Cited by 80Nicotinic Acetylcholine Receptors StudyGinseng Biological Effects and ApplicationsNeuroscience and Neuropharmacology Research

Effects of ginsenoside Rg2 on human neuronal nicotinic acetylcholine receptors

Sala, Francisco, Mulet, José, Choi, Seok, Jung, Se-Yeon, Nah, Seung-Yeol, Rhim, Hyewhon, Valor, Luis Miguel, Criado, Manuel +1 more·2002·The Journal of Pharmacology and Experimental Therapeutics

Abstract

Ginseng saponins, major active components of ginseng root used by folk medicine in the treatment of various diseases, produce multiple pharmacological responses having many effects on the central and peripheral nervous system. Specifically, ginsenoside Rg(2) has been shown to block the nicotinic acetylcholine receptors in bovine chromaffin cells. We have studied the effect of Rg(2) on different types of human neuronal nicotinic acetylcholine receptors (nAChRs), both homomeric and heteromeric, expressed in Xenopus oocytes. Rg(2) did not affect the acetylcholine (ACh)-induced currents in alpha(7) human receptors, however Rg(2) affected the peak currents, and mainly the desensitization of heteromeric receptors alpha(3)beta(4), alpha(3)beta(2), alpha(4)beta(4), and alpha(4)beta(2). Both effects, a diminution of peak current and an increase of desensitization, are dose-dependent and are very similar for all the receptors. The mechanism of action has been studied in more detail in alpha(3)beta(4) and alpha(4)beta(2) receptors where we found a negligible shift in the ACh dose-response curves and a persistence of the Rg(2) effects at high ACh concentrations, indicative of a noncompetitive antagonism. A lack of voltage dependence on the reduction of the peak currents induced by ACh also suggests that Rg(2) does not act as an open channel blocker of human nAChR. The results indicate that Rg(2) acts specifically on heteromeric human nAChRs modulating their desensitization and suggest a possible mechanism by which this saponin contributes to the multiple therapeutic effects of ginseng.

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Crossref · 10.1124/jpet.301.3.1052

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  • Ginseng extract enhances relaxation caused by transmural electrical stimulation or nicotine in monkey cerebral arterial strips.

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Authors
Sala, F., Mulet, J., Choi, S., Jung, S.-Y., Nah, S.-Y., Rhim, H., Valor, L. M., Criado, M., & Sala, S.
Affiliations
Consejo Superior de Investigaciones Científicas (ES)
Venue
The Journal of Pharmacology and Experimental Therapeutics
Publisher
Elsevier BV
Published
2002-06
Volume
301
Issue
3
Pages
1052-1059
ISSN
0022-3565 (ISSN-L)
OpenAlex
W2126352957
Cited by
80
References
37
Citations by year
2025: 1 · 2024: 1 · 2023: 2 · 2022: 1 · 2021: 1 · 2020: 2 · 2019: 2 · 2018: 2 · 2017: 2 · 2016: 1 · 2015: 2 · 2014: 3 · 2013: 1 · 2012: 2
FWCI
3.24
Type
journal article
Language
en
Open access
closed
Locations
  • Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
  • PubMed (publishedVersion)
  • DIGITAL.CSIC (Spanish National Research Council (CSIC)) (submittedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ginseng Biological Effects and Applications
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords
ginsenoside Rg2, ginsenosides, neuronal nicotinic acetylcholine receptors, alpha4beta2 receptor, receptor desensitization, non-competitive antagonism, acetylcholine-induced currents
MeSH terms
Animals, Dose-Response Relationship, Drug, Genetic Vectors, Panax, Humans, Ion Channels, Membrane Potentials, Oocytes, Receptors, Nicotinic, Saponins, Transfection, Xenopus, Patch-Clamp Techniques, Ginsenosides

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