Chapter 4 - Recent patents on sesquiterpene lactones with therapeutic application

Abstract

Sesquiterpene lactones are secondary metabolites mainly found in the Asteraceae family. The chemical structure of these compounds is based on a 15-carbon skeleton containing an α,β-unsaturated-γ-lactone moiety. Occasionally, a saturated γ-lactone or a closely related functionality can be found in place of a classical α,β-unsaturated-γ-lactone moiety. According to their carbocyclic skeletons, they are classified into four major groups: germacranolides, eudesmanolides, guaianolides, and pseudoguaianolides. This type of compounds has a wide range of biological activities, such as antiinflammatory, antiparasitic, antiviral, and cytotoxic, among others. The biological activity of sesquiterpene lactones can largely be attributed to the presence of α-methylene-γ-lactone group in its chemical structure. Chemical transformations of sesquiterpene lactones have been a strategy for improving the activity as well as the bioavailability of this type of compounds. In this chapter, a summary of the patents on sesquiterpene lactones with therapeutic application published over the past 10 years (2009–2019) is presented. Both natural and semisynthetic derivatives are considered, focusing on sesquiterpene lactones as candidates for the development of new drugs for the treatment of different disorders.