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KMID : 0352720130370030324
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Journal of Ginseng Research
2013 Volume.37 No. 3 p.324 ~ p.331
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Differential effects of ginsenoside metabolites on slowly activating delayed rectifier K+ and KCNQ1 K+ channel currents
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Choi Sun-Hye
Lee Byung-Hwan
Kim Hyeon-Joong
Jung Seok-Won
Hwang Sung-Hee
Nah Seung-Yeol
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Abstract
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Channels formed by the co-assembly of the KCNQ1 subunit and the mink (KCNE1) subunit underline the slowly activating
delayed rectifier K+ channels (IKs) in the heart. This K+ channel is one of the main pharmacological targets for the development of drugs against cardiovascular disease. Panax ginseng has been shown to exhibit beneficial cardiovascular effects. In a previous study, we showed that ginsenoside Rg3 activates human KCNQ1 K+ channel currents through interactions with the K318 and V319 residues. However, little is known about the effects of ginsenoside metabolites on KCNQ1 K+ alone or the KCNQ1 + KCNE1 K+ (IKs) channels. In the present study, we examined the effect of protopanaxatriol (PPT) and compound K (CK) on KCNQ1 K+ and IKs channel activity expressed in Xenopus oocytes. PPT more strongly inhibited the IKs channel currents than the currents of KCNQ1 K+ alone in concentration- and voltage-dependent manners. The IC50 values on IKs and KCNQ1 alone currents for PPT were 5.18±0.13 and 10.04±0.17 μM, respectively. PPT caused a leftward shift in the activation curve of IKs channel activity, but minimally affected KCNQ1 alone. CK exhibited slight inhibition on IKs and KCNQ1 alone K+ channel currents. These results indicate that ginsenoside metabolites show limited effects on IKs channel activity, depending on the structure of the ginsenoside metabolites.
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KEYWORD
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Panax ginseng, Ginsenoside metabolites, Slowly activating delayed rectifier K+ channels (IKs), Human heart
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