Modulation of radioligand binding to the GABA(A)-benzodiazepine receptor complex by a new component from Cyperus rotundus.

Jeoung Hee Ha; Kwang Youn Lee; Hyoung Chul Choi; Jungsook Cho; Byung Soo Kang; Jae Chul Lim; Dong Ung Lee

doi:10.1248/bpb.25.128

Modulation of radioligand binding to the GABA(A)-benzodiazepine receptor complex by a new component from Cyperus rotundus.

Jeoung Hee Ha, Kwang Youn Lee, Hyoung Chul Choi, Jungsook Cho, Byung Soo Kang, Jae Chul Lim, Dong Ung Lee

Department of Medicine

Yeungnam University

Research output: Contribution to journal › Article › peer-review

41 Scopus citations

Abstract

Four sesquiterpenes, beta-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 gamma-aminobutyric acid (GABA(A))-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.

Original language	English
Pages (from-to)	128-130
Number of pages	3
Journal	Biological and Pharmaceutical Bulletin
Volume	25
Issue number	1
DOIs	https://doi.org/10.1248/bpb.25.128
State	Published - Jan 2002

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AU - Kang, Byung Soo

AU - Lim, Jae Chul

AU - Lee, Dong Ung

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Modulation of radioligand binding to the GABA(A)-benzodiazepine receptor complex by a new component from Cyperus rotundus.

Abstract

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