Inhibition of TNF‐α‐mediated endothelial cell–monocyte cell adhesion and adhesion molecules expression by the resveratrol derivative,trans‐3,5,4′‐trimethoxystilbene

Resveratrol (RSV) has been shown to have anti‐inflammatory activity and to have a protective role against atherosclerosis. Here it is shown, for the first time, that its derivative trans‐3,5,4′‐trimethoxystilbene (TMS) may be a more potent anti‐inflammatory agent than resveratrol. A comparative analysis of the inhibitory activities of related stilbenes, resveratrol, TMS and polydatin (PD), on monocyte adhesion to TNF‐α‐activated endothelial cells showed TMS to be the most effective, with PD being the least effective. RSV and its analogues inhibited, albeit differentially, the protein and mRNA expression levels of inducible cell adhesion molecules, ICAM‐1 and VCAM‐1, in cultured endothelial cells. The mechanism of the inhibitory effects of these stilbenes on endothelial cell–monocyte cell adhesion can be attributed mainly to inhibition of NF‐κB pathway activation. The results demonstrate that all three investigated stilbene compounds, especially TMS, exhibit a potent inhibitory effect on inflammation‐induced cell–cell adhesion, expression of adhesion molecules and activation of the NF‐κB pathway. Copyright © 2010 John Wiley & Sons, Ltd.