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KMID : 0352720110350020191
Journal of Ginseng Research
2011 Volume.35 No. 2 p.191 ~ p.199
Differential Effects of Ginsenoside Metabolites on HERG K? Channel Currents
Choi Sun-Hye

Shin Tae-Joon
Hwang Sung-Hee
Lee Byung-Hwan
Kang Ji-Yeon
Kim Hyeon-Joong
Oh Jae-Wook
Bae Chun-Sik
Lee Soo-Han
Nah Seung-Yeol
Abstract
The human ether-a-go-go-related gene (HERG) cardiac K? channels are one of the representative pharmacological targets for development of drugs against cardiovascular diseases such as arrhythmia. Panax ginseng has been known to exhibit cardioprotective effects. In a previous report we demonstrated that ginsenoside Rg©ý regulates HERG K? channels by decelerating deactivation. However, little is known about how ginsenoside metabolites regulate HERG K? channel activity. In the present study, we examined the effects of ginsenoside metabolites such as compound K (CK), protopanaxadiol (PPD), and protopanaxatriol (PPT) on HERG K? channel activity by expressing human a subunits in Xenopus oocytes. CK induced a large persistent deactivatingtail current (Ideactivating-tail) and significantly decelerated deactivating current decay in a concentration-dependent manner. The EC?? for persistent Ideactivating-tail was 16.6¡¾1.3 ¥ìM. In contrast to CK, PPT accelerated deactivating-tail current deactivation. PPD itself had no effects on deactivating-tail currents, whereas PPD inhibited ginsenoside Rg©ý-induced persistent Ideactivating-tail and accelerated HERG K+ channel deactivation in a concentration-dependent manner. These results indicate that ginsenoside metabolites exhibit differential regulation on Ideactivating-tail of HERG K? channel.
KEYWORD
Panax ginseng, Ginsenoside metabolites, Human ether-a-go-go-related gene K? channel, Human heart
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