A novel purification method of artemisinin from Artemisia annua

Abstract

Treatment of uncomplicated malaria relies heavily on the sesquiterpene lactone artemisinin (ART), derived from the Chinese herb Artemisia annua. It is currently used as the first line treatment in the form of ART combination therapies in which different ART derivatives are combined with a non ART-like drug, which displays a different mechanism of action. This treatment regime is prescribed by the WHO in order to (1) effectively treat uncomplicated malaria and (2) to reduce the risk that drug resistance will develop. Considering the importance of ART in this treatment regime, various methods have been developed to increase the global production of ART. These methods include: large scale solvent extraction and purification from high yielding A. annua varieties, chemical/semi-chemical synthesis of artemisinin, and genetic engineering of unrelated organisms to produce ART in high quantities. Currently most of the commercial approaches to produce ART are based on solvent extraction and purification from the plant material. Classical extraction solvents include hexane or petroleum ether while ethanol, which is a more polar solvent, has recently been shown to be equally efficient. We developed a purification method from an ethanolic extract by using a diatomite-based purification protocol. Various volumes and ratios of solvents and diatomite were tested which resulted in ≥98% pure ART with a total recovery of around 60%. Our protocol for the isolation of ART may form a commercial scale alternative as it is both economically attractive due to the small amounts of purification materials needed and also environmentally friendlier than the methods previously described.