TRPA1 channels as targets for resveratrol and related stilbenoids

Bioorg Med Chem Lett. 2016 Feb 1;26(3):899-902. doi: 10.1016/j.bmcl.2015.12.065. Epub 2015 Dec 19.

Abstract

A series of twenty resveratrol analogues was synthesized and tested on TRPA1 and TRPV1 channels. None was able to significantly modulate TRPV1 channels. Conversely, most of them exhibited remarkably higher TRPA1 modulating activity than resveratrol. Optimal potency was observed with ortho monoxygenated stilbenes 6 and 17.

Keywords: Resveratrol; Stilbenoids; TRP channels; TRPA1; TRPV1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium / metabolism
  • HEK293 Cells
  • Humans
  • Inhibitory Concentration 50
  • Ion Transport / drug effects
  • Protein Binding
  • Rats
  • Resveratrol
  • Stilbenes / chemistry*
  • Stilbenes / metabolism
  • Stilbenes / pharmacology
  • TRPA1 Cation Channel
  • TRPC Cation Channels / chemistry
  • TRPC Cation Channels / genetics
  • TRPC Cation Channels / metabolism*

Substances

  • Stilbenes
  • TRPA1 Cation Channel
  • TRPC Cation Channels
  • Trpa1 protein, rat
  • Resveratrol
  • Calcium