| Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). | |
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MedLine Citation:
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PMID: 19667291 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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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Authors:
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N Cachet; F Hoakwie; S Bertani; G Bourdy; E Deharo; D Stien; E Houel; H Gornitzka; J Fillaux; S Chevalley; A Valentin; V Jullian |
Publication Detail:
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Type: Journal Article Date: 2009-08-10 |
Journal Detail:
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Title: Antimicrobial agents and chemotherapy Volume: 53 ISSN: 1098-6596 ISO Abbreviation: Antimicrob. Agents Chemother. Publication Date: 2009 Oct |
Date Detail:
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Created Date: 2009-09-22 Completed Date: 2009-12-14 Revised Date: 2010-09-27 |
Medline Journal Info:
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Nlm Unique ID: 0315061 Medline TA: Antimicrob Agents Chemother Country: United States |
Other Details:
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Languages: eng Pagination: 4393-8 Citation Subset: IM |
Affiliation:
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Laboratoire de Pharmacochimie des Substances Naturelles et Pharmacophores Redox, UMR 152, UPS, Université de Toulouse, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antimalarials / chemistry, pharmacology* Cell Line, Tumor Cell Survival / drug effects Cercopithecus aethiops Humans Magnetic Resonance Spectroscopy Malaria / drug therapy, parasitology Molecular Structure Plasmodium falciparum / drug effects* Quassins / chemistry, pharmacology* Simaroubaceae / chemistry* Vero Cells |
| Chemical | |
Reg. No./Substance:
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0/Antimalarials; 0/Quassins |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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