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http://dx.doi.org/10.5762/KAIS.2011.12.6.2660

The effect of flavonoids on the TREK-1 channel  

Kim, Yang-Mi (Dept. of Physiology, College of Medicine, Chungbuk National University)
Kim, Kyung-Ah (Dept. of Biomedical Engineering, College of Medicine, Chungbuk National University)
Publication Information
Journal of the Korea Academia-Industrial cooperation Society / v.12, no.6, 2011 , pp. 2660-2667 More about this Journal
Abstract
TREK-1 channel is a member of the two-pore domain potassium (K2P) channel family that is regulated by intracellular pH, membrane stretch, polyunsaturated fatty acids, temperature, and some neuroprotectant agents. TREK-1 channel can influence neuronal excitability by regulating leakage of potassium ions and resting membrane potential. TREK-1 channel has been shown to be overexpressed in prostate cancer cells. Although the importance of these properties, relatively little is known about flavonoid effects in the regulations of TREK-1 channel. The purpose of the study was to screening of flavonoids as the TREK-1 channel modulator using one of electrophysiological techniques such as excised inside-out patch configuration. We demonstrated blocking effect on TREK-1 channel by flavonoids such as epigallocatechin-3-gallate (EGCG), curcumin and quercetin in CHO cells transiently expressing TREK-1 channel. The inhibition of TREK-1 channel by quercetin and curcumin was reversible, whereas EGCG was little reversible. Quercetin, EGCG and curcumin decreased the relative channel activity to 73%, 91% and 94%, respectively. The half-inhibitory concentration (IC50) of curcumin, quercetin and EGCG was $1.04{\pm}0.19\;{\mu}M$, $1.13{\pm}0.26\;{\mu}M$ and $13.5{\pm}2.20\;{\mu}M$ in CHO cells expressing TREK-1 channel, respectively. These results indicate that flavonoids might regulate TREK-1 and this regulation might be one of the pharmacological actions of flavonoid in nervous systems and cancer cells.
Keywords
TREK-1; Epigallocatechin-3-gallate (EGCG); Curcumin; Quercetin; Flavonoid; Single Channel;
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