Inhibition of the Human Ether-a-go-go-related Gene (HERG) K+ Channels by Lindera erythrocarpa.
10.3346/jkms.2009.24.6.1089
- Author:
Hee Kyung HONG
1
;
Weon Jong YOON
;
Young Ho KIM
;
Eun Sook YOO
;
Su Hyun JO
Author Information
1. Department of Physiology, Institute of Bioscience and Biotechnology, Kangwon National University College of Medicine, Chuncheon, Korea. suhyunjo@kangwon.ac.kr
- Publication Type:Original Article ; Research Support, Non-U.S. Gov't
- Keywords:
Anti-Tumor Activity;
Arrhythmias, Cardiac;
HERG Channel;
I(Kr);
Lindera erythrocarpa
- MeSH:
Animals;
Butanols/chemistry/metabolism;
Ether-A-Go-Go Potassium Channels/*antagonists & inhibitors/metabolism;
Female;
Humans;
Lindera/*chemistry;
Oocytes/cytology/physiology;
Patch-Clamp Techniques;
Plant Extracts/*metabolism;
Potassium Channel Blockers/*metabolism;
Xenopus laevis
- From:Journal of Korean Medical Science
2009;24(6):1089-1098
- CountryRepublic of Korea
- Language:English
-
Abstract:
Lindera erythrocarpa Makino (Lauraceae) is used as a traditional medicine for analgesic, antidote, and antibacterial purposes and shows anti-tumor activity. We studied the effects of Lindera erythrocarpa on the human ether-a-go-go-related gene (HERG) channel, which appears of importance in favoring cancer progression in vivo and determining cardiac action potential duration. Application of MeOH extract of Lindera erythrocarpa showed a dose-dependent decrease in the amplitudes of the outward currents measured at the end of the pulse (I(HERG)) and the tail currents of HERG (I(tail)). When the BuOH fraction and H2O fraction of Lindera erythrocarpa were added to the perfusate, both I(HERG) and I(tail) were suppressed, while the hexane fraction, CHCl3 fraction, and EtOAc fraction did not inhibit either I(HERG) or I(tail). The potential required for half-maximal activation caused by EtOAc fraction, BuOH fraction, and H2O fraction shifted significantly. The BuOH fraction and H2O fraction (100 microgram/mL) decreased gmax by 59.6% and 52.9%, respectively. The H2O fraction- and BuOH fraction-induced blockades of I(tail) progressively decreased with increasing depolarization, showing the voltage-dependent block. Our findings suggest that Lindera erythrocarpa, a traditional medicine, blocks HERG channel, which could contribute to its anticancer and cardiac arrhythmogenic effect.
