Effect of matrine on human ether à go-go related gene (HERG) channels expressed in Chinese hamster ovary cells.
OBJECTIVE
To observe the effect of matrine on human ether à go-go related gene (HERG) potassium channels expressed in Chinese hamster ovary (CHO) cells and investigate whether HERG channel is a new target of the pharmacological effect of matrine on arrhythmia and tumor


METHODS
HERG channel potassium current in CHO cell was recorded using whole-cell patch-clamp technique, and the influence of matrine on the current was explored.


RESULTS
Matrine inhibited HERG potassium current in a dose-dependent manner, and the 50% inhibitory concentration (IC IC(50)) was 411±23 μmol/L. Matrine had no significant effect on the activation kinetics, and mainly blocked HERG channels in their closed state.


CONCLUSIONS
The blocking effect of matrine on HERG channels might be one of the mechanisms against arrythmias and tumors. Unlike most other blockers exerting blocking effect at the intracellular sites by entering the cell with the opening of HERG channel, matrine blocked HERG channels at the extracellular sites.
Wu
Hong-jin
HJ
Beijing Hospital of Integrated Traditional Chinese and Western Medicine, China. whjyuanzhang@yahoo.com.cn
Zou
An-ruo
AR
Xie
Fang
F
Du
Yi-mei
YM
Cao
Yu
Y
Liu
Yu-na
YN
Yang
Ji-yuan
JY
Li
Xin-min
XM
D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels / Q000235:genetics* / Q000378:metabolism; D006801:Humans; D011807:Quinolizines / Q000494:pharmacology*; D000093842:Matrines
D000470:Alkaloids; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; C000606913:KCNH2 protein, human; D011807:Quinolizines; D000093842:Matrines