Anti-Cancer Potential of Sesquiterpene Lactones: Bioactivity and Molecular Mechanisms

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Anti-Cancer Potential of Sesquiterpene Lactones: Bioactivity and Molecular Mechanisms

Anti-Cancer Agents in Medicinal Chemistry, 5(3): 239-249.

Author(s): Siyuan Zhang, Yen-Kim Won, Choon-Nam Ong and Han-Ming Shen.

Affiliation: Department of Community,Occupational and Family Medicine, Faculty of Medicine (MD3), NationalUniversity of Singapore, 16 Medical Drive, Singapore 117597, Republic of Singapore.


Sesquiterpene lactones (SLs) are the active constituents of a variety of medicinal plants used in traditional medicine for the treatment of inflammatory diseases. In recent years, the anti-cancer property of various SLs has attracted a great deal of interest and extensive research work has been carried out to characterize the anti-cancer activity, the molecular mechanisms, and the potential chemopreventive and chemotherapeutic application of SLs. In this review, we attempt to summarize the current knowledge of the anti-cancer properties of SLs by focusing on the following important issues. First, we discuss the structure-activity relationship of SLs. All SLs contain a common functional structure, an α- methylene-γ-lactone group, and this important chemical characteristic means that the thiol-reactivity of SLs is an underlying mechanism responsible for their bioactivities. Second, we assess the experimental evidence for the anti-cancer function of SLs obtained from both in vitro cell culture and in vivo animal models. Various SLs have been demonstrated to execute their anti-cancer capability via inhibition of inflammatory responses, prevention of metastasis and induction of apoptosis. Thirdly, we outline the molecular mechanisms involved in the anti-cancer activity of SLs, in particular, the SLthiols reaction, the effect of SLs on cell signaling pathways such as nuclear transcription factor-kappaB (NF-κB) and mitogen-activated protein kinases (MAPK). Finally, we recapitulate some important SLs with regards to their anti-cancer activities and their potential in anti-cancer drug development. Taken together, many SLs are emerging as promising anticancer agents with potential applications in both cancer chemotherapy and chemoprevention.


sesquiterpene lactones, anti-cancer, apoptosis, thiols, anti-inflammatory, bf-kb.

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Article Details

Volume: 5
Issue Number: 3
First Page: 239
Last Page: 249
Page Count: 11
DOI: 10.2174/1568011053765976
Price: $58
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