Artesunate-d4 is intended for use as an internal standard for the quantification of artesunate by GC- or LC-MS. Artesunate is a derivative of artemisinin that is active against P. falciparum in vitro (IC50 = 1.28 nM).1 It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.2 Artesunate inhibits proliferation of germinal center B cells in vitro and prevents development of arthritis via inhibition of germinal center formation and autoantibody production in the K/BxN mouse model of rheumatoid arthritis.3 It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin in rats.4
|1. Akoachere, M., Buchholz, K., Fischer, E., et al. In vitro assessment of methylene blue on chloroquine-sensitive and -resistant Plasmodium falciparum strains reveals synergistic action with artemisinins. Antimicrob. Agents Chemother. 49(11), 4592-4597 (2005).|2. Ooko, E., Saeed, M.E.M., Kadioglu, O., et al. Artemisinin derivatives induce iron-dependent cell death (ferroptosis) in tumor cells. Phytomedicine 22(11), 1045-1054 (2015).|3. Hou, L., Block, K.E., and Huang, H. Artesunate abolishes germinal center B cells and inhibits autoimmune arthritis. PloS One 9(8), e104762 (2014).|4. Wang, Y., Huang, G., Mo, B., et al. Artesunate modulates expression of matrix metalloproteinases and their inhibitors as well as collagen-IV to attenuate pulmonary fibrosis in rats. Genet. Mol. Res. 15(2), (2016).