In vitro gametocytocidal activity of artemisinin and its derivatives on Plasmodium falciparum.

Artemisinin and six of its derivatives were evaluated for their in vitro gametocytocidal and erythrocytic schizontocidal properties on an Indian isolate of Plasmodium falciparum. One of the metabolic derivatives, DADF-dihydroartemisinin (NIH02), was found to possess gametocytocidal and erythrocytic schizontocidal properties similar to those of artemisinin. Gametocytes of this isolate were highly susceptible to the toxic effect of NIH02 (IC50 = 6.6 ng/ml) and younger stages were more sensitive. This is the first report about the in vitro gametocytocidal properties of a derivative of artemisinin.