Journal of Ginseng Research

The Korean Society of Ginseng (고려인삼학회)
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Effects of Ginsenoside Metabolites on GABAA Receptor-Mediated Ion Currents

  • Lee, Byung-Hwan (Ginsentology Research Laboratory and Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University) ;
  • Choi, Sun-Hye (Ginsentology Research Laboratory and Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University) ;
  • Shin, Tae-Joon (Ginsentology Research Laboratory and Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University) ;
  • Hwang, Sung-Hee (Ginsentology Research Laboratory and Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University) ;
  • Kang, Ji-Yeon (Ginsentology Research Laboratory and Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University) ;
  • Kim, Hyeon-Joong (Ginsentology Research Laboratory and Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University) ;
  • Kim, Byung-Ju (Division of Longevity and Biofunctional Medicine, Pusan National University School of Korean Medicine) ;
  • Nah, Seung-Yeol (Ginsentology Research Laboratory and Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University)
  • Received : 2011.10.14
  • Accepted : 2011.12.05
  • Published : 2012.01.11
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Abstract

In a previous report, we demonstrated that ginsenoside Rc, one of major ginsenosides from Panax ginseng, enhances ${\gamma}$-aminobutyric acid (GABA) $receptor_A$ ($GABA_A$)-mediated ion channel currents. However, little is known about the effects of ginsenoside metabolites on $GABA_A$ receptor channel activity. The present study investigated the effects of ginsenoside metabolites on human recombinant $GABA_A$ receptor (${\alpha}_1{\beta}_1{\gamma}_{2s}$) 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 ($I_{GABA}$) than protopanaxadiol (PPD), a metabolite of PPD ginsenosides. The effect of M4 and PPD on $I_{GABA}$ was both concentration-dependent and reversible. The half-inhibitory concentration ($IC_{50}$) values of M4 and PPD were 17.1${\pm}$2.2 and 23.1${\pm}$8.6 ${\mu}M$, respectively. The inhibition of $I_{GABA}$ by M4 and PPD was voltage-independent and non-competitive. This study implies that the regulation of $GABA_A$ receptor channel activity by ginsenoside metabolites differs from that of ginsenosides.

Keywords

References

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