Overview

MARTINO V; SÜLSEN V

Sesquiterpene lactones.Advances in their chemistry and biological aspects

Springer

Año: 2018; p. 3 - 17

Sesquiterpene lactones (STLs) are a group of naturally occurringcompounds, most of them found in the Asteraceae family but also present inApiaceae, Magnoliaceae, and Lauraceae. To date about 8000 compounds havebeen reported. They consist of a C15 backbone with numerous modificationsresulting in a variety of structures but with the common feature of a γ-lactonering. They are classified in four major groups: germacranolides, eudesmanolides,guaianolides, and pseudoguaianolides, though there are other subtypes. Therehas been an increasing interest in sesquiterpene lactones due to the wide rangeof biological activities they present. Among the activities found, antimicrobial,antitumor, anti-inflammatory, antioxidant, antiulcerogenic, molluscicidal,antihelminthic, hepatoprotective and hepatotherapeutic, antiprotozoal,antidepressant, and bitter properties have been described. Besides, theyplay an important role in the interaction of plants with insects acting asattractants, deterrents, and antifeedants. These compounds were consideredat first highly cytotoxic, but chemical transformations have enhanced theirbiological activities and diminished their cytotoxicity, so considerableattention has been drawn again on them as lead molecules. Artemisininderivatives, artesunate, and artemether are drugs currently being employed,and dimethylaminoparthenolide, a parthenolide synthetic analogue, andmipsagargin, a prodrug from thapsigargin, are under clinical trials.A summary with the most important findings about the known sesquiterpenelactones, artemisinin, parthenolide, cynaropicrin, dehydroleucodine,mexicanin, helenalin, costunolide, santonin, arglabin, and thapsigargin, willbe given.Studies about the adverse health effects, toxicity, and ecological roles of somesesquiterpene lactones are also mentioned.