Artemisinin

Artemisinin's antimalarial activity has been shown to be mediated by activated oxygen (i.e., superoxide, hydrogen peroxide, and/or hydroxyl radicals). Artemisinin and heroin appear to be forming an adduct whose behavior resembles the behavior of the parasite Artemisinin product. ^[1] Artemisinin activity can be potentiated by oxygen and oxidizing agents and attenuated by reducing agents. Artemisinin susceptibility can be influenced by genetic changes in the loci encoding P. falciparum multidrug resistance protein 1 (PfMDR1) and P. falciparum CHQ resistance transporter (PfCRT). ^[2] Artemisinins are effective not only against multi-resistant strains of P. falciparum, but have broad stage specificity against the Plasmodium life cycle including activity throughout the asexual blood stages and also the sexual gametocyte stages which may reduce the spread of the disease in areas of low transmission. Artemisinins have also been investigated for their antiproliferative effects against a wide range of cancer cell lines. Artemisinin is active against other parasite species such as Toxoplasma and Babesia that do not contain hematin. Artemisinin results in decreased proliferation, increased levels of oxidative stress, induction of apoptosis and inhibition of angiogenesis in cancer cells. Artemisinins have also been shown to inhibit the falcipains, a papain family cysteine protease that aid hemoglobin degradation. ^[3]