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用膜片钳技术研究了植物杀虫剂苦皮藤素Ⅳ对棉铃虫幼虫离体培养中枢神经细胞钠通道门控过程的影响。结果表明,苦皮藤素Ⅳ对钠通道具有迅速的浓度依赖性阻滞作用,使电流-电压关系(I-V)曲线上移。0.1、1和10μmol/L苦皮藤素Ⅳ作用3min后,分别使钠电流峰值(INaMax)较给药前下降27.35%±4.05%、62.72%±2.81%和88.53%±5.56%(P<0.05),1和10μmol/L苦皮藤素Ⅳ还使钠通道的激活电压和峰电压分别向正电位方向移动了10mV和20mV左右。同时比较研究了利多卡因对棉铃虫幼虫神经细胞钠通道的影响,利多卡因对钠通道也具有阻滞作用,但有效作用浓度明显高于苦皮藤素Ⅳ。1、70mmol/L的利多卡因注射液作用3min后,使INaMax较用药前下降21.21%±2.52%和95.63%±2.10%(P<0.05)。苦皮藤素Ⅳ对钠通道门控过程的影响与利多卡因等局部麻醉剂非常相似,因此,对钠通道的阻滞作用可能是其发挥麻醉作用的重要机制。
Patch clamp technique was used to study the effect of cephornin IV on gating of sodium channels in cultured CNS of Helicoverpa armigera larvae. The results showed that celangulin Ⅳ had a rapid concentration-dependent block effect on the sodium channel and shifted the current-voltage relationship (I-V) curve upward. After treated with 0.1, 1, 10μmol / L celangulin Ⅳ for 3min, peak currents of INaMax decreased by 27.35% ± 4.05%, 62.72% ± 2.81% and 88.53% ± 5.56%, respectively ), And 1 and 10 μmol / L celangulin Ⅳ also caused the sodium channel activation voltage and peak voltage to move toward the positive potential by about 10mV and 20mV, respectively. At the same time, the effect of lidocaine on the sodium channels of the neurons in the larvae of cotton bollworm (Helicoverpa armigera) was also comparatively studied. Lidocaine also had a block effect on sodium channels, but the effective concentration of lidocaine was significantly higher than that of Celangulin Ⅳ. After 1 and 70 mmol / L lidocaine injection for 3 minutes, INaMax decreased by 21.21% ± 2.52% and 95.63% ± 2.10%, respectively (P <0.05). The effects of celangulin Ⅳ on sodium channel gating process are very similar to those of local anesthetics such as lidocaine. Therefore, the blockade of sodium channel may be an important mechanism of its anesthetic effect.