The antimalarial trioxaquine DU1301 alkylates heme in malaria-infected mice.
The in vivo alkylation of heme by the antimalarial trioxaquine DU1301 afforded covalent heme-drug adducts that were detected in the spleens of Plasmodium sp.-infected mice. This result indicates that the alkylation capacities of trioxaquines in mammals infected with Plasmodium strains are similar to that of artemisinin, a natural antimalarial trioxane-containing drug.
Laboratoire de Chimie de Coordination du CNRS, 205 route de Narbonne, 31077 Toulouse Cedex 4, France.
Fatima
F
Bousejra-El Garah
Catherine
C
Claparols
Françoise
F
Benoit-Vical
Bernard
B
Meunier
Anne
A
Robert
D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D002853:Chromatography, Liquid; D006418:Heme / Q000737:chemistry / Q000378:metabolism*; D008288:Malaria / Q000188:drug therapy* / Q000378:metabolism; D013058:Mass Spectrometry; D051379:Mice; D015394:Molecular Structure; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; C503606:DU1301; D012717:Sesquiterpenes; D006418:Heme