Biological Activities of Artemisinins Beyond Anti-Malarial: a Review

Artemisinins, as a class of bioactive molecules, are mainly derived from the extracts of Artemisia annua L. and are the mainstay for malaria treatment, including severe malaria, uncomplicated malaria and multi-drug resistant malaria. They are well-known for their good tolerability, safety and rapid onset of action. Their efficacy is not only limited to malaria but also extends to a variety of human diseases such as cancer, tuberculosis, viral diseases (e.g. Human cytomegalovirus), immune diseases and parasitic infections like schistosomiasis. Being a cheap and safe drug class, which saves millions of lives at risk from malaria around the globe, can also have significant potential in oncology as they have shown anti-cancer properties in both cell lines and animal models. Active derivatives (e.g. artesunate, artemether and arteether etc.) have also been synthesized which can be used for oral, rectal, intramuscular and intravenous administration. A comprehensive update on the non-malarial use of artemisinins and/or their derivatives and artemisinin-based drug development beyond anti-malarial is discussed in this review. With the collaborative efforts in the clinical pharmacology of artemisinins and novel synthesis of artemisinin analogues, it is likely that artemisinin-based drugs will become an important armamentarium impeding a number of diseases beyond malaria.