Bioorganic & Medicinal Chemistry 2010-05-01

Identification of serotonin 5-HT1A receptor partial agonists in ginger.

Andreas Nievergelt, Peter Huonker, Roland Schoop, Karl-Heinz Altmann, Jürg Gertsch

Index: Bioorg. Med. Chem. 18 , 3345-51, (2010)

Full Text: HTML

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.(c) 2010 Elsevier Ltd. All rights reserved.