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Dihydroartemisinin is a semi-synthetic derivative and active metabolite of artemisinin, a sesquiterpene lactone isolated from *Artemisia annua*. It is the most potent antimalarial metabolite of the artemisinin derivatives, and it acts rapidly against the erythrocytic stage of *Plasmodium* parasites. Its mechanism of action involves generation of free radicals upon cleavage of its endoperoxide bridge by intra-parasitic iron, leading to multiple damaging reactions within the parasite. Dihydroartemisinin also exhibits potential anti-inflammatory and investigational anti-cancer effects. It is poorly water soluble and mostly used in combination therapies for malaria due to rapid clearance and risk of resistance when used alone.
Dihydroartemisinin and artemisinin derivatives undergo activation by iron (heme), generating reactive radicals that cause oxidative stress and damage vital parasite macromolecules, leading to death of malaria parasites.
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