Bufalin, a bufanolide steroid from the parotoid glands of the Chinese toad, suppresses hERG K+ currents expressed in HEK293 cells

被引:8
|
作者
Song, Tao [1 ]
Zhang, Yuanyuan [1 ,2 ]
Song, Qiongtao [1 ]
Han, Xue [1 ]
Guan, Shengjiang [1 ]
Zhang, Xuan [1 ,2 ]
Chu, Xi [3 ]
Zhang, Fenghua [1 ]
Zhang, Jianping [1 ,2 ]
Chu, Li [1 ,2 ]
机构
[1] Hebei Univ Chinese Med, 3 Xingyuan Rd, Shijiazhuang 050200, Hebei, Peoples R China
[2] Hebei Key Lab Integrat Med Liver Kidney Patterns, Shijiazhuang 050200, Hebei, Peoples R China
[3] Hebei Med Univ, Hosp 4, Dept Pharm, 12 Jiankang Rd, Shijiazhuang 050011, Hebei, Peoples R China
关键词
Bufalin; cardiac arrhythmia; hERG K+ channels; LONG QT SYNDROME; IN-VITRO; PROTEIN TRAFFICKING; POTASSIUM CHANNELS; CALCIUM-CHANNEL; HEK-293; CELLS; BUFADIENOLIDES; BLOCK; DRUG; MICE;
D O I
10.1111/fcp.12306
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In this study, we investigated the effect of bufalin on the human ether-a-go-go-related gene (hERG) K+ channels using the perforated patch recording technique. We measured a half-maximal inhibitory concentration (IC50) of 24.83 M and maximal inhibitory effect of 39.45 +/- 1.14% with bufalin. These findings suggest that bufalin is a potent hERG K+ channel blocker and may provide a new way for understanding Chan Su-induced arrhythmia.
引用
收藏
页码:695 / 700
页数:6
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