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EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF NOVEL SYNTHESIZED PHENYLPROPANOID ESTERS

Abstract

Cindy LH Yang, Stanley CC Chik, KY Au, Allan Sik-Yin Lau, and Godfrey Chi-Fung Chan*

Inflammation plays an important role in the pathogenesis of various chronic and acute diseases. Our previous study showed that cimiracemate A (PubChem: CID 5315874) (1) possessed potent anti-inflammatory effect by suppressing LPS-induced TNF- production in primary blood macrophage and inhibiting the 5-lipoxygenase enzymatic activity. In light of the biological activities of compound-1, we synthesize 3 analogues of compound-1 and then screen their anti-inflammatory effects. The results showed that (E)-2-oxo-3-phenylpropyl 3-(3-hydroxy-4-methoxyphenyl)acrylate (4) was toxic to primary blood macrophage at concentration of 50 g.mL-1. (E)-3-(3,4-dihydroxyphenyl)-2-oxopropyl 3-(4-methoxyphenyl)acrylate (3) showed the highest suppressive effect on LPS-induced TNF- production in primary blood macrophage when compared with compound-1 and (E)-3-(3-hydroxyphenyl)-2-oxopropyl 3-(3,4-dihydroxyphenyl)acrylate (2). Compounds-1 and -3 showed similar inhibitive effects on LPS-induced mRNA levels of cytokines (TNF-, IL-6, and IL-1) and chemokines (IP-10, CCL-3, and CCL-5). Compound-3 showed greater suppressive effect than compound-1 on LPS-induced nitric oxide production in RAW264.7 and BV-2 cells. The result revealed that compound-3 may have the potential to be further developed as a new class of anti-inflammatory therapeutic agent.

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