Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Modulation of Radioligand Binding to the GABAA-benzodiazepine Receptor Complex by a New Component from Cyperus Rotundus
Jeoung-Hee HaKwang-Youn LeeHyoung-Chul ChoiJungsook ChoByung-Soo KangJae-Chul LimDong-Ung Lee
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2002 Volume 25 Issue 1 Pages 128-130


Four sesquiterpenes, β-selinene, isocurcumenol, nootkatone and aristolone and one triterpene, oleanolic acid were isolated from the ethylacetate fraction of the rhizomes of Cyperus rotundus and tested for their ability to modulate γ-aminobutyric acid (GABAA)-benzodiazepine receptor function by radioligand binding assays using rat cerebrocortical membranes. Among these compounds, only isocurcumenol, one of the newly identified constituents of this plant, was found to inhibit [3H]Ro15-1788 binding and enhance [3H]flunitrazepam binding in the presence of GABA. These results suggest that isocurcumenol may serve as a benzodiazepine receptor agonist and allosterically modulate GABAergic neurotransmission via enhancement of endogenous receptor ligand binding.

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© 2002 The Pharmaceutical Society of Japan
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