Artesunate (88495-63-0) is a semisynthetic derivative of the natural product artemisinin which is clinically useful for treatment of malaria and other parasitic diseases. Depolarizes mitochondrial membrane via generation of reactive oxygen species which disrupt the electron transport chain.1 Generation of mitochondrial ROS is dependent on RIP1.2 Inhibits TNFα-induced production of proinflammatory cytokines in human RA fibroblast-like synoviocytes.3 Displays cytotoxicity against a variety of cancer cells4 and cancer stem cells5.
1) Li et al. (2005), Yeast model uncovers dual roles of mitochondria in action of artemisinin; PLoS Genet., 1(3) e36
2) Chauhan et al. (2017), RIP1-dependent reactive oxygen species production executes artesunate-induced cell death in renal carcinoma Caki cells; Mol. Cell. Biochem., 435 15
3) Xu et al. (2007), Anti-malarial agent artesunate inhibits TNF-alpha-induced production of proinflammatory cytokines via inhibition of NF-kappaB and PI3 kinase/AKt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes; Rheumatology (Oxford), 46 920
4) Ghantous et al. (2010), What made sesquiterpene lactones reach cancer clinical trials?; Drug. Disc. Today, 15 668
5) Subedi et al. (2016), High-throughput screening identifies artesunate as selective inhibitor of cancer stemness: Involvement of mitochondrial metabolism; Biochem. Biophys. Res. Commun., 477 737