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