The mode of action of antimalarial endoperoxides.
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.
Meshnick
S R
SR
Department of Epidemiology, University of Michigan School of Public Health, Ann Arbor 48109.
D000478:Alkylation; D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D037621:Artemisinins; D001711:Biotransformation; D005609:Free Radicals; D006418:Heme / Q000378:metabolism; D006801:Humans; D007501:Iron / Q000378:metabolism; D010545:Peroxides / Q000378:metabolism; D010961:Plasmodium / Q000187:drug effects; D012717:Sesquiterpenes / Q000494:pharmacology*
D000962:Antimalarials; D000981:Antiprotozoal Agents; D037621:Artemisinins; D005609:Free Radicals; D010545:Peroxides; D012717:Sesquiterpenes; D006418:Heme; C031327:artemisinin; D007501:Iron