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Molecules 2010, 15(3), 1378-1397; doi:10.3390/molecules15031378

Biological Actions of Artemisinin: Insights from Medicinal Chemistry Studies

State Key Laboratory of Biomembrane and Membrane Biotechnology, School of Life Sciences, Tsinghua University, Beijing 100084, China
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Received: 13 January 2010 / Revised: 23 February 2010 / Accepted: 2 March 2010 / Published: 8 March 2010
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Abstract

Artemisinins have become essential antimalarial drugs for increasingly widespread drug-resistant malaria strains. Although tremendous efforts have been devoted to decipher how this class of molecules works, their exact antimalarial mechanism is still an enigma. Several hypotheses have been proposed to explain their actions, including alkylation of heme by carbon-centered free radicals, interference with proteins such as the sarcoplasmic/endoplasmic calcium ATPase (SERCA), as well as damaging of normal mitochondrial functions. Besides artemisinins, other endoperoxides with various backbones have also been synthesized, some of which showed comparable or even higher antimalarial effects. It is noteworthy that among these artemisinin derivatives, some enantiomers displayed similar in vitro malaria killing efficacy. In this article, the proposed mechanisms of action of artemisinins are reviewed in light of medicinal chemistry findings characterized by efficacy-structure studies, with the hope of gaining more insight into how these potent drugs work.
Keywords: artemisinin; PfATP6; heme; iron; mitochondria artemisinin; PfATP6; heme; iron; mitochondria
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Li, J.; Zhou, B. Biological Actions of Artemisinin: Insights from Medicinal Chemistry Studies. Molecules 2010, 15, 1378-1397.

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