Anti-cancer potential of sesquiterpene lactones: Bioactivity and molecular mechanisms

Siyuan Zhang, Yen Kim Won, Choon Nam Ong, Han Ming Shen

Research output: Contribution to journalReview articlepeer-review

359 Scopus citations


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 SL-thiols 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 anti-cancer agents with potential applications in both cancer chemotherapy and chemoprevention.

Original languageEnglish (US)
Pages (from-to)239-249
Number of pages11
JournalCurrent Medicinal Chemistry - Anti-Cancer Agents
Issue number3
StatePublished - May 2005
Externally publishedYes


  • Anti-cancer
  • Anti-inflammatory
  • Apoptosis
  • NF-κB
  • Sesquiterpene lactones
  • Thiols

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Cancer Research


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