Heme activates artemisinin more efficiently than hemin, inorganic iron, or hemoglobin

Artemisinin derivatives appear to mediate their anti-malarial effects through an initial redox-mediated reaction. Heme, inorganic iron, and hemoglobin have all been implicated as the key molecules that activate artemisinins. The reactions of artemisinin with different redox forms of heme, ferrous iron, and deoxygenated and oxygenated hemoglobin were analyzed under similar in vitro conditions. Heme reacted with artemisinin much more efficiently than the other iron-containing molecules, supporting the role of redox active heme as the primary activator of artemisinin. (c) 2008 Elsevier Ltd. All rights reserved.