Artesunate

Artesunate is a derivative of artemisinin (Item No. 11816) that is active against P. falciparum in vitro (IC50 = 1.28 nM).{21232} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} It inhibits the activity of the P. falciparum EXP1, a glutathione S-transferase (GST) that degrades hematin, with an IC50 value of 2.05 nM.{57853} 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 when administered at a dose of 100 mg/kg twice per day.{42468} It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin (Item No. 13877) in rats.{42469} Artesunate increases the activity of GST in mice infected with P. berghei compared to uninfected and infected control animals.{57854}