Identification of serotonin 5-HT1A receptor partial agonists in ginger.
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.
Nievergelt
Andreas
A
Department of Chemistry and Applied Biosciences, ETH 8093 Zurich, Switzerland.
Huonker
Peter
P
Schoop
Roland
R
Altmann
Karl-Heinz
KH
Gertsch
Jürg
J
D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D018938:Caco-2 Cells; D002396:Catechols / Q000494:pharmacology*; D002460:Cell Line; D005233:Fatty Alcohols / Q000494:pharmacology*; D020939:Zingiber officinale / Q000737:chemistry*; D006801:Humans; D015394:Molecular Structure; D058825:Serotonin 5-HT1 Receptor Agonists
D014151:Anti-Anxiety Agents; D002396:Catechols; D005233:Fatty Alcohols; D058825:Serotonin 5-HT1 Receptor Agonists; C040115:shogaol; C007845:gingerol