina ReserpineAntihypertensive, tranquilizerRauvolfia serpentina RhomitoxinAntihypertensive, tranquilizerRhododendron molle (rhododendron) RorifoneAntitussiveRorippa indica RotenonePiscicide, InsecticideLonchocarpus nicou RotundineAnalagesic, sedative, traquilizerStephania sinica RutinTreatment for capillary fragilityCitrus species (e.g., orange, grapefruit)

9 Ethnopharmacology to modern medicine (Cont.) Drug/ChemicalActionPlant Source SanguinarineDental plaque inhibitorSanguinaria canadensis (bloodroot) SantoninAscaricideArtemisia maritma (wormwood) Scillarin ACardiotonicUrginea maritima (squill) ScopolamineSedativeDatura species (e.g., Jimsonweed) Sennosides A, BLaxativeCassia species (cinnamon) SilymarinAntihepatotoxicSilybum marianum (milk thistle) SparteineOxytocicCytisus scoparius (scotch broom) SteviosideSweetenerStevia rebaudiana (stevia) StrychnineCNS stimulantStrychnos nux-vomica (poison nut tree) TaxolAntitumor agentTaxus brevifolia (Pacific yew) TeniposideAntitumor agentPodophyllum peltatum (mayapple or mandrake) a-Tetrahydrocannabinol (THC)Antiemetic, decreases occular tensionCannabis sativa (marijuana) TetrahydropalmatineAnalgesic, sedative, tranquilizerCorydalis ambigua TetrandrineAntihypertensiveStephania tetrandra TheobromineDiuretic, vasodilatorTheobroma cacao (cocoa) TheophyllineDiuretic, bronchodilatorTheobroma cacao and others (cocoa, tea) ThymolTopical antifungalThymus vulgaris (thyme)

10 Ethnopharmacology to modern medicine (Cont.) Drug/ChemicalActionPlant source TrichosanthinAbortifacientTrichosanthes kirilowii (snake gourd) TubocurarineSkeletal muscle relaxantChondodendron tomentosum (curare vine) ValapotriatesSedativeValeriana officinalis (valerian) VasicineCerebral stimulantVinca minor (periwinkle) VinblastineAntitumor, Antileukemic agentCatharanthus roseus (Madagascar periwinkle) VincristineAntitumor, Antileukemic agentCatharanthus roseus (Madagascar periwinkle) YohimbineAphrodisiacPausinystalia yohimbe (yohimbe) YuanhuacineAbortifacientDaphne genkwa (lilac) YuanhuadineAbortifacientDaphne genkwa (lilac)

11 Ctotoxicity of crude plant extracts  Nguta et al., Pharmacologyonline 2: 458-478 (2011); 4 th ICDDT (Dubai, 12-15 th /02/12)  Screened crude extracts: 170  97.6% of all the screened organic extracts and 73% of the investigated aqueous extracts demonstrated LC 50 values <1000 μg/ml, hence non toxic  Hence could make safe antimalarial formulations

12 In vivo ant malarial activity Unpublished data 4-day suppressive test(Peters et al., 1975)  Adansonia digitata, Zanthoxylum chalybeum, Launaea cornuta and Canthium glaucum had 60.47%, 44.93%, 38.13% and 31.98% chemosuppression respectively-all acqueous  Chloroquine (positive control) had 87.23% Both Adansonia digitata and Canthium glaucum were non toxic Possible candidates for drug discovery????

13 Treatments against average chemosuppressions

14 Treatments against average parasitaemia

15 Phytochemical analysis Aqueous extractsAlkaloidsFlavonoidsSesquiterpene lactones Saponins A.digitata L.+ve -ve C.glaucum Hiern+ve -ve L.cornuta (Hocht.ex.Oliv.)C.Je ffrey +ve -ve+ve Z.chalybeum Engl.+ve -ve CHCl 3 : MeOH extracts AlkaloidsFlavonoidsSesquiterpene lactones Saponins A.digitata L.+ve C.glaucum Hiern.+ve L.cornuta (Hocht.ex.Oliv.)C.Je ffrey +ve Z.chalybeum.Engl.+ve

16 In vivo antimalarial activity (cont.) Securidaca longenpendunculata (roots), Flacourtia indica (leaves), Ocimum gratissimum (leaves) and Hoslundia opposita (roots) had 96.4%; 90.3%; 91.98% and 96.3% parasite growth inhibition respectively

17 STUDY AREA Msambweni district

18 Acknowledgements  The Carnegie Corporation of New York  Nairobi Node-RISE- AFNNET)  The community of Msambweni district  University of Nairobi  KEMRI-CTMDR COLLABORATORS:  KIAMA GITAHI  JAMES MBARIA  DANIEL GAKUYA  PETER GATHUMBI  JOHN DAVID KABASA

19 THANK YOU FOR ACTIVE PARTICIPATION