4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 15, Pages 4413-4418

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.05.058

Keywords

Resveratrol dimers; Resveratrol analogues; Anti-inflammation; MAPK

Funding

  1. National Natural Science Foundation of China [30973612]
  2. Shanghai Municipal Committee of Science and Technology [10431903100]
  3. National Basic Research Program of China (973 Program) [2010CB912603]

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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 mu M, IC50 = 3.38 mu M). Further study revealed that compound 12b could suppress LPS-induced iNOS expression, NO production, and IL-1 beta 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. (C) 2013 Elsevier Ltd. All rights reserved.

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