Synthesis and biological evaluation of chalcone, dihydrochalcone, and 1,3-diarylpropane analogs as anti-inflammatory agents

Mopur Vijaya Bhaskar Reddy, Hsin Yi Hung, Ping Chung Kuo, Guan Jhong Huang, Yu Yi Chan, Shiow Chyn Huang, Shwu Jen Wu, Susan L. Morris-Natschke, Kuo Hsiung Lee, Tian Shung Wu

Research output: Contribution to journalArticlepeer-review

22 Citations (Scopus)

Abstract

Twenty-one chalcones were prepared via aldol condensation and subsequent reduction of these compound led to the corresponding dihydrochalcone and 1,3-diphenylpropane derivatives. The synthetic products were examined for their effects on NO inhibition in LPS-activated mouse peritoneal macrophages. Among the tested compounds, a 1,3-diarylpropane analog, 2-(3-(3,4-dimethoxyphenyl)propyl)-5-methoxyphenol (3p), displayed the most significant inhibitory effects against NO production. To investigate the mechanism of action, the effects of 3p on iNOS and COX-2 protein expression were studied by immunoblot. The results concluded that 3p is capable of inhibiting iNOS expression in LPS-induced RAW264.7 cells via attenuation of NF-κB signaling by ERK, p38, and JNK.

Original languageEnglish
Pages (from-to)1547-1550
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number7
DOIs
Publication statusPublished - 2017

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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