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人参皂苷在神经系统中的药理学:参与离子通道和受体的调节

Ginseng ginsenoside pharmacology in the nervous system: involvement in the regulation of ion channels and receptors.

作者信息

Nah Seung-Yeol

机构信息

Ginsentology Research Laboratory, Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University Seoul, South Korea.

出版信息

Front Physiol. 2014 Mar 19;5:98. doi: 10.3389/fphys.2014.00098. eCollection 2014.

DOI:10.3389/fphys.2014.00098
PMID:24678300
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3958645/
Abstract

Ginseng, the root of Panax ginseng C.A. Meyer, is one of the oldest traditional medicines and is thought to be a tonic. It has been claimed that ginseng may improve vitality and health. Recent studies have advanced ginseng pharmacology and shown that ginseng has various pharmacological effects in the nervous system. Ginsenosides, steroid glycosides extracted from ginseng, were one of the first class of biologically active plant glycosides identified. The diverse pharmacological effects of ginsenosides have been investigated through the regulation of various types of ion channels and receptors in neuronal cells and heterologous expression systems. Ginsenoside Rg3 regulates voltage-gated ion channels such as Ca(2+), K(+), and Na(+) channels, and ligand-gated ion channels such as GABAA, 5-HT3, nicotinic acetylcholine, and N-methyl-D-aspartate (NMDA) receptors through interactions with various sites including channel blocker binding sites, toxin-binding sites, channel gating regions, and allosteric channel regulator binding sites when the respective ion channels or receptors are stimulated with depolarization or ligand treatment. Treatment with ginsenoside Rg3 has been found to stabilize excitable cells by blocking influxes of cations such as Ca(2+) and Na(+), or by enhancing Cl(-) influx. The aim of this review is to present recent findings on the pharmacological functions of the ginsenosides through the interactions with ion channels and receptors. This review will detail the pharmacological applications of ginsenosides as neuroprotective drugs that target ion channels and ligand-gated ion channels.

摘要

人参是五加科人参属植物人参(Panax ginseng C.A. Meyer)的根,是最古老的传统药物之一,被认为是一种滋补品。据称人参可以改善活力和健康状况。最近的研究推动了人参药理学的发展,并表明人参在神经系统中具有多种药理作用。人参皂苷是从人参中提取的甾体糖苷,是最早被鉴定出的一类生物活性植物糖苷之一。人参皂苷的多种药理作用已通过调节神经元细胞和异源表达系统中各种类型的离子通道和受体进行了研究。人参皂苷Rg3通过与包括通道阻滞剂结合位点、毒素结合位点、通道门控区域和变构通道调节剂结合位点在内的各种位点相互作用,调节电压门控离子通道,如Ca(2+)、K(+)和Na(+)通道,以及配体门控离子通道,如GABAA、5-HT3、烟碱型乙酰胆碱和N-甲基-D-天冬氨酸(NMDA)受体,当相应的离子通道或受体受到去极化或配体处理刺激时。已发现用人参皂苷Rg3处理可通过阻断Ca(2+)和Na(+)等阳离子的内流,或通过增强Cl(-)内流来稳定可兴奋细胞。本综述的目的是介绍人参皂苷通过与离子通道和受体相互作用所发挥药理功能的最新研究结果。本综述将详细阐述人参皂苷作为靶向离子通道和配体门控离子通道的神经保护药物的药理应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/07aa/3958645/552ffbf10a30/fphys-05-00098-g0005.jpg
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Effects of ginsenoside Rg3 on α9α10 nicotinic acetylcholine receptor-mediated ion currents.人参皂苷 Rg3 对 α9α10 烟碱型乙酰胆碱受体介导的离子流的影响。
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Ginsenoside Rg₃ regulates GABAA receptor channel activity: involvement of interaction with the γ₂ subunit.
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Emerging evidence that ginseng components improve cognition in subjective memory impairment, mild cognitive impairment, and early Alzheimer's disease dementia.新出现的证据表明,人参成分可改善主观记忆障碍、轻度认知障碍和早期阿尔茨海默病痴呆症患者的认知能力。
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