Molecules and Cells

Korean Society for Molecular and Cellular Biology (한국분자세포생물학회)
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A Role for the Carbohydrate Portion of Ginsenoside Rg3 in Na+ Channel Inhibition

  • Kim, Jong-Hoon (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University) ;
  • Hong, Yoon-Hee (College of Pharmacy, Kyung Hee University) ;
  • Lee, Jun-Ho (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University) ;
  • Kim, Dong-Hyun (College of Pharmacy, Kyung Hee University) ;
  • Nam, Ghilsoo (Biochemicals Research Center, Korea Institute of Science and Technology) ;
  • Jeong, Sang Min (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University) ;
  • Lee, Byung-Hwan (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University) ;
  • Lee, Sang-Mok (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University) ;
  • Nah, Seung-Yeol (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University)
  • Received : 2004.08.03
  • Accepted : 2004.09.07
  • Published : 2005.02.28
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Abstract

We showed recently that ginsenosides inhibit the activity of various types of ion channel. Here we have investigated the role of the carbohydrate component of ginsenoside $Rg_3$ in the inhibition of $Na^+$ channels. The channels were expressed in Xenopus oocytes by injecting cRNAs encoding rat brain Nav1.2 ${\alpha}$ and ${\beta}1$ subunits, and analyzed by the two-electrode voltage clamp technique. Treatment with $Rg_3$ reversibly inhibited the inward $Na^+$ peak current ($I_{Na}$) with an $IC_{50}$ of $32.2{\pm}4.5{\mu}M$, and the inhibition was voltage-dependent. To examine the role of the sugar moiety, we prepared a straight chain form of the second glucose and a conjugate of this glucose with 3-(4-hydroxyphenyl) propionic acid hydrazide (HPPH). Neither derivative inhibited $I_{Na}$. Treatment with the carbohydrate portion of ginsenoside $Rg_3$, sophorose [${\beta}-D-glucopyranosyl$ ($1{\rightarrow}2$)-${\beta}-glucopyranoside$], or the aglycone (protopanaxadiol), on their own or in combination had no effect on $I_{Na}$. These observations indicate that the carbohydrate portion of ginsenoside $Rg_3$ plays an important role in its effect on the $Na^+$ channel.

Keywords

Acknowledgement

Supported by : Korea Ministry of Science and Technology

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