Phytochemical and pharmacological study of roots and leaves of Guiera senegalensis J.F. Gmel (Combretaceae).
The chemical composition of total alkaloids from leaves and roots of Guiera senegalensis was investigated. Three beta-carboline alkaloids were purified: in addition to harman and tetrahydroharman, known in roots and leaves, harmalan (dihydroharman) was isolated for the first time from roots of Guiera senegalensis. Guieranone A, a naphthyl butenone, was also purified from leaves and roots. The in vitro antiplasmodial activity and the cytotoxicity of extracts and pure compounds were evaluated. Each total alkaloid extract and beta-carboline alkaloids presented an interesting antiplasmodial activity associated with a low cytotoxicity. Harmalan was less active than harman and tetrahydroharman. Guieranone A showed a strong antiplasmodial activity associated with a high cytotoxicity toward human monocytes. Its cytotoxicity was performed against two cancer cell lines and normal skin fibroblasts in order to study its anticancer potential: guieranone A presented a strong cytotoxicity against each cell strains. Finally, we evaluated the potent synergistic antimalarial interaction between Guiera senegalensis and two plants commonly associated in traditional remedies: Mitragyna inermis and Pavetta crassipes. Three associations evaluated were additive. A synergistic effect was shown between total alkaloids extracted from leaves of Guiera senegalensis and those of Mitragyna inermis. This result justified the traditional use of the plants in combination to treat malaria.
Fiot
Julien
J
Laboratory of Pharmacognosy, Faculty of Pharmacy, Marseille, France.
Sanon
Souleymane
S
Azas
Nadine
N
Mahiou
Valérie
V
Jansen
Olivia
O
Angenot
Luc
L
Balansard
Guy
G
Ollivier
Evelyne
E
D000470:Alkaloids / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002074:Butanones; D002243:Carbolines / Q000494:pharmacology; D002470:Cell Survival; D029764:Combretaceae; D004357:Drug Synergism; D006246:Harmaline / Q000031:analogs & derivatives / Q000494:pharmacology; D006247:Harmine / Q000031:analogs & derivatives / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D009000:Monocytes / Q000187:drug effects; D009281:Naphthalenes; D000078183:Oxindoles; D021261:Parasitic Sensitivity Tests; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D018515:Plant Leaves; D018517:Plant Roots; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D019666:Rubiaceae
D000470:Alkaloids; D000962:Antimalarials; D002074:Butanones; D002243:Carbolines; D009281:Naphthalenes; D000078183:Oxindoles; D010936:Plant Extracts; C476838:guieranone A; C023426:tetrahydroharmane; C104393:speciophylline; D006247:Harmine; C045323:harmalan; C005010:harman; D006246:Harmaline