This review provides a recent perspective of artesunate and other artemisinins as antimalarial drugs and their uses in cancer therapy. Artesunate is an artemisinin derivative. Artemisinin is extracted from the plant Artemisia annua. Artemisinin and its derivatives have been the most useful drug for malarial treatment in human history. The artesunate has an advantage of a hydrophilic group over other artemisinins which makes it a more potent drug. On the industrial scale, artemisinins are synthesized in semisynthetic ways. The 1,2,4-endoperoxide bridge of artemisinins is responsible for the drug's antimalarial activity. There is the emergence of artemisinin resistance on Plasmodium falciparum and pieces of evidence suggest that it is mainly due to the mutation at Kelch13 protein of P. falciparum. Clinical trial data show that the artesunate is more favorable than quinine and other artemisinins to treat patients with severe malaria. Pieces of evidence indicate that artemisinins can be developed as anticancer drugs. The mechanism of actions on how artemisinins act as an anticancer drug involves oxidative stress, DNA damage and repair, and various types of cell deaths.

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