【摘 要】
:
The present study was designed to synthesize 2-Cyano-3,12-dioxooleana-1,9(11)-en-28-oate-13β,28-olide (1),a lactone derivative of oleanolic acid (OA) and evaluate its anti-inflammatory activity.Compound 1 significantly diminished nitric oxide (NO) product
【机 构】
:
State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Discovery, for Metabolic D
论文部分内容阅读
The present study was designed to synthesize 2-Cyano-3,12-dioxooleana-1,9(11)-en-28-oate-13β,28-olide (1),a lactone derivative of oleanolic acid (OA) and evaluate its anti-inflammatory activity.Compound 1 significantly diminished nitric oxide (NO) production and down-regulated the mRNA expression of iNOS,COX-2,IL-6,IL-1β,and TNF-α in lipopolysaccharide (LPS)-stimulated RAW264.7 cells.Further in vivo studies in murine model of LPS-induced acute lung injury (ALI) showed that 1 possessed more potent protective effects than the well-known anti-inflammatory drug dexamethasone by inhibiting myeloperoxidase (MPO) activity,reducing total cells and neutrophils,and suppressing inflammatory cytokines expression,and thus ameliorating the histopathological conditions of the injured lung tissue.In conclusion,compound 1 could be developed as a promising anti-inflammatory agent for intervention of LPS-induced ALI.
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