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Author  |
Cachet, N.; Hoakwie, F.; Bertani, S.; Bourdy, G.; Deharo, E.; Stien, D.; Houel, E.; Gornitzka, H.; Fillaux, J.; Chevalley, S.; Valentin, A.; Jullian, V. |
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Title |
Antimalarial Activity of Simalikalactone E, a New Quassinoid from Quassia amara L. (Simaroubaceae) |
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Journal Article |
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Year |
2009 |
Publication |
Antimicrobial Agents and Chemotherapy |
Abbreviated Journal |
Antimicrob. Agents Chemother. |
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53 |
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10 |
Pages |
4393-4398 |
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Abstract |
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. |
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Address |
[Cachet, N.; Hoakwie, F.; Bourdy, G.; Deharo, E.; Chevalley, S.; Valentin, A.; Jullian, V.] Univ Toulouse, UPS, Lab Pharmacochim Subst Nat & Pharmacophores Redox, UMR 152, F-31062 Toulouse 9, France, Email: jullian@cict.fr |
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AMER SOC MICROBIOLOGY |
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0066-4804 |
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ISI:000270020600047 |
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EcoFoG @ eric.marcon @ |
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103 |
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