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Decursin from Angelica gigas Nakai Blocks hKv1.5 Channel

  • Kwak, Yong-Geun (Department of Pharmacology, Chonbuk National University Medical School, Institute for Medical Research) ;
  • Choi, Bok-Hee (Department of Pharmacology, Chonbuk National University Medical School, Institute for Medical Research) ;
  • Kim, Dae-Keun (College of Pharmacy, Woosuk University) ;
  • Eun, Jae-Soon (College of Pharmacy, Woosuk University)
  • Received : 2010.10.14
  • Accepted : 2010.12.22
  • Published : 2011.01.31

Abstract

Decursin was purified from Angelica gigas Nakai, and its effects on the human Kv1.5 (hKv1.5) currents were recorded in mouse fibroblasts ($Ltk^-$ cells) by whole-cell patch-clamp technique. Decursin inhibited hKv1.5 current in a concentration-dependent manner, with an $IC_{50}$ value of $2.7\;{\mu}M$ at +60 mV. Decursin 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. Also, decursin inhibited the hKv1.5 current in a use-dependent manner. These results strongly suggest that decursin is a kind of open-channel blocker of the hKv1.5 channel.

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