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The Antimalarial Drug Artemisinin Alkylates Heme in Infected Mice

Anne Robert, Françoise Benoit-Vical, Catherine Claparols, Bernard Meunier and Jean-Marie P. Lehn
Proceedings of the National Academy of Sciences of the United States of America
Vol. 102, No. 38 (Sep. 20, 2005), pp. 13676-13680
Stable URL: http://www.jstor.org/stable/3376692
Page Count: 5
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The Antimalarial Drug Artemisinin Alkylates Heme in Infected Mice
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Abstract

Heme alkylation by the antimalarial drug artemisinin is reported in vivo, within infected mice that have been treated at pharmacologically relevant doses. Adducts resulting from the alkylation of heme by the drug were characterized in the spleen of treated mice, and their glucuroconjugated derivatives were present in the urine. Because these heme-artemisinin adducts were not observed in noninfected mice, this report confirms that the alkylating activity of this antimalarial drug is related to the presence of the parasite in infected animals. The identification of heme-artemisinin adducts in mice should be considered as the signature of the alkylation capacity of artemisinin in vivo.

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