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荷叶碱通过阻断电压依赖性L型钙通道和非选择性阳离子通道舒张气管环。

Nuciferine Relaxes Tracheal Rings via the Blockade of VDLCC and NSCC Channels.

作者信息

Yang Xiao, Yu Meng-Fei, Lei Jun, Peng Yong-Bo, Zhao Ping, Xue Lu, Chen Weiwei, Ma Li-Qun, Liu Qing-Hua, Shen Jinhua

机构信息

Institute for Medical Biology and Hubei Provincial Key Laboratory for Protection and Application of Special Plant Germplasm in Wuling Area of China, College of Life Sciences, South-Central University for Nationalities, Wuhan, China.

出版信息

Planta Med. 2018 Jan;84(2):83-90. doi: 10.1055/s-0043-118178. Epub 2017 Aug 17.

Abstract

This study aimed to elucidate the mechanisms of nuciferine (a main aporphine alkaloid of lotus leaf extract), which can induce relaxation in contracted tracheal rings. Under Ca-free and 2 mM Ca conditions, we found that nuciferine had no effect on the resting muscle tone of tracheal rings. In contrast, nuciferine relaxed high K-contracted mouse tracheal rings in a dose-dependent manner and inhibited both Ca influx and voltage-dependent L-type Ca channel currents induced by high K. Similarly, nuciferine also inhibited acetylcholine-induced contractions in mouse tracheal rings in a dose-dependent manner. Meanwhile, both acetylcholine-induced intracellular Ca influx and whole-cell currents of nonselective cation channels were blocked by nuciferine. Together, the results indicate that nuciferine-induced relaxation in tracheal rings mainly occurred due to the inhibition of extracellular Ca influx through the blockade of voltage-dependent L-type Ca channels and/or nonselective cation channels. These results suggest that nuciferine has a therapeutic effect on respiratory diseases associated with the aberrant contraction of airway smooth muscles and/or bronchospasm.

摘要

本研究旨在阐明荷叶提取物的主要阿朴啡生物碱荷叶碱诱导收缩气管环舒张的机制。在无钙和2 mM钙条件下,我们发现荷叶碱对气管环的静息肌张力没有影响。相反,荷叶碱以剂量依赖的方式舒张高钾收缩的小鼠气管环,并抑制高钾诱导的钙内流和电压依赖性L型钙通道电流。同样,荷叶碱也以剂量依赖的方式抑制小鼠气管环中乙酰胆碱诱导的收缩。同时,荷叶碱阻断了乙酰胆碱诱导的细胞内钙内流和非选择性阳离子通道的全细胞电流。总之,结果表明荷叶碱诱导的气管环舒张主要是由于通过阻断电压依赖性L型钙通道和/或非选择性阳离子通道抑制了细胞外钙内流。这些结果表明荷叶碱对与气道平滑肌异常收缩和/或支气管痉挛相关的呼吸系统疾病具有治疗作用。

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