The mode of action of antimalarial endoperoxides

Trans R Soc Trop Med Hyg. 1994 Jun;88 Suppl 1:S31-2. doi: 10.1016/0035-9203(94)90468-5.

Abstract

The mechanism of action of artemisinin appears to involve two steps. In the first step, activation, intra-parasitic iron catalyses the cleavage of the endoperoxide bridge and the generation of free radicals. In the second step, alkylation, the artemisinin-derived free radical forms covalent bonds with parasite proteins.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Alkylation
  • Animals
  • Antimalarials / pharmacology*
  • Antiprotozoal Agents / pharmacology*
  • Artemisinins*
  • Biotransformation
  • Free Radicals
  • Heme / metabolism
  • Humans
  • Iron / metabolism
  • Peroxides / metabolism
  • Plasmodium / drug effects
  • Sesquiterpenes / pharmacology*

Substances

  • Antimalarials
  • Antiprotozoal Agents
  • Artemisinins
  • Free Radicals
  • Peroxides
  • Sesquiterpenes
  • Heme
  • artemisinine
  • Iron