Identification of serotonin 5-HT1A receptor partial agonists in ginger

Bioorg Med Chem. 2010 May 1;18(9):3345-51. doi: 10.1016/j.bmc.2010.02.062. Epub 2010 Mar 15.

Abstract

Animal studies suggest that ginger (Zingiber officinale Roscoe) reduces anxiety. In this study, bioactivity-guided fractionation of a ginger extract identified nine compounds that interact with the human serotonin 5-HT(1A) receptor with significant to moderate binding affinities (K(i)=3-20 microM). [(35)S]-GTP gamma S assays indicated that 10-shogaol, 1-dehydro-6-gingerdione, and particularly the whole lipophilic ginger extract (K(i)=11.6 microg/ml) partially activate the 5-HT(1A) receptor (20-60% of maximal activation). In addition, the intestinal absorption of gingerols and shogaols was simulated and their interactions with P-glycoprotein were measured, suggesting a favourable pharmacokinetic profile for the 5-HT(1A) active compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Anxiety Agents / pharmacology*
  • Caco-2 Cells
  • Catechols / pharmacology*
  • Cell Line
  • Fatty Alcohols / pharmacology*
  • Ginger / chemistry*
  • Humans
  • Molecular Structure
  • Serotonin 5-HT1 Receptor Agonists*

Substances

  • Anti-Anxiety Agents
  • Catechols
  • Fatty Alcohols
  • Serotonin 5-HT1 Receptor Agonists
  • shogaol
  • gingerol