Anti-inflammatory activity of 4-methoxycinnamyl p-coumarate isolated from Etlingera pavieana rhizomes in lipopolysaccharide-induced macrophages

Sakulrat Mankhong, Dr. Ekaruth Srisook, Dr.Klaokwan Srisook


Nitric oxide (NO) and prostaglandins E2 (PGE2)play a critical role as inflammatory mediators but overproductioncan lead to inflammatory diseases. Regulation of NO and PGE2 secretion is a particular target in the development of anti-inflammatory agents. 4-methoxycinnamyl p-coumarate (MCC) was isolated from rhizomes of Etlingera pavieana by NO inhibitory activity-guided isolation. In this study, we evaluated the inhibitory effect of MCC on NO and PGE2 production as well as enzymatic activities of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. MTT assay showed that MCC at 6.25 to 25 µM has no significant cytotoxicity compared to unstimulated control cells. MCC significantly reduced NO and PGE2 production with IC50 values of 8.5±0.4 and 26.2±3.7 µM, respectively. MCC at concentrations to 25 µM significantly inhibited iNOS enzyme activity but it did not suppress COX-2 enzyme activity. Interestingly, MCC itself did not reduce COX-1 expression and reversed the suppressive effect on COX-1 expression in LPS-stimulated RAW 264.7 macrophages. Collectively, these results suggest that MCC inhibits NO and PGE2 production, as well as iNOS enzyme activity. MCC exhibits potent anti-inflammatory action with selective inhibitory effect on COX expression and might be used in the development of an anti-inflammatory agent with fewer side effects than current drugs.

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