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- Title
Effects of ginsenosides on GABA<sub>A</sub> receptor channels expressed in xenopus oocytes.
- Authors
Choi, Se-Eun; Choi, Seok; Lee, Jun-Ho; Whiting, Paul; Lee, Sang-Mok; Nah, Seung-Yeol
- Abstract
Ginsenosides, major active ingredients of Panax ginseng, are known to regulate excitatory ligand-gated ion channel activity such as nicotinic acetylcholine and NMDA receptor channel activity. However, it is not known whether ginsenosides affect inhibitory ligand-gated ion channel activity. We investigated the effect of ginsenosides on human recombinant GABAA receptor (α1β1γ2S) channel activity expressed in Xenopus oocytes using a two-electrode voltage-clamp technique. Among the eight individual ginsenosides examined, namely, Rb1, Rb2, Rc, Rd, Re, Rf, Rg1 and Rg2, we found that Rc most potently enhanced the GABA-induced inward peak current ( l GABA). Ginsenoside Rc alone induced an inward membrane current in certain batches of oocytes expressing the GABAA receptor. The effect of ginsenoside Rc on I GABA was both dose-dependent and reversible. The half-stimulatory concentration (EC50) of ginsenoside Rc was 53.2 ± 12.3 μM. Both bicuculline, a GABAA receptor antagonist, and picrotoxin, a GABAA channel blocker, blocked the stimulatory effect of ginsenoside Rc on I GABA. Niflumic acid (NFA) and 4,4′-diisothiocyanostilbene-2,2′-disulfonic acid (DIDS), both Cl− channel blockers, attenuated the effect of ginsenoside Rc on I GABA. This study suggests that ginsenosides regulated GABAA receptor expressed in Xenopus oocytes and implies that this regulation might be one of the pharmacological actions of Panax ginseng.
- Publication
Archives of Pharmacal Research, 2003, Vol 26, Issue 1, p28
- ISSN
0253-6269
- Publication type
Article
- DOI
10.1007/BF03179927