Effect of matrine on human ether à go-go related gene (HERG) channels expressed in Chinese hamster ovary cells.
- Author:
Hong-jin WU
1
;
An-ruo ZOU
;
Fang XIE
;
Yi-mei DU
;
Yu CAO
;
Yu-na LIU
;
Ji-yuan YANG
;
Xin-min LI
Author Information
- Publication Type:Journal Article
- MeSH: Alkaloids; pharmacology; Animals; CHO Cells; Cricetinae; Cricetulus; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; genetics; metabolism; Humans; Quinolizines; pharmacology
- From: Chinese journal of integrative medicine 2010;16(5):430-434
- CountryChina
- Language:English
-
Abstract:
OBJECTIVETo 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
METHODSHERG channel potassium current in CHO cell was recorded using whole-cell patch-clamp technique, and the influence of matrine on the current was explored.
RESULTSMatrine 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.
CONCLUSIONSThe 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.
