The Korean Journal of Physiology and Pharmacology

The Korean Society of Pharmacology (대한약리학회)
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Taxifolin Glycoside Blocks Human ether-a-go-go Related Gene $K^+$ Channels

  • Yun, Jihyun (Department of Physiology, College of Medicine, Chung-Ang University) ;
  • Bae, Hyemi (Department of Physiology, College of Medicine, Chung-Ang University) ;
  • Choi, Sun Eun (Department of Cosmetology Science, Nambu University) ;
  • Kim, Jung-Ha (Department of Family Medicine, College of Medicine, Chung-Ang University) ;
  • Choi, Young Wook (College of Pharmacy, Chung-Ang University) ;
  • Lim, Inja (Department of Physiology, College of Medicine, Chung-Ang University) ;
  • Lee, Chung Soo (Department of Pharmacology, College of Medicine, Chung-Ang University) ;
  • Lee, Min Won (College of Pharmacy, Chung-Ang University) ;
  • Ko, Jae-Hong (Department of Physiology, College of Medicine, Chung-Ang University) ;
  • Seo, Seong Jun (Department of Dermatology, College of Medicine, Chung-Ang University) ;
  • Bang, Hyoweon (Department of Physiology, College of Medicine, Chung-Ang University)
  • Received : 2012.10.22
  • Accepted : 2012.12.11
  • Published : 2013.02.28
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Abstract

Taxifolin glycoside is a new drug candidate for the treatment of atopic dermatitis (AD). Many drugs cause side effects such as long QT syndrome by blocking the human ether-a-go-go related gene (hERG) $K^+$ channels. To determine whether taxifolin glycoside would block hERG $K^+$ channels, we recorded hERG $K^+$ currents using a whole-cell patch clamp technique. We found that taxifolin glycoside directly blocked hERG $K^+$ current in a concentration-dependent manner ($EC_{50}=9.6{\pm}0.7{\mu}M$). The activation curve of hERG $K^+$ channels was negatively shifted by taxifolin glycoside. In addition, taxifolin glycoside accelerated the activation time constant and reduced the onset of the inactivation time constant. These results suggest that taxifolin glycoside blocks hERG $K^+$ channels that function by facilitating activation and inactivation process.

Keywords

References

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