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Effects of equol on multiple K+ channels stably expressed in HEK 293 cells.

Effects of equol on multiple K+ channels stably expressed in HEK 293 cells.
Author Information (click to view)

Deng XL, Wang Y, Xiao GS,


Deng XL, Wang Y, Xiao GS, (click to view)

Deng XL, Wang Y, Xiao GS,

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PloS one 2017 08 2312(8) e0183708 doi 10.1371/journal.pone.0183708
Abstract

The present study investigated the effects of equol on cardiovascular K+ channel currents. The cardiovascular K+ channel currents were determined in HEK 293 cells stably expressing cloned differential cardiovascular K+ channels with conventional whole-cell patch voltage-clamp technique. We found that equol inhibited hKv1.5 (IC50: 15.3 μM), hKv4.3 (IC50: 29.2 μM and 11.9 μM for hKv4.3 peak current and charge area, respectively), IKs (IC50: 24.7 μM) and IhERG (IC50: 31.6 and 56.5 μM for IhERG.tail and IhERG.step, respectively), but not hKir2.1 current, in a concentration-dependent manner. Interestingly, equol increased BKCa current with an EC50 of 0.1 μM. It had no significant effect on guinea pig ventricular action potentials at concentrations of ≤3 μM. These results demonstrate that equol inhibits several cardiac K+ currents at relatively high concentrations, whereas it increases BKCa current at very low concentrations, suggesting that equol is a safe drug candidate for treating patients with cerebral vascular disorders.

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