%0 Journal Article
%T Antimalarial Activity of Simalikalactone E, a New Quassinoid from Quassia amara L. (Simaroubaceae)
%A Cachet, N.
%A Hoakwie, F.
%A Bertani, S.
%A Bourdy, G.
%A Deharo, E.
%A Stien, D.
%A Houel, E.
%A Gornitzka, H.
%A Fillaux, J.
%A Chevalley, S.
%A Valentin, A.
%A Jullian, V.
%J Antimicrobial Agents and Chemotherapy
%D 2009
%V 53
%N 10
%I AMER SOC MICROBIOLOGY
%@ 0066-4804
%F Cachet_etal2009
%O ISI:000270020600047
%O exported from refbase (http://php.ecofog.gf/refbase/show.php?record=103), last updated on Wed, 04 May 2011 10:47:45 -0300
%X 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.
%P 4393-4398