KMID : 0352720110350020191
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Journal of Ginseng Research 2011 Volume.35 No. 2 p.191 ~ p.199
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Differential Effects of Ginsenoside Metabolites on HERG K? Channel Currents
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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
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Abstract
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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.
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KEYWORD
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Panax ginseng, Ginsenoside metabolites, Human ether-a-go-go-related gene K? channel, Human heart
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