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The novel mechanism of oxymatrine Affecting hERG currents at different temperatures

机译：氧化苦参碱在不同温度下影响hERG电流的新机制

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Background/Aims: Human ether-à-go-go-related gene (hERG) has an important role in the repolarization of the cardiac action potential. Our studies were to investigate the effects of oxymatrine (one of the natural constituents extracted from Chinese herb Sophora flavescens Ait) on hERG-encoded K~+ channels at different temperatures and its underlying mechanism. Methods: The effects of oxymatrine were examined on hERG channels stably expressed in HEK293 cells using a whole-cell patch clamp technique. Results: At the temperature 30°C, oxymatrine inhibited hERG current in a concentration-dependent manner and the IC_(50) was ～665 μM. However at the temperature of 20°C, low concentration oxymatrine C≤100 μM increased hERG current density. However, high concentration oxymatrine C>100 μM inhibited the hERG current density significantly. Oxymatrine only affected the activation kinetic of hERG channels at all temperatures and had a high binding affinity for open state of hERG channels except the 300 μM-20°C group which had a high binding affinity for inactive state of hERG channels. Conclusion: Oxymatrine is a low potency blocker of hERG K+ channels at 30°C, low concentration oxymatrine affect the hERG activation gating with accelerating hERG tail current at 20°C, oxymatrine is a potential hERG activator at low temperatures.
机译：背景/目的：人类走走相关基因（hERG）在心脏动作电位的复极化中起重要作用。我们的研究旨在研究氧化苦参碱（从中草药苦参提取的天然成分之一）在不同温度下对hERG编码的K〜+通道的作用及其潜在机制。方法：采用全细胞膜片钳技术检测氧化苦参碱对HEK293细胞中稳定表达的hERG通道的影响。结果：在30℃的温度下，氧化苦参碱以浓度依赖的方式抑制hERG电流，IC_（50）为〜665μM。然而，在20°C的温度下，低浓度的氧化苦参碱C≤100μM会增加hERG电流密度。然而，高浓度氧化苦参碱C> 100μM会显着抑制hERG电流密度。氧化苦参碱仅在所有温度下影响hERG通道的活化动力学，并且对hERG通道的开放状态具有高结合亲和力，除了300μM-20°C组对hERG通道的非激活状态具有高结合亲和力。结论：氧化苦参碱在30°C时是hERG K +通道的低效阻滞剂，低浓度氧化苦参碱在20°C时会加速hERG尾电流，从而影响hERG激活门控，氧化苦参碱在低温下是潜在的hERG激活剂。

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