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

Biological Actions of Artemisinin: Insights from Medicinal Chemistry Studies

 and *
Received: 13 January 2010; in revised form: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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

AMA Style

Li J, Zhou B. Biological Actions of Artemisinin: Insights from Medicinal Chemistry Studies. Molecules. 2010; 15(3):1378-1397.

Chicago/Turabian Style

Li, Jian; Zhou, Bing. 2010. "Biological Actions of Artemisinin: Insights from Medicinal Chemistry Studies." Molecules 15, no. 3: 1378-1397.


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