文章基本信息

标题：Modulation of Radioligand Binding to the GABAA-benzodiazepine Receptor Complex by a New Component from Cyperus Rotundus
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作者：Jeoung-Hee Ha ; Kwang-Youn Lee ; Hyoung-Chul Choi 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2002
卷号：25
期号：1
页码：128-130
DOI：10.1248/bpb.25.128
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：Cyperus rotundus;isocurcumenol;neuromodulation;γ-aminobutyric acid (GABAA)-benzodiazepine receptor;radioligand binding