PMID- 15992352 OWN - NLM STAT- MEDLINE DCOM- 20050728 LR - 20240109 IS - 1568-0118 (Print) IS - 1568-0118 (Linking) VI - 5 IP - 3 DP - 2005 May TI - Anti-cancer potential of sesquiterpene lactones: bioactivity and molecular mechanisms. PG - 239-49 AB - 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 alpha-methylene-gamma-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-kappaB) 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. FAU - Zhang, Siyuan AU - Zhang S AD - Department of Community, Occupational and Family Medicine, Faculty of Medicine, National University of Singapore, Republic of Singapore. FAU - Won, Yen-Kim AU - Won YK FAU - Ong, Choon-Nam AU - Ong CN FAU - Shen, Han-Ming AU - Shen HM LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review PL - Netherlands TA - Curr Med Chem Anticancer Agents JT - Current medicinal chemistry. Anti-cancer agents JID - 101123597 RN - 0 (Antineoplastic Agents, Phytogenic) RN - 0 (Lactones) RN - 0 (Sesquiterpenes) SB - IM MH - Animals MH - *Antineoplastic Agents, Phytogenic/chemistry/pharmacology/therapeutic use MH - Humans MH - *Lactones/chemistry/pharmacology/therapeutic use MH - Molecular Structure MH - Neoplasms/*drug therapy MH - *Sesquiterpenes/chemistry/pharmacology/therapeutic use MH - Structure-Activity Relationship RF - 116 EDAT- 2005/07/05 09:00 MHDA- 2005/07/29 09:00 CRDT- 2005/07/05 09:00 PHST- 2005/07/05 09:00 [pubmed] PHST- 2005/07/29 09:00 [medline] PHST- 2005/07/05 09:00 [entrez] AID - 10.2174/1568011053765976 [doi] PST - ppublish SO - Curr Med Chem Anticancer Agents. 2005 May;5(3):239-49. doi: 10.2174/1568011053765976.