Antimalarial activity of cedronin
1994
Moretti, Gian Carlo | Deharo, E. | Sauvain, M. | Jardel, C. | David, P.T. | Gasquet, M.
Cedronin was isolated from Simaba cedron Planchon (Simaroubaceae), a species popularly believed in South America to have antimalarial properties. It was examined for in vitro and in vivo antimalarial activities and for cytotoxicity against KB cells. Experimental results showed that cedronin was active against chloroquine-sensitive and resistant strain, with an IC(50) of 0.25 micrograms/ml (0.65 micromoles/ml). It was also found to be active in vivo against Plasmodium vinkei with an IC(50) of 1.8 mg/kg (4.7 nM/kg) in the classic 4-day test. Cedronin belongs to the small group of quassinoids with a C(19) basic skeleton and shows a rather low cytotoxicity against KB cells [IC(50) = 4 micrograms/ml, 10.4 micromolar] as compared with C(20) biologically active quassinoids; however its toxic/therapeutic ratio (10/1.8) remains lower than chloroquine (10/0.5).
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