The antimalarial trioxaquine DU1301 alkylates heme in malaria-infected mice

Antimicrob Agents Chemother. 2008 Aug;52(8):2966-9. doi: 10.1128/AAC.00165-08. Epub 2008 Jun 16.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Chromatography, Liquid
  • Heme / chemistry
  • Heme / metabolism*
  • Malaria / drug therapy*
  • Malaria / metabolism
  • Mass Spectrometry
  • Mice
  • Molecular Structure
  • Sesquiterpenes / chemistry
  • Sesquiterpenes / pharmacology*

Substances

  • Antimalarials
  • DU1301
  • Sesquiterpenes
  • Heme