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目的研究3,5,4’-三甲基白藜芦醇(trans-resveratrol derivative3,5,4’-trimethoxystilbene,TMS)对豚鼠心室肌细胞钠电流(INa)和钾电流(IK1)的直接作用,探讨其心肌保护作用。方法用全细胞膜片钳技术记录TMS对单个心室肌细胞INa和IK1的作用。结果TMS(10μmol·L-1)可快速抑制豚鼠心室肌细胞INa,用药后3min左右即开始起效,10min时抑制率为(36.8±5.6)%(P<0.005),洗脱后可完全恢复;1,3μmol·L-1TMS未影响INa大小。TMS不改变INa的最大激活电压,也不影响IK1的大小。10μmol·L-1使半数最大失活电压(V1/2)由(-87.0±3.3)mV变化到(-96.7±3.5)mV(P<0.001),使失活曲线斜率(S)由(4.9±0.3)mV变化到(5.4±0.3)mV(P<0.01);使半数最大激活电压(V1/2)(-38.9±1.4)mV变化到(-47.3±1.3)mV(P<0.001),未改变激活S。结论TMS可直接作用于豚鼠心室肌细胞,快速抑制INa,且此作用快速、可逆。
Objective To investigate the direct effect of trans-resveratrol derivative 3,5,4’-trimethoxystilbene (TMS) on sodium current (INa) and potassium current (IK1) in guinea pig ventricular myocytes , To explore its myocardial protective effect. Methods Whole-cell patch-clamp technique was used to record the effects of TMS on INa and IK1 in isolated ventricular myocytes. Results TMS (10μmol·L-1) could rapidly inhibit the INa of guinea pig ventricular myocytes, which started to function at about 3min after treatment. The inhibition rate was (36.8 ± 5.6)% at 10min (P <0.005) ; 1,3μmol·L-1TMS did not affect the size of INa. TMS does not change the maximum activation voltage of INa, nor does it affect the size of IK1. The slope of the inactivation curve (S) was changed from (4.9) to (-96.7 ± 3.5) mV (-96.7 ± 3.5) mV by the addition of 10μmol·L- (-4.3 ± 1.3) mV (P <0.001), and the maximum activation voltage (V1 / 2) (-38.9 ± 1.4) mV changed to (5.4 ± 0.3) mV S unchanged Conclusion TMS can directly act on guinea pig ventricular myocytes and rapidly inhibit INa, and its effect is rapid and reversible.