Song Tao, Chu Xi, Zhang Xuan, Song Qiongtao, Zhang Ying, Zhang Yuanyuan, Han Xue, Zhang Jianping, Chu Li
Hebei Medical University, No. 361, East Zhongshan Road, Shijiazhuang, 050017, Hebei, China.
The Fourth Hospital of Hebei Medical University, No. 12, Jiankang Road, Shijiazhuang, 050011, Hebei, China.
Fundam Clin Pharmacol. 2017 Jun;31(3):340-346. doi: 10.1111/fcp.12265. Epub 2017 Mar 1.
Bufalin is a bufanolide steroid compound in Chan Su. Chan Su is a traditional Chinese medicine prepared from the dried white secretion of the auricular and skin glands of toads and has been used as an oriental drug. However, the effect of bufalin on cardiac function and its underlying cellular mechanisms remain unclear. Here, we explore the cellular mechanisms of bufalin on myocardial protection via the whole-cell patch-clamp recording and video-based edge detection system. Exposure to bufalin resulted in a concentration-dependent blockade of I , with the half-maximal inhibitory concentration (IC ) of 60 μm and the maximal inhibitory effect of 71.50 ± 2.67%. Bufalin at 100 μm reduced cell shortening by 33.83 ± 4.01%. Bufalin restrained L-type Ca channels conductance, and contractility in rat ventricular myocytes. Thus, the protective effects of bufalin on the heart may be determined by the inhibitory effect on I and the negative inotropic action caused by the decrease of intracellular Ca in rat myocardial cells.
蟾毒灵是蟾酥中的一种蟾蜍甾二烯类甾体化合物。蟾酥是一种由蟾蜍耳后腺及皮肤腺的干燥白色分泌物制成的传统中药，一直被用作一种东方药物。然而，蟾毒灵对心脏功能的影响及其潜在的细胞机制仍不清楚。在此，我们通过全细胞膜片钳记录和基于视频的边缘检测系统探索蟾毒灵心肌保护作用的细胞机制。暴露于蟾毒灵导致I的浓度依赖性阻断，半数最大抑制浓度（IC）为60μm，最大抑制作用为71.50±2.67%。100μm的蟾毒灵使细胞缩短减少33.83±4.01%。蟾毒灵抑制大鼠心室肌细胞L型钙通道电导和收缩性。因此，蟾毒灵对心脏的保护作用可能取决于对I的抑制作用以及大鼠心肌细胞内钙减少引起的负性肌力作用。
