Inhibitory effect of resveratrol dimerized derivatives on nitric oxide production in lipopolysaccharide-induced RAW 264.7 cells

  • Bioorg Med Chem Lett. 2013 Aug 1;23(15):4413-8. doi: 10.1016/j.bmcl.2013.05.058.
Chen Zhong  1 ,  Xin-Hua Liu ,  Jun Chang ,  Jian-Ming Yu ,  Xun Sun
Affiliations
  • 1. Department of Natural Products Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
PMID: 23791078 DOI: 10.1016/j.bmcl.2013.05.058
Abstract

Four types of resveratrol dimerized analogues were synthesized and evaluated in vitro on LPS-induced NO production in RAW 264.7 cells. The results showed that several compounds, especially those containing 1,2-diphenyl-2,3-dihydro-1H-indene core (type I), exhibited good inhibitory activities. Among 25 analogues, 12b showed a significant inhibitory activity (49% NO production at 10 μM, IC50=3.38 μM). Further study revealed that compound 12b could suppress LPS-induced iNOS expression, NO production, and IL-1β release in a concentration-dependently manner. The mechanism of action (MOA) involved for its anti-inflammatory responses was through signaling pathways of p38 MAPK and JNK1/2, but not ERK1/2.