EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF NOVEL SYNTHESIZED PHENYLPROPANOID ESTERS

  • Cindy LH Yang Molecular Chinese Medicine Laboratory, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong Special Administrative Region, China
  • Stanley CC Chik Molecular Chinese Medicine Laboratory, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong Special Administrative Region, China
  • KY Au Molecular Chinese Medicine Laboratory, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong Special Administrative Region, China
  • Allan Sik-Yin Lau Department of Paediatrics and Adolescent Medicine, The University of Hong Kong, Hong Kong Special Administrative Region, China
  • Godfrey Chi-Fung Chan Department of Paediatrics and Adolescent Medicine, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong Special Administrative Region, China

Abstract

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.

Published
Mar 20, 2018
How to Cite
LH YANG, Cindy et al. EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF NOVEL SYNTHESIZED PHENYLPROPANOID ESTERS. International Journal of Drug Research and Technology, [S.l.], v. 8, n. 1, mar. 2018. ISSN 2277-1506. Available at: <http://ijdrt.com/index.php/drug-research-and-technology/article/view/evaluation-of-anti-inflammatory-activity-of-novel-synthesized-phenylpropanoid-esters>. Date accessed: 22 sep. 2018.
Section
Research Article