利科哈尔科尼通过准电压关闭的通道来调解疼痛缓解
Qianru Zhao1, Xu Zhang1, Siru Long1
1Department of Chemical Biology, School of Pharmaceutical Sciences, South-Central Minzu University, Wuhan, People's Republic of China (Q.Z., X.Z., S.L., S.W., H.Y., Y.Z., Y.H., S.Y.) and Institute for Medical Biology and Hubei Provincial Key Laboratory for Protection and Application of Special Plants in Wuling Area of China, College of Life Sciences, South-Central Minzu University, Wuhan, People's Republic of China (Y.L., L.X.).
Molecular pharmacology
|July 7, 2023
概括
来自甘的利科哈尔康A抑制通道,并减少神经元和动物模型中的疼痛反应. 利科哈尔科尼B显示了一些缓解疼痛的效果,这表明有可能开发新的止痛药.
科学领域:
- 神经科学和药理学 神经科学和药理学
- 传统中国医药 传统中国医药
- 分子生物学分子生物学
背景情况:
- 甘草具有传统的止痛作用,但其潜在的分子机制在很大程度上仍未被阐明.
- 利可卡尔A (LCA) 和利可卡尔B (LCB) 是甘中发现的关键化合物,具有潜在的治疗应用.
- 电压接 (NaV) 通道,特别是NaV1.7,对于疼痛信号和神经元刺激性至关重要.
研究的目的:
- 为了比较Licochalcone A和Licochalcone B的止痛作用.
- 调查分子机制,重点关注电压关闭的电流和神经元刺激性.
- 在临床前疼痛模型中评估LCA和LCB的疗效.
主要方法:
- 背部根性质神经元 (DRG) 和表达NaV1.7通道的HEK293T细胞的电生理学记录 (全细胞补丁).
- 测量电压关闭的 (NaV) 电流和作用电位.
- 在动物模型中进行形式素诱导的疼痛行为测试.
主要成果:
- 利科哈尔孔A显著抑制了NaV电流,并降低了DRG神经元的刺激性.
- 利科哈尔科恩A还抑制了外源表达的NaV 1.7通道.
- 利科哈尔康B并没有抑制NaV电流,但在甲素测试的后期阶段显示出止痛作用,而LCA在两个阶段都显示出效果.
结论:
- 利科哈尔A通过抑制NaV电流和神经元刺激性,特别是通过NaV1.7通道,表现出强大的止痛特性.
- LCA和LCB对NaV电流的独特影响为开发新型NaV通道抑制剂提供了基础.
- 利科哈尔科尼,特别是LCA,代表了开发有效止痛药物的有前途的化合物.
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