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Antimicrobial Agents and Chemotherapy, October 2009, p. 4393-4398, Vol. 53, No. 10
0066-4804/09/$08.00+0 doi:10.1128/AAC.00951-09
Copyright © 2009, American Society for Microbiology. All Rights Reserved.
Antimalarial Activity of Simalikalactone E, a New Quassinoid from Quassia amara L. (Simaroubaceae) 
,
N. Cachet,1,2,
F. Hoakwie,1,2,
S. Bertani,3,¶
G. Bourdy,1,2
E. Deharo,1,4
D. Stien,5
E. Houel,5
H. Gornitzka,6
J. Fillaux,7
S. Chevalley,1,2
A. Valentin,1,2,|| and
V. Jullian1,2,||*
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,1 Institut de Recherche pour le Développement, UMR 152, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France,2 USM 0307, Laboratoire de Parasitologie Comparée et Modèles Expérimentaux, Muséum National d'Histoire Naturelle, Paris, France,3 Institut de Recherche pour le Développement, UMR 152, Mission IRD Casilla 18-1209 Lima, Peru,4 CNRS, UMR Ecofog, Université des Antilles et de la Guyane, Cayenne, France,5 CNRS, LCC, UPR 8241, 205 Route de Narbonne, 31077 Toulouse Cedex 4, France,6 Service de Parasitologie-Mycologie, CHU Rangueil, 1 Avenue de Pr. Jean Pouldhès, TSA 50032, 31095 Toulouse Cedex, France7
Received 9 July 2009/ Returned for modification 17 July 2009/ Accepted 29 July 2009
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.
* Corresponding author. Mailing address: Institut de Recherche pour le Développement, UMR 152, Faculté de Pharmacie, Université de Toulouse 3, 35 Chemin des Maraichers, Toulouse 31062, France. Phone: 33 5 62 25 68 23. E-mail: jullian{at}cict.fr
Published ahead of print on 10 August 2009.
Supplemental material for this article may be found at http://aac.asm.org/.
Present address: LCMBA, UMR 6001, CNRS-Université Nice Sophia Antipolis, 06108 Nice Cedex 02, France.
Present address: LSPCMIB, UMR 5068, CNRS-Université Paul Sabatier, 31062 Toulouse Cedex 09, France.
¶ Present address: Department of Biochemistry; University of California, Riverside, CA 92521.
|| These two senior investigators made equal contributions to this study.
Antimicrobial Agents and Chemotherapy, October 2009, p. 4393-4398, Vol. 53, No. 10
0066-4804/09/$08.00+0 doi:10.1128/AAC.00951-09
Copyright © 2009, American Society for Microbiology. All Rights Reserved.
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