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Selective modulation of L-type calcium current by magnesium lithospermate B in guinea-pig ventricular myocytes

机译：紫草酸镁B对豚鼠心室肌​​细胞选择性调节L型钙电流

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摘要

Magnesium lithospermate B (MLB) is the main water-soluble principle of Salviae Miltiorrhizae Radix (also called as 'Danshen' in the traditional Chinese medicine) for the treatment of cardiovascular diseases. MLB was found to possess a variety of pharmacological actions. However, it is unclear whether and how MLB affects the cardiac ion channels. In the present study, the effects of MLB on the voltage-activated ionic currents were investigated in single ventricular myocytes of adult guinea pigs. MLB reversibly inhibited L-type Ca2+ current (I-Ca.L) The inhibition was use-dependent and voltage-dependent (the IC50 value of MLB was 30 mu M and 393 mu M, respectively, at the holding potential of -50 mV and -100 mV). In the presence of 100 mu M MLB, both the activation and steady-state inactivation curves of I-Ca.L were markedly shifted to hyperpolarizing membrane potentials, whereas the time course of recovery of ICa.L from inactivation was not altered. MLB up to 300 PM had no significant effect on the fast-inactivating Na+ current (I-Na), delayed rectifier K+ current (I-K) and inward rectifier K+ current (I-K1). The results suggest that the voltage-dependent Ca2+ antagonistic effect of MLB work in concert with its antioxidant action for attenuating heart ischemic injury. (c) 2005 Elsevier Inc. All rights reserved.
机译：紫草酸镁B（MLB）是丹参（在传统中药中也称为“丹参”）的主要水溶性成分，可用于治疗心血管疾病。发现MLB具有多种药理作用。但是，目前尚不清楚MLB是否以及如何影响心脏离子通道。在本研究中，研究了成年豚鼠单心室心肌细胞中MLB对电压激活离子电流的影响。 MLB可逆地抑制L型Ca2 +电流（I-Ca.L）抑制作用取决于用途和电压依赖性（在保持电位为-50 mV时，MLB的IC50值分别为30μM和393μM。和-100 mV）。在存在100μMMLB的情况下，I-Ca.L的活化和稳态失活曲线均明显移向超极化膜电位，而从失活中恢复ICa.L的时间过程未改变。最高300 PM的MLB对快速灭活的Na +电流（I-Na），延迟整流器K +电流（I-K）和内向整流器K +电流（I-K1）没有明显影响。结果表明，MLB的电压依赖性Ca2 +拮抗作用与其减轻心肌缺血性损伤的抗氧化作用协同作用。 （c）2005 Elsevier Inc.保留所有权利。

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