Evidence for a Common Non-Heme Chelatable-Iron-Dependent Activation Mechanism for Semisynthetic and Synthetic Endoperoxide Antimalarial Drugs

摘要

Herbal extracts of Artemisia annua have been used to treat malaria since ancient times.Artemisinin(1),the refined natural product,is extremely potent and displays little or no cross-resistance with other antimalarial compounds.However,it is relatively expensive,has poor bioavailability,and has poor pharmacokinetics,properties that are shared by semisynthetic derivatives such as artesunate(2)and artem-ether(3).