The Korean Journal of Physiology and Pharmacology

The Korean Society of Pharmacology (대한약리학회)
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Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner

  • Wijerathne, Tharaka Darshana (Department of Physiology, College of Veterinary Medicine, Chungnam National University) ;
  • Kim, Ji Hyun (Department of Physiology, College of Veterinary Medicine, Chungnam National University) ;
  • Kim, Min Ji (Department of Physiology, College of Veterinary Medicine, Chungnam National University) ;
  • Kim, Chul Young (College of Pharmacy, Hanyang University) ;
  • Chae, Mee Ree (Department of Urology, Samsung Medical Center, Samsung Biomedical Research Institute, Sungkyunkwan University School of Medicine) ;
  • Lee, Sung Won (Department of Urology, Samsung Medical Center, Samsung Biomedical Research Institute, Sungkyunkwan University School of Medicine) ;
  • Lee, Kyu Pil (Department of Physiology, College of Veterinary Medicine, Chungnam National University)
  • Received : 2019.07.03
  • Accepted : 2019.08.02
  • Published : 2019.09.01
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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.

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References

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