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Original Article

Korean J Physiol Pharmacol 2019; 23(5): 381-392

Published online September 1, 2019 https://doi.org/10.4196/kjpp.2019.23.5.381

Copyright © The Korean Journal of Physiology & Pharmacology.

Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner

Tharaka Darshana Wijerathne1, Ji Hyun Kim1, Min Ji Kim1, Chul Young Kim2, Mee Ree Chae3, Sung Won Lee3,*, and Kyu Pil Lee1,*

1Department of Physiology, College of Veterinary Medicine, Chungnam National University, Daejeon 34134, 2College of Pharmacy, Hanyang University, Ansan 15588, 3Department of Urology, Samsung Medical Center, Samsung Biomedical Research Institute, Sungkyunkwan University School of Medicine, Seoul 06351, Korea

Correspondence to:*Kyu Pil Lee, E-mail: kplee@cnu.ac.kr
*Sung Won Lee, E-mail: drswlee@skku.edu

Received: July 3, 2019; Revised: August 2, 2019; Accepted: August 2, 2019

This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License, which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Sperm function and male fertility are closely related to pH dependent K+ current (KSper) in human sperm, which is most likely composed of Slo3 and its auxiliary subunit leucine-rich repeat-containing protein 52 (LRRC52). Onion peel extract (OPE) and its major active ingredient quercetin are widely used as fertility enhancers; however, the effect of OPE and quercetin on Slo3 has not been elucidated. The purpose of this study is to investigate the effect of quercetin on human Slo3 channels. Human Slo3 and LRRC52 were co-transfected into HEK293 cells and pharmacological properties were studied with the whole cell patch clamp technique. We successfully expressed and measured pH sensitive and calcium insensitive Slo3 currents in HEK293 cells. We found that OPE and its key ingredient quercetin inhibit Slo3 currents. Inhibition by quercetin is dose dependent and this degree of inhibition decreases with elevating internal alkalization and internal free calcium concentrations. Functional moieties in the quercetin polyphenolic ring govern the degree of inhibition of Slo3 by quercetin, and the composition of such functional moieties are sensitive to the pH of the medium. These results suggest that quercetin inhibits Slo3 in a pH and calcium dependent manner. Therefore, we surmise that quercetin induced depolarization in spermatozoa may enhance the voltage gated proton channel (Hv1), and activate non-selective cation channels of sperm (CatSper) dependent calcium influx to trigger sperm capacitation and acrosome reaction.

Keywords: KSper, LRRC52, Phosphoinositides, Quercetin, Slo3