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The Pharmaceutical Society of Korea (대한약학회)
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Torilin from Torilis japonica (Houtt.) DC. Blocks hKv1.5 Channel Current

  • Kwak, Yong-Geun (Department of Pharmacology, Chonbuk National University Medical School) ;
  • Kim, Dae-Keun (College of Pharmacy, Woosuk University) ;
  • Ma, Tian-Ze (Department of Pharmacology, Chonbuk National University Medical School) ;
  • Park, Sun-Ah (Department of Pharmacology, Chonbuk National University Medical School) ;
  • Park, Hoon (College of Pharmacy, Woosuk University) ;
  • Jung, Young-Hoon (College of Pharmacy, SungKyunKwan University) ;
  • Yoo, Dong-Jin (Department of Chemistry, Seonam University) ;
  • Eun, Jae-Soon (College of Pharmacy, Woosuk University)
  • Published : 2006.10.01
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Abstract

Torilin was purified from Torilis japonica (Houtt.) DC., and its effects on a rapidly activating delayed rectifier $K^+$ channel (hKv1.5), cloned from human heart and stably expressed in Ltk cells, as well as the corresponding $K^+$ current (the ultrarapid delayed rectifier, $I_{KUR}$) were assessed in human atrial myocytes. Using the whole cell configuration of the patch-clamp technique, torilin was found to inhibit the hKv1.5 current in time and voltage-dependent manners, with an $IC_50$ value of $2.51{\pm}0.34\;{\mu}M$ at +60 mV. Torilin accelerated the inactivation kinetics of the hKv1.5 channel, and slowed the deactivation kinetics of the hKv1.5 current, resulting in a tail crossover phenomenon. Additionally, torilin inhibited the hKv1.5 current in a use dependent manner. These results strongly suggest that torilin is a type of open-channel blocker of the hKv1.5 channel.

Keywords

References

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