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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

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.

	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.