Mechanism of Action of Artemisinins: a Long Unsettled Challenge

Chen SUN, Bing Zhou, Jian Li · Scientia Sinica Vitae · 2012

Artemisinin, discovered by Chinese scientists in the early 1970s, is an effective antimalarial drug with low toxicity. Artemisinins (artemisinin and its derivatives) remain as the gold standard in combating ever increasing drug-resistant malaria. Although intensive efforts have been devoted to explore the mode of action of this class of drugs, its exact mechanism remains an enigma. Many hypotheses have been proposed, such as iron and heme model, mitochondria model, PfATP6 model, and so forth. Recent studies have demonstrated that artemisinin and its analogs also possess potent inhibitory activities on some other parasites, cancer, virus and rheumatism. The aim of this review is to provide a mechanistic overview of the action of artemisinins.

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