Gingerols

A novel class of vanilloid receptor (VR1) agonists

Vadim N. Dedov, Van H. Tran, Colin C. Duke, Mark Connor, MacDonald J. Christie, Sravan Mandadi, Basil D. Roufogalis*

*Corresponding author for this work

Research output: Contribution to journalArticle

143 Citations (Scopus)

Abstract

1. Gingerols, the pungent constituents of ginger, were synthesized and assessed as agonists of the capsaicin-activated VR1 (vanilloid) receptor. 2. [6]-Gingerol and [8]-gingerol evoked capsaicin-like intracellular Ca 2+ transients and ion currents in cultured DRG neurones. These effects of gingerols were blocked by capsazepine, the VR1 receptor antagonist. 3. The potency of gingerols increased with increasing size of the side chain and with the overall hydrophobicity in the series. 4. We conclude that gingerols represent a novel class of naturally occurring VR1 receptor agonists that may contribute to the medicinal properties of ginger, which have been known for centuries. The gingerol structure may be used as a template for the development of drugs acting as moderately potent activators of the VR1 receptor.

Original languageEnglish
Pages (from-to)793-798
Number of pages6
JournalBritish Journal of Pharmacology
Volume137
Issue number6
DOIs
Publication statusPublished - Nov 2002
Externally publishedYes

Keywords

  • DRG neurones
  • Ginger
  • Gingerols
  • Intracellular calcium
  • Plasma membrane currents
  • VR1 receptor

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    Dedov, V. N., Tran, V. H., Duke, C. C., Connor, M., Christie, M. J., Mandadi, S., & Roufogalis, B. D. (2002). Gingerols: A novel class of vanilloid receptor (VR1) agonists. British Journal of Pharmacology, 137(6), 793-798. https://doi.org/10.1038/sj.bjp.0704925