AAC Accepts, published online ahead of print on 16 June 2008
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Antimicrob. Agents Chemother. doi:10.1128/AAC.00165-08
Copyright (c) 2008, American Society for Microbiology and/or the Listed Authors/Institutions. All Rights Reserved.

The antimalarial trioxaquine DU1301 alkylates heme in malaria-infected mice

Fatima Bousejra-El Garah, Catherine Claparols, Françoise Benoit-Vical, Bernard Meunier, and Anne Robert*

Laboratoire de Chimie de Coordination du CNRS, 205 route de Narbonne, 31077 Toulouse cedex 4, France; Service de Parasitologie et Mycologie, CHU Rangueil, Université de Toulouse, TSA 50032, 31059 Toulouse cedex 9, France; Palumed, Rue Pierre et Marie Curie, BP 28262, 31682 Labège cedex, France

* To whom correspondence should be addressed. Email: anne.robert{at}lcc-toulouse.fr.


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Abstract

The in vivo alkylation of heme by the antimalarial trioxaquine DU1301 afforded covalent heme-drug adducts that have been detected in the spleen of malaria-infected mice. This result indicates that the alkylation capacity of trioxaquines in mammals infected by Plasmodium is similar to that of artemisinin, a natural antimalarial trioxane-containing drug.




This article has been cited by other articles:

  • Cosledan, F., Fraisse, L., Pellet, A., Guillou, F., Mordmuller, B., Kremsner, P. G., Moreno, A., Mazier, D., Maffrand, J.-P., Meunier, B. (2008). Selection of a trioxaquine as an antimalarial drug candidate. Proc. Natl. Acad. Sci. USA 105: 17579-17584 [Abstract] [Full Text]  


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