TY  - JOUR
AU  - Cachet, N.
AU  - Hoakwie, F.
AU  - Bertani, S.
AU  - Bourdy, G.
AU  - Deharo, E.
AU  - Stien, D.
AU  - Houel, E.
AU  - Gornitzka, H.
AU  - Fillaux, J.
AU  - Chevalley, S.
AU  - Valentin, A.
AU  - Jullian, V.
PY  - 2009//
TI  - Antimalarial Activity of Simalikalactone E, a New Quassinoid from Quassia amara L. (Simaroubaceae)
T2  - Antimicrob. Agents Chemother.
JO  - Antimicrobial Agents and Chemotherapy
SP  - 4393
EP  - 4398
VL  - 53
IS  - 10
PB  - AMER SOC MICROBIOLOGY
N2  - We report the isolation and identification of a new quassinoid named simalikalactone E (SkE), extracted from a widely used Amazonian antimalarial remedy made out of Quassia amara L. (Simaroubaceae) leaves. This new molecule inhibited the growth of Plasmodium falciparum cultured in vitro by 50%, in the concentration range from 24 to 68 nM, independently of the strain sensitivity to chloroquine. We also showed that this compound was able to decrease gametocytemia with a 50% inhibitory concentration sevenfold lower than that of primaquine. SkE was found to be less toxic than simalikalactone D (SkD), another antimalarial quassinoid from Q. amara, and its cytotoxicity on mammalian cells was dependent on the cell line, displaying a good selectivity index when tested on nontumorogenic cells. In vivo, SkE inhibited murine malaria growth of Plasmodium vinckei petteri by 50% at 1 and 0.5 mg/kg of body weight/day, by the oral or intraperitoneal routes, respectively. The contribution of quassinoids as a source of antimalarial molecules needs therefore to be reconsidered.
SN  - 0066-4804
N1  - ISI:000270020600047
ID  - Cachet_etal2009
ER  -