Inhibition of Kv7/M Channel Currents by Fangchinoline.

IF 2.9 4区医学 Q2 PHARMACOLOGY & PHARMACY Pharmacology Pub Date : 2023-01-01 DOI:10.1159/000527464

Han Li, DanDan Geng, Rong Zheng, Runmeng Wang, Yaning Li, Yidong Liu, Qingzhong Jia, Fan Zhang

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Abstract

Introduction: Voltage-gated Kv7/M potassium channels play an essential role in the control of membrane potential and neuronal excitability. Fangchinoline, a bisbenzylisoquinoline alkaloid, displays extensive biological activities including antitumor, anti-inflammatory, and antihypertension effects. In this study, we investigated the effects of fangchinoline on Kv7/M channels.

Methods: A perforated whole-cell patch technique was used to record Kv7 currents from HEK293 cells and M-type currents from mouse dorsal root ganglion (DRG) neurons.

Results: Fangchinoline inhibited Kv7.2/Kv7.3 currents in a concentration-dependent manner, with an IC50 of 9.5 ± 1.2 μM. Fangchinoline significantly inhibited Kv7.1, Kv7.2, Kv7.3, Kv7.4, and Kv7.3/Kv7.5 channels without selective effects. Furthermore, fangchinoline significantly slowed the activation of Kv7.1-Kv7.5 channels and inhibited native M-channel currents of DRG neurons.

Conclusion: Taken together, our findings indicate that fangchinoline concentration-dependently inhibited Kv7/M channel currents.

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芳胆碱对Kv7/M通道电流的抑制作用。

电压门控的Kv7/M钾通道在控制膜电位和神经元兴奋性中起着重要作用。芳喹啉是一种双苄基异喹啉类生物碱，具有抗肿瘤、抗炎、降压等广泛的生物活性。在本研究中，我们研究了防胆碱对Kv7/M通道的影响。方法:采用全细胞穿孔贴片技术记录HEK293细胞的Kv7电流和小鼠背根神经节(DRG)神经元的m型电流。结果:芳胆碱抑制Kv7.2/Kv7.3电流呈浓度依赖性，IC50为9.5±1.2 μM。方胆碱对Kv7.1、Kv7.2、Kv7.3、Kv7.4和Kv7.3/Kv7.5通道的抑制作用无选择性。此外，fangchinoline显著减缓了Kv7.1-Kv7.5通道的激活，抑制了DRG神经元的m通道电流。结论:综上所述，我们的研究结果表明，抗胆碱浓度依赖于抑制Kv7/M通道电流。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Pharmacology 医学-药学

CiteScore

5.60

自引率

0.00%

发文量

审稿时长

6-12 weeks

期刊介绍： ''Pharmacology'' is an international forum to present and discuss current perspectives in drug research. The journal communicates research in basic and clinical pharmacology and related fields. It covers biochemical pharmacology, molecular pharmacology, immunopharmacology, drug metabolism, pharmacogenetics, analytical toxicology, neuropsychopharmacology, pharmacokinetics and clinical pharmacology. In addition to original papers and short communications of investigative findings and pharmacological profiles the journal contains reviews, comments and perspective notes; research communications of novel therapeutic agents are encouraged.