The pharmacological activities and mechanisms of artemisinin and its derivatives: a systematic review

Artemisinin and its derivatives have now become essential antimalarial drugs for increasingly widespread drug-resistant malaria strains. Although artemisinin was first used for the treatment of malarial ailments, lots of subsequent studies have demonstrated it possesses other multiple pharmacological functions such as antitumor, antiarrhythmic, anti-fibrosis, as well as the activity against schistosomiasis. A wide array of the molecular mechanisms based on above-mentioned functions of artemisinin and its derivatives have also been explored. Experimental evidences suggest that artemisinin compounds may exert its functions via mechanisms like regulating key factors such as apoptosis-related BAX, FASL and caspase-3, multi-drug resistence genes, cytokines such as CD4+ and CD8+, inflammation-related NF-kappa B and COX2, telomerase, oxidative stress molecules, and so on. In this article, the proposed mechanisms of action of artemisinins are reviewed with the hope of gaining more insight into the multiple actions of these potent drugs and how they work.