Artemisinin antimalarials: mechanisms of action and resistance
Meshnick, S.R.
Medecine Tropicale Revue du Corps de Sante Colonial 58(3 Suppl): 13-17
1998
ISSN/ISBN: 0025-682X PMID: 10212891 Document Number: 489365
Artemisinin derivatives are an important new class of antimalarial agents. These compounds contain endoperoxide bridges which are essential for antimalarial activity. Artemisinin is believed to act via a two-step mechanism. Artemisinin is first activated by intraparasitic heme-iron which catalyzes the cleavage of this endoperoxide. A resulting free radical intermediate may then kill the parasite by alkylating and poisoning one or more essential malarial protein(s). No clinically relevant artemisinin-resistant human malaria has yet been reported. However, an artemisinin-resistant strain of murine malaria has been developed and may offer clues to the kinds of resistance that may someday develop in human malarias.