Antimalarial activity of some plants traditionally used in treatment of malaria in Msambweni district of Kenya

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Antimalarial activity of some plants
traditionally used in treatment of malaria in
Msambweni district of Kenya
J.M.Ngutaa, J.M.Mbariaa, D.W.Gakuyab,
P.K.Gathumbic, J.D.Kabasad, S.G.Kiamae
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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)

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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.

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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.

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Ethnopharmacology to modern medicine
Drug/Chemical Action Plant Source
Acetyldigoxin Cardiotonic Digitalis lanata (Grecian foxglove, woolly foxglove)
Adoniside Cardiotonic Adonis vernalis (pheasant's eye, red chamomile)
Aescin Antiinflammatory Aesculus hippocastanum (horse chestnut)
Aesculetin Antidysentery Frazinus rhychophylla
Agrimophol Anthelmintic Agrimonia supatoria
Ajmalicine Treatment for circulatory disorders Rauvolfia sepentina
Allantoin Vulnerary Several plants
Allyl isothiocyanate Rubefacient Brassica nigra (black mustard)
Anabesine Skeletal muscle relaxant Anabasis sphylla
Andrographolide Treatment for baccillary dysentery Andrographis paniculata
Anisodamine Anticholinergic Anisodus tanguticus
Anisodine Anticholinergic Anisodus tanguticus
Arecoline Anthelmintic Areca catechu (betel nut palm)
Asiaticoside Vulnerary Centella asiatica (gotu cola)
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Ethnopharmacology to modern medicine (Cont.)
Drug/Chemical Action Plant Source
Atropine Anticholinergic Atropa belladonna (deadly nightshade)
Benzyl benzoate Scabicide Several plants
Berberine Treatment for bacillary dysentery Berberis vulgaris (common barberry)
Bergenin Antitussive Ardisia japonica (marlberry)
Betulinic acid Anticancerous Betula alba (common birch)
Hyoscyamine Anticholinergic Hyoscyamus niger (black henbane, stinking nightshade, henpin)
Irinotecan Anticancer, antitumor agent Camptotheca acuminata
Kaibic acud Ascaricide Digenea simplex (wireweed)
Kawain Tranquilizer Piper methysticum (kava kava)
Kheltin Bronchodilator Ammi visaga
Lanatosides A, B, C Cardiotonic Digitalis lanata (Grecian foxglove, woolly foxglove)
Lapachol Anticancer, antitumor Tabebuia species (trumpet tree)
a-Lobeline Smoking deterrant, respiratory stimulant Lobelia inflata (Indian tobacco)
Menthol Rubefacient Mentha species (mint)
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Ethnopharmacology to modern medicine (Cont.)
Drug/Chemical Action Plant Source
Monocrotaline Topical antitumor agent Crotalaria sessiliflora
Morphine Analgesic Papaver somniferum (poppy)
Neoandrographolide Treatment of dysentery Andrographis paniculata
Nicotine Insecticide Nicotiana tabacum (tobacco)
Nordihydroguaiaretic acid Antioxidant Larrea divaricata (creosote bush)
Noscapine Antitussive Papaver somniferum (poppy)
Ouabain Cardiotonic Strophanthus gratus (ouabain tree)
Pachycarpine Oxytocic Sophora pschycarpa
Palmatine Antipyretic, detoxicant Coptis japonica (Chinese goldenthread, goldthread, Huang-Lia)
Papain Proteolytic, mucolytic Carica papaya (papaya)
Papavarine Smooth muscle relaxant Papaver somniferum (opium poppy, common poppy)
Phyllodulcin Sweetener Hydrangea macrophylla (bigleaf hydrangea, French hydrangea)
Physostigmine Cholinesterase inhibitor Physostigma venenosum (Calabar bean)
Picrotoxin Analeptic Anamirta cocculus (fish berry)
Pilocarpine Parasympathomimetic Pilocarpus jaborandi (jaborandi, Indian hemp)
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Ethnopharmacology to modern medicine (Cont.)
Drug/Chemical Action Plant Source
Podophyllotoxin Antitumor, anticancer agent Podophyllum peltatum (mayapple)
Protoveratrines A, B Antihypertensives Veratrum album (white false hellebore)
Pseudoephredrine Sympathomimetic Ephedra sinica (ephedra, ma huang)
nor-pseudoephedrine Sympathomimetic Ephedra sinica (ephedra, ma huang)
Quinidine Antiarrhythmic Cinchona ledgeriana (quinine tree)
Quinine Antimalarial, antipyretic Cinchona ledgeriana (quinine tree)
Qulsqualic acid Anthelmintic Quisqualis indica (Rangoon creeper, drunken sailor)
Rescinnamine Antihypertensive, tranquilizer Rauvolfia serpentina
Reserpine Antihypertensive, tranquilizer Rauvolfia serpentina
Rhomitoxin Antihypertensive, tranquilizer Rhododendron molle (rhododendron)
Rorifone Antitussive Rorippa indica
Rotenone Piscicide, Insecticide Lonchocarpus nicou
Rotundine Analagesic, sedative, traquilizer Stephania sinica
Rutin Treatment for capillary fragility Citrus species (e.g., orange, grapefruit)
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Ethnopharmacology to modern medicine (Cont.)
Drug/Chemical Action Plant Source
Sanguinarine Dental plaque inhibitor Sanguinaria canadensis (bloodroot)
Santonin Ascaricide Artemisia maritma (wormwood)
Scillarin A Cardiotonic Urginea maritima (squill)
Scopolamine Sedative Datura species (e.g., Jimsonweed)
Sennosides A, B Laxative Cassia species (cinnamon)
Silymarin Antihepatotoxic Silybum marianum (milk thistle)
Sparteine Oxytocic Cytisus scoparius (scotch broom)
Stevioside Sweetener Stevia rebaudiana (stevia)
Strychnine CNS stimulant Strychnos nux-vomica (poison nut tree)
Taxol Antitumor agent Taxus brevifolia (Pacific yew)
Teniposide Antitumor agent Podophyllum peltatum (mayapple or mandrake)
a-Tetrahydrocannabinol (THC) Antiemetic, decreases occular tension Cannabis sativa (marijuana)
Tetrahydropalmatine Analgesic, sedative, tranquilizer Corydalis ambigua
Tetrandrine Antihypertensive Stephania tetrandra
Theobromine Diuretic, vasodilator Theobroma cacao (cocoa)
Theophylline Diuretic, bronchodilator Theobroma cacao and others (cocoa, tea)
Thymol Topical antifungal Thymus vulgaris (thyme)
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Ethnopharmacology to modern medicine (Cont.)
Drug/Chemical Action Plant source
Trichosanthin Trichosanthin Abortifacient Abortifacient Trichosanthes kirilowii (snake gourd) Trichosanthes kirilowii (snake gourd)
Tubocurarine Tubocurarine Skeletal muscle relaxant Skeletal muscle relaxant Chondodendron tomentosum (curare vine) Chondodendron tomentosum (curare vine)
Valapotriates Valapotriates Sedative Sedative Valeriana officinalis (valerian) Valeriana officinalis (valerian)
Vasicine Vasicine Cerebral stimulant Cerebral stimulant Vinca minor (periwinkle) Vinca minor (periwinkle)
Vinblastine Vinblastine Antitumor, Antileukemic agent Antitumor, Antileukemic agent Catharanthus roseus (Madagascar periwinkle) Catharanthus roseus (Madagascar periwinkle)
Vincristine Vincristine Antitumor, Antileukemic agent Antitumor, Antileukemic agent Catharanthus roseus (Madagascar periwinkle) Catharanthus roseus (Madagascar periwinkle)
Yohimbine Yohimbine Aphrodisiac Aphrodisiac Pausinystalia yohimbe (yohimbe) Pausinystalia yohimbe (yohimbe)
Yuanhuacine Yuanhuacine Abortifacient Abortifacient Daphne genkwa (lilac) Daphne genkwa (lilac)
Yuanhuadine Yuanhuadine Abortifacient Abortifacient Daphne genkwa (lilac) Daphne genkwa (lilac)




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Ctotoxicity of crude plant extracts

• Nguta et al., Pharmacologyonline 2 458-478
  (2011) 4th ICDDT (Dubai, 12-15th/02/12)
• Screened crude extracts 170
• 97.6 of all the screened organic extracts and
  73 of the investigated aqueous extracts
  demonstrated LC50 values lt1000 µg/ml, hence non
  toxic
• Hence could make safe antimalarial formulations

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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????

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Treatments against average chemosuppressions
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Treatments against average parasitaemia
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Phytochemical analysis
Aqueous extracts Alkaloids Flavonoids Sesquiterpene lactones Saponins Saponins
A.digitata L. ve ve -ve -ve -ve
C.glaucum Hiern ve ve -ve -ve -ve
L.cornuta (Hocht.ex.Oliv.)C.Jeffrey ve ve -ve ve ve
Z.chalybeum Engl. ve ve -ve -ve -ve
CHCl3 MeOH extracts Alkaloids Flavonoids Sesquiterpene lactones Saponins  
A.digitata L. ve ve ve ve  
C.glaucum Hiern. ve ve ve ve  
L.cornuta (Hocht.ex.Oliv.)C.Jeffrey ve ve ve ve  
Z.chalybeum .Engl. ve ve ve ve  
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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

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STUDY AREA

• Msambweni district

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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

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THANK YOU FOR ACTIVE PARTICIPATION