THE INTERACTION OF ARTEMISININ WITH MALARIAL HEMOZOIN

[C-14]Artemisinin was taken up by Plasmodium falciparum in culture and concentrated in hemozoin. In vitro, hemin and artemisinin were found to undergo a chemical reaction forming two major products which were i solated by highperformance liquid chromatography (HPLC). The m/z value s of the two products were 856 and 871. Thin-layer chromatography (TLC ) and HPLC of hemozoin isolated from [C-14]artemisinin-treated parasit es showed that the majority of the hemozoin-associated radioactivity c omigrated with the synthetic adducts. When [C-14]artemisinin was incub ated with isolated hemozoin, [C-14]artemisinin disappeared from the so lution in a time-dependent manner. Some of the radioactivity present i n the treated hemozoin also comigrated with the adducts on TLC. Thus, artemisinin appears to react covalently with heme in malaria hemozoin both in vitro and in situ.