Sunday, March 18, 2018

Dihydroartemisinin


Mechanism of action

The proposed mechanism of action of artemisinin involves cleavage of endoperoxide bridges by iron, producing free radicals (hypervalent iron-oxo species, epoxides, aldehydes, and (dicarbonyl compounds) which damage biological macromolecules causing oxidative stress in the cells of the parasite. Malaria is caused by apicomplexans, primarily Plasmodium falciparum, which largely reside in red blood cells and itself contains iron-rich heme-groups (in the form of hemozoin) In 2015 artemisinin was shown to bind to a large number targets suggesting that it acts in a promiscuous manner. Recent mechanism research discovered that artemisinin targets a broad spectrum of proteins in the human cancer cell proteome through heme-activated radical alkylation.




Reference: Tripathi K.D., "Essentials of medical pharmacology", Jaypee brothers medical publishers, Seventh edition, New Delhi, page no. 829, 830.

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