Nuciferine relaxes tracheal rings via the blockade of VDLCC and NSCC channels
Nuciferine relaxes tracheal rings via the blockade of VDLCC and NSCC channels
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荷叶碱通过阻断 VDLCC 和 NSCC 通道来放松气管环
DOI：
10.1055/s-0043-118178
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发表时间：
2017-08
期刊：
影响因子：
2.7
通讯作者：
JINHUA SHEN
中科院分区：
文献类型：
--
作者：
XIAO YANG;MENG-FEI YU;JUN LEI;YONG-BO PENG;PING ZHAO;LU XUE;WEIWEI CHEN;LI-QUN MA;LIU-QING LIU;JINHUA SHEN
本研究旨在阐明荷叶提取物中主要的阿啡类生物碱荷叶碱（nuciferine）诱导气管环收缩松弛的作用机制。在无Ca2+和2 mM Ca2+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放松高K+收缩的小鼠气管环，抑制高K+诱导的Ca2+内流和电压依赖的l型Ca2+通道电流。同样，荷叶碱也以剂量依赖的方式抑制乙酰胆碱诱导的小鼠气管环收缩。同时，乙酰胆碱诱导的细胞内Ca2+内流和非选择性阳离子通道的全细胞电流均被nucifine阻断。总之，结果表明，在气管环中，nucifine诱导的松弛主要是由于通过阻断电压依赖性的l型Ca2+通道和/或非选择性阳离子通道来抑制细胞外Ca2+内流。这些结果表明，灯盏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有治疗作用
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 Ca2+-free and 2 mM Ca2+ 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 Ca2+ influx and voltage-dependent L-type Ca2+ 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 Ca2+ 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 Ca2+ influx through the blockade of voltage-dependent L-type Ca2+ 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
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