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

Abstract

In this study, we investigated the effect of bufalin on the human ether-à-go-go-related gene (hERG) K+ channels using the perforated patch recording technique. We measured a half-maximal inhibitory concentration (IC50 ) of 24.83 μM 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.

• Authors: Tao Song, Yuanyuan Zhang, Qiongtao Song, Xue Han, Shengjiang Guan, Xuan Zhang, Xi Chu, Fenghua Zhang, Jianping Zhang, Li Chu
• Journal: Fundamental & clinical pharmacology (Fundam Clin Pharmacol) Vol. 31 Issue 6 Pg. 695-700 (Dec 2017) ISSN: 1472-8206 [Electronic] England
• PMID: 28755515 (Publication Type: Journal Article)
• Copyright: © 2017 Société Française de Pharmacologie et de Thérapeutique.

Chemical References

• Bufanolides
• Calcium Channels, L-Type
• Steroids
• chan su
• bufalin

Topics

• Animals
• Anura
• Arrhythmias, Cardiac (chemically induced, drug therapy)
• Bufanolides (adverse effects, pharmacology)
• Calcium Channels, L-Type (metabolism)
• HEK293 Cells (drug effects, metabolism)
• Humans
• Medicine, Chinese Traditional
• Parotid Gland (chemistry)
• Steroids (pharmacology)