Modulation of Radioligand Binding to the GABAA-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

Notes

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

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Keywords: Cyperus rotundus, isocurcumenol, neuromodulation, γ-aminobutyric acid (GABA_A)-benzodiazepine receptor, radioligand binding

JOURNAL FREE ACCESS

2002 Volume 25 Issue 1 Pages 128-130

DOI https://doi.org/10.1248/bpb.25.128

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Abstract

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 (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.

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