Artemisia annua L.: a source of novel antimalarial drugs

Abstract

Artemisia annua L. contains artemisinin, an endoperoxide sesquiterpene lactone, mainly in its leaves and inflorescences. This compound and a series of derivatives have attracted attention because of their potential value as antimalarial drugs. In this review a survey of the currently available literature data is given. It includes phytochemical aspects, such as constituents of A. annua, the artemisinin content during the development of the plant and its biosynthesis, isolation, analysis and stability. Total chemical synthesis of artemisinin is referred to, as well as structure-activity relationships of derivatives and simplified analogues. Pharmacological studies are summarized, including the mechanism of action, interaction of the antimalarial activity with other drugs, possible occurrence of resistance to artemisinin, clinical results, toxicological aspects, metabolism and pharmacokinetics. Finally, plant cell biotechnology is mentioned as a possible means to obtain plants and cell cultures with higher artemisinin contents, allowing an industrial production of pharmaceuticals containing this novel drug.

Treatment of Diarrhoea Using Traditional Medicines: Contemporary Research in South Africa and Zimbabwe

“…Herbal medicines have played an important role in the past in the discovery and isolation of new drugs as has been the case of an antimalarial drug derived from Artemisia annua L. (family Asteraceae), a herbal plant used for generations in traditional Chinese medicine to treat and manage malaria (Woerdenbag et al, 1990). Research by Hostettmann et al (2000) showed that the knowledge on the use of medicinal plants in sub-Saharan Africa is widespread and such indigenous knowledge need to be researched and documented for the benefit of both current and future generations.…”

Isolation and characterization of culturable endophytic actinobacteria associated with Artemisia annua L.

“…(Woerdenbag et al 1990). To date, artemisinin and its derivatives have provided the basis for the most effective treatments for malaria (Korenromp et al 2003).…”

A randomized controlled trial of artemotil (beta-arteether) in Zambian children with cerebral malaria.

“…One promising group of drugs is derived from the plant Artemisia annua L, which is used as an herbal remedy in China for fever and malaria. 1,2 Following the isolation of the active ingredient artemisinin (qinghaosu) in 1972, various compounds have been developed by chemical modification; four of these have now reached the stage of pharmaceutical development for use in humans. 3,4 One of these compounds, a semi-synthetic betaethylether derivative of artemisinin originally known as ␤-arteether, but now renamed artemotil (ARTECEF ), has been developed collaboratively.…”