Title:New Drugs from Old Natural Compounds: Scarcely Investigated Sesquiterpenes as New Possible Therapeutic Agents
VOLUME: 25 ISSUE: 10
Author(s):Stefania Sut, Filippo Maggi, Marcello Nicoletti, Valeria Baldan and Stefano Dall`Acqua*
Affiliation:Department of Pharmaceutical and Pharmacological Sciences University of Padova, Padova, School of Pharmacy, University of Camerino, Camerino, Department of Biology, La Sapienza University, Roma, Department of Pharmaceutical and Pharmacological Sciences University of Padova, Padova, Department of Pharmaceutical and Pharmacological Sciences University of Padova, Padova
Keywords:Alpha-methylen-gamma lactone, Lactone group, sesquiterpenes, antineoplastic, tumor, therapeutic
agents, disease.
Abstract:Sesquiterpenes are natural products that have been extensively studied for their
bioactivities, evidencing their potentiality as useful scaffolds for the development of
drugs. Considering the different derivatives, the sesquiterpene lactones have been evaluated,
especially on cancer cell and antineoplastic efficacy in in vivo studies. Their bioactivity
is strictly related to the presence of the reactive α-methylene-γ-lactone group
(αMγL). Nevertheless, several other sesquiterpenes lacking αMγL are known and have
been studied for their biological effects and potential usefulness in the development of
new drugs. In this review, we focused on several sesquiterpenes that are not presenting
the αMγL moiety and may have future potential as scaffold for the development of new
drugs, namely the bicyclic compounds belonging to the carotane type (daucanes) that present
significant effects as antiproliferative and estrogenic agents. The monocyclic humulane
derivatives correlated to zerumbone, and the bicyclic compound beta-caryophyllene
and its derivatives that have been considered in the field of cancer and inflammation. It is
noteworthy that published studies on sesquiterpenes, reported in this review, focus on pathologies
of increasing importance, like estrogen, anti-proliferative, bone loss, immunity
deficiency and anti-tumour activities. Some of the natural “old” sesquiterpenes can be
considered for their possible role in drug discovery and in counteracting these “new”
challenges.
