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.
Keywords: Alpha-methylen-gamma lactone, Lactone group, sesquiterpenes, antineoplastic, tumor, therapeutic agents, disease.
Current Medicinal Chemistry
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,Italy
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.
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Cite this article as:
Sut Stefania, Maggi Filippo , Nicoletti Marcello, Baldan Valeria and Dall`Acqua Stefano*, New Drugs from Old Natural Compounds: Scarcely Investigated Sesquiterpenes as New Possible Therapeutic Agents, Current Medicinal Chemistry 2018; 25 (10) . https://dx.doi.org/10.2174/0929867324666170404150351
DOI https://dx.doi.org/10.2174/0929867324666170404150351 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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