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KMID : 0352720120360010055
Journal of Ginseng Research
2012 Volume.36 No. 1 p.55 ~ p.60
Effects of Ginsenoside Metabolites on GABAA Receptor-Mediated Ion Currents
Lee Byung-Hwan

Choi Sun-Hye
Shin Tae-Joon
Hwang Sung-Hee
Kang Ji-yeon
Kim Hyeon-Joong
Kim Byung-Joo
Nah Seung-Yeol
Abstract
In a previous report, we demonstrated that ginsenoside Rc, one of major ginsenosides from Panax ginseng, enhances
¥ã-aminobutyric acid (GABA) receptorA (GABAA)-mediated ion channel currents. However, little is known about the effects of ginsenoside metabolites on GABAA receptor channel activity. The present study investigated the effects of ginsenoside metabolites on human recombinant GABAA receptor (¥á1¥â1¥ã2s) channel activity expressed in Xenopus oocytes using a two-electrode voltage clamp technique. M4, a metabolite of protopanaxatriol ginsenosides, more potently inhibited the GABA-induced inward peak current (IGABA) than protopanaxadiol (PPD), a metabolite of PPD ginsenosides. The effect of M4 and PPD on IGABA was both concentration-dependent and reversible. The half-inhibitory concentration (IC50) values of M4 and PPD were 17.1¡¾2.2 and 23.1¡¾8.6 ¥ìM, respectively. The inhibition of IGABA by M4 and PPD was voltage- independent and non-competitive. This study implies that the regulation of GABAA receptor channel activity by ginsenoside metabolites differs from that of ginsenosides.
KEYWORD
Panax ginseng, Ginsenoside metabolites, Gamma-aminobutyric acid recepior A receptor , Xenopus oocytes,
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