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目的:观察川芎嗪对去氧肾上腺素(phenylcphrine,PHE)诱导大鼠胸主动脉收缩的阻断作用及机理。方法:用离体 SD 大鼠胸主动脉环作为实验对象,测定川芎嗪对其张力的影响。用细胞贴附式培养得到的单个平滑肌细胞,用标准的全细胞膜片钳技术记录大鼠平滑肌肌细胞膜 Cl通道的电流,观察不同浓度的川芎嗪对其影响。结果:川芎嗪对 PHE 引起动脉环双相收缩反应均有明显的阻断作用(P<0.01,n=8),其 IC_(50)值为3.2mmol/L;川芎嗪呈浓度依赖性的抑制100 mol/L KCl 的血管收缩效应,其 IC_(50)值为4.1mmo/L(P<0.01,n=6)。川芎嗪呈浓度依赖的抑制电压依赖性的 Cl~-通道电流-电压关系曲线(Ⅰ—Ⅴ)电流,但不影响其翻转电位。在测试电压为+100mV 时2.5、5mmol/L 川芎嗪对 Cl~-电流抑制率为45.45%、81.81%(P<0.01,n=6)。结论:川芎嗪对 PHE 诱导大鼠胸主动脉收缩有较好的松弛效应,其机理可能与影响 Ca~(2+)和 Cl~-通道跨膜转运有关。
OBJECTIVE: To observe the inhibitory effect of tetramethylpyrazine on phenylcrythine (PHE)-induced contraction of thoracic aorta in rats and its mechanism. METHODS: The effect of tetramethylpyrazine on the tension of isolated SD rat thoracic aorta rings was determined. The single smooth muscle cells obtained by cell attachment culture were used to record the Cl channel current of rat smooth muscle cell membrane using standard whole cell patch clamp technique. The effects of different concentrations of tetramethylpyrazine were observed. RESULTS: Tetramethylpyrazine had significant blockade effect on biphasic contraction of arterial rings induced by PHE (P<0.01, n=8). The IC50 value was 3.2 mmol/L; Tetramethylpyrazine was concentration-dependently inhibited. The vasoconstriction effect of 100 mol/L KCl had an IC 50 value of 4.1 mmo/L (P<0.01, n=6). Tetramethylpyrazine is a concentration-dependent voltage-dependent current-voltage curve (I-V), but does not affect its inversion potential. When the test voltage was +100 mV, the inhibitory rate of tetramethylpyrazine against Cl~- current was 45.45% and 81.81% (P<0.01, n=6). Conclusion: Tetramethylpyrazine has a good relaxation effect on PHE-induced thoracic aorta contraction, and its mechanism may be related to the transmembrane transport of Ca~(2+) and Cl~- channels.