Artemisinins

Artemisinin, also known as Qinghaosu, is the active principle extract of Qinghao (Artemisia annua L.), a plant that has been used for centuries in traditional Chinese medicine. The antimalarial properties of artemisinin were first reported in the Western literature in 1979 (Jiang et al., 1982). Extensive clinical studies have demonstrated that these drugs have a highly potent antimalarial activity, which, combined with a broad stage specificity of action, results in a faster clinical and parasitologic response than any other antimalarial agent in clinical use (Hien and White, 1993). Artemisinin drugs are structurally distinct from all other classes of antimalarials (China Cooperative Research Group, 1982), consisting of a peroxide within a 1,2,4-trioxane configuration. The unique feature of these compounds is the presence of a sesquiterpene lactone ring with an endoperoxide bridge that is essential for their antimalarial activity (Cumming et al., 1997) (see Figure 169.1).