Document Detail


Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae).
MedLine Citation:
PMID:  19667291     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
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:
Type:  Journal Article     Date:  2009-08-10
Journal Detail:
Title:  Antimicrobial agents and chemotherapy     Volume:  53     ISSN:  1098-6596     ISO Abbreviation:  Antimicrob. Agents Chemother.     Publication Date:  2009 Oct 
Date Detail:
Created Date:  2009-09-22     Completed Date:  2009-12-14     Revised Date:  2013-06-02    
Medline Journal Info:
Nlm Unique ID:  0315061     Medline TA:  Antimicrob Agents Chemother     Country:  United States    
Other Details:
Languages:  eng     Pagination:  4393-8     Citation Subset:  IM    
Affiliation:
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.
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MeSH Terms
Descriptor/Qualifier:
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:
0/Antimalarials; 0/Quassins
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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