Document Detail

Effects of ginsenosides on glycine receptor alpha1 channels expressed in Xenopus oocytes.
MedLine Citation:
PMID:  12661758     Owner:  NLM     Status:  MEDLINE    
Ginsenosides, major active ingredients of Panax ginseng, are known to regulate the excitatory ligand-gated ion channel activity. Recent reports showed that ginsenosides attenuate nicotinic acetylcholine and NMDA receptor channel activity. However, it is not known whether ginsenosides also affect the inhibitory ligand-gated ion channel activity. We investigated the effect of ginsenosides on human glycine alpha1 receptor channel activity expressed in Xenopus oocytes using a two-electrode voltage clamp technique. Treatment of ginsenoside Rf enhances glycine-induced inward peak current (IGly) with dose dependent and reversible manner but ginsenoside Rf itself did not elicit membrane currents. The half-stimulatory concentrations (EC50) of ginsenoside Rf was 49.8 +/- 8.9 microM. Glycine receptor antagonist strychnine completely blocked the inward current elicited by glycine plus ginsenoside Rf. Cl- channel blocker 4,4'-disothiocyanostilbene-2,2'-disulfonic acid (DIDS) also blocked the inward current elicited by glycine plus ginsenoside Rf. We also tested the effect of eight individual ginsenosides (i.e., Rb1, Rb2, Rc, Rd, Re, Rg1, Rg2, and Ro) in addition to ginsenoside Rf. We found that five of them significantly enhanced the inward current induced by glycine with the following order of potency: Rb1 > Rb2 > Rg2 > or = Rc > Rf > Rg1 > Re. These results indicate that ginsenosides might regulate gylcine receptor expressed in Xenopus oocytes and this regulation might be one of the pharmacological actions of Panax ginseng.
Jin-Hyeong Noh; Seok Choi; Jun-Ho Lee; Heinrich Betz; Jae-il Kim; Chul-Seung Park; Sang-Mok Lee; Seung-Yeol Nah
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Molecules and cells     Volume:  15     ISSN:  1016-8478     ISO Abbreviation:  Mol. Cells     Publication Date:  2003 Feb 
Date Detail:
Created Date:  2003-03-28     Completed Date:  2003-05-01     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9610936     Medline TA:  Mol Cells     Country:  Korea (South)    
Other Details:
Languages:  eng     Pagination:  34-9     Citation Subset:  IM    
Research Laboratory for the Study of Ginseng Signal Transduction, Department of Physiology, College of Veterinary Medicine Konkuk University, Seoul 143-701, Korea.
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MeSH Terms
4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid / pharmacology
Dose-Response Relationship, Drug
Ginsenosides / chemistry,  pharmacology*
Glycine / pharmacology
Molecular Structure
Panax / chemistry*
Patch-Clamp Techniques
Receptors, Glycine / drug effects*,  physiology
Recombinant Fusion Proteins / drug effects,  physiology
Strychnine / pharmacology
Xenopus laevis
Reg. No./Substance:
0/Ginsenosides; 0/Receptors, Glycine; 0/Recombinant Fusion Proteins; 0/glycine receptor alpha1; 53005-05-3/4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid; 56-40-6/Glycine; 57-24-9/Strychnine

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