Chapter 2 Chemistry, biosynthesis and biological activity of artemisinin and related natural peroxides

Artemisinin is a heterocyclic natural product and belongs to the natural product class of sesquiterpenoids with an unusual 1,2,4 trioxane substructure. Artemisinin is one of the most potent antimalarial drugs available. It serves as a lead compound in the drug development process to identify new chemical derivatives with optimized antimalarial activity and improved bioavailability. In this review we report about the latest status of research on chemical and physical properties of the drug and its derivatives. We describe new strategies to produce artemisinin on a biotechnological level in heterologous hosts and in plant cell cultures. We also summarize recent reports on its pharmacokinetic profile. Furthermore we describe attempts to develop drug delivery systems to overcome bioavailability problems and to target the drug to Plasmodium infected erythrocytes as main target cells