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Sesquiterpene Lactones as a Potent Class of NF-κB Activation Inhibitors

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Sesquiterpene lactones (SLs) are biologically active compounds found in various medicinal plants. Although the compounds are reported to possess numerous biological activities, but the most important is their immunoregulatory role in inflammatory cells. This is because 1) over-activation of inflammatory cells secretes a large amount of different pro-inflammatory mediators such as cytokines, nitric oxide (NO) and prostaglandin (PG)E2 and 2) SLs can modulate these phenomena effectively through inhibiting the activation pathway of nuclear factor (NF)-κB via the reactivity of some functional groups in SLs such as α-methylene-γ- lactone. This review, therefore, discusses in detail the molecular mechanism and structural features of SLs in blocking NF-κB activation with a general introduction of NF-κB and proposes the possibility that SLs can be developed pharmaceutically useful drugs against NF-κB-mediated diseases and that they can be chemically modified to improve their anti-NF-κB efficacy.

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Keywords: I-κB; NF-κB; Sesquiterpene lactones; cytokines; inflammatory mediators; structure-activity relationship study

Document Type: Research Article

Affiliations: School of Biotechnology and Bioengineering, Kangwon National University, 192-1 Hyja-2-dong,Chuncheon, Kangwon-do 200-701, Korea.

Publication date: November 1, 2006

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  • Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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