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槲皮素对大鼠DRG神经元Nav1.8电流的作用及机制

刘丽娜, 于鹏, 陈利, 孙志广, 汤依群

刘丽娜, 于鹏, 陈利, 孙志广, 汤依群. 槲皮素对大鼠DRG神经元Nav1.8电流的作用及机制[J]. 中国药科大学学报, 2015, 46(1): 94-99. DOI: 10.11665/j.issn.1000-5048.20150114
引用本文: 刘丽娜, 于鹏, 陈利, 孙志广, 汤依群. 槲皮素对大鼠DRG神经元Nav1.8电流的作用及机制[J]. 中国药科大学学报, 2015, 46(1): 94-99. DOI: 10.11665/j.issn.1000-5048.20150114
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LIU Lina, YU Peng, CHEN Li, SUN Zhiguang, TANG Yiqun. Effects and mechanism of quercetin on electric current of Nav1.8 in rat dorsal root ganglion neurons[J]. Journal of China Pharmaceutical University, 2015, 46(1): 94-99. DOI: 10.11665/j.issn.1000-5048.20150114
Citation: LIU Lina, YU Peng, CHEN Li, SUN Zhiguang, TANG Yiqun. Effects and mechanism of quercetin on electric current of Nav1.8 in rat dorsal root ganglion neurons[J]. Journal of China Pharmaceutical University, 2015, 46(1): 94-99. DOI: 10.11665/j.issn.1000-5048.20150114
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槲皮素对大鼠DRG神经元Nav1.8电流的作用及机制

  • 1.

    南京中医药大学附属医院江苏省中医院

  • 2.

    南京中医药大学第一临床医学院

  • 3.

    中国药科大学药理学研究室

  • 4.

    香港浸会大学中医药学院

基金项目: 江苏省自然科学基金青年基金资助项目(No.BK20140959)；高等学校博士学科点专项科研基金资助项目(No.20133237110008)

Effects and mechanism of quercetin on electric current of Nav1.8 in rat dorsal root ganglion neurons

摘要

    摘要
  • 摘要: 研究槲皮素(Que)对大鼠脊髓背根神经节(DRG)神经元Nav1.8通道电流(INav1.8)的作用。在急性分离的大鼠DRG神经元上，用全细胞膜片钳技术，观察Que干预INav1.8的剂量-反应关系以及Que影响的Nav1.8通道电压依赖的激活和失活特性。结果显示Que(10，30，100 μmol/L)可浓度依赖地抑制DRG神经元INav1.8峰值，峰值抑制率分别为(15.32±3.43)%，(22.92±8.24)%和(47.29±11.42)%，半数抑制浓度(IC50)为121.38 μmol/L，Hill系数为0.76；100 μmol/L Que可使DRG神经元的Nav1.8通道激活曲线向去极化方向偏移了0.83 mV，失活曲线向超极化方向偏移了1.86 mV；且与干预前比，半数失活电压(V1/2)为-(40.23±0.25)mV，有显著性差异(P<；0.01)。说明Que可浓度依赖和电压依赖地抑制DRG神经元Nav1.8通道活性，进而降低痛觉信息的传递，改善慢性内脏痛。
    Abstract: To study the effects of quercetin(Que)on the electric current of Nav1. 8(INav1. 8)in rat dorsal root ganglion(DRG)neurons, dose-effect relationship of Que on INav1. 8 and the activation and inactivation properties of voltage-dependent Nav1. 8 influenced by Que were studied by using the whole-cell patch clamp technique in fresh isolated rat DRG neurons. It was found that diffeent concerntrations of Que(10, 30, 100 μmol/L)could inhibit INav1. 8 peak value of DRG neurons in concentration-dependent manner. The inhibition of peak currents were(15. 32±3. 43)%, (22. 92±8. 24)% and(47. 29±11. 42)% respectively, the IC50 was 121. 38 μmol/L and the Hill coefficient was 0. 76. In the existence of Que(100 μmol/L), the activation curve of Nav1. 8 channel in DRG was slightly shifted to depolarizing direction for 0. 83 mV, and the inactivation curve was shifted to hyperpolarizing direction for 1. 86 mV. Compared with the stage before intervention, the half-activation voltage(V1/2=-40. 23±0. 25 mV)was significantly different(P< 0. 01). In conclusion, Que inhibits the Nav1. 8 channel activity in dose and voltage-dependent manner, which may count for the reduction of algesthesia transmission and the alleviation of chronic visceral pain.
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  • 刊出日期:  2015-02-24

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