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Effects of Ginsenosides on GABAA Receptor Channels Expreaaed in Xenopus Oocytes
Se-EunChoi,SeokChoi,Jun-HoLee,PaulJ.Whiting,Sang-MokLee,Seoung-YeolNah 대한약학회 2003 Archives of Pharmacal Research Vol.26 No.1
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 (a1b1g2S) channel activity expressed in Xenopus oocytes using a two-electrode voltageclamp 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 ( IGABA). Ginsenoside Rc alone induced an inward membrane current in certain batches of oocytes expressing the GABAA receptor. The effect of ginsenoside Rc on IGABA was both dose-dependent and reversible. The half-stimulatory concentration (EC50) of ginsenoside Rc was 53.2 ± 12.3 mM. Both bicuculline, a GABAA receptor antagonist, and picrotoxin, a GABAA channel blocker, blocked the stimulatory effect of ginsenoside Rc on IGABA. Niflumic acid (NFA) and 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS), both Cl- channel blockers, attenuated the effect of ginsenoside Rc on IGABA. 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.