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

Deng, Xiu-Ling; Wang, Yan; Xiao, Guo-Sheng

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.

VOLTAGE-clamp techniques (Electrophysiology); CARDIOVASCULAR disease treatment; POTASSIUM channels; GENE expression; ACTION potentials; ANIMAL models in research

PLoS ONE, 2017, Vol 12, Issue 8, p1

1932-6203

Academic Journal

10.1371/journal.pone.0183708