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Open Channel Block of hKv1.5 by Psoralen from Heracleum moellendorffii Hance

Eun Jae Soon    (College of Pharmacy, Woosuk University   ); Cho Bok Hee    (Department of Pharmacology, Chonbuk National University Medical School   ); Park Jeong Ah    (Department of Pharmacology, Chonbuk National University Medical School   ); Lee Ggot Im    (Department of Pharmacology, Chonbuk National University Medical School   ); Lee Taek Yul    (College of Pharmacy, Woosuk University   ); Kim Dae Keun    (College of Pharmacy, Woosuk University   ); Jung Young Hoon    (College of Pharmacy, Woosuk University   ); Yoo Dong Jin    (Department of Chemistry, Seonam University   ); Kwak Yong Geun    (Department of Pharmacology, Chonbuk National University Medical School  );
  • 초록

    A furocoumarin derivative, psoralen (7H-furo[3,2-g][1]benzopyran-7-one), was isolated from the n-hexane fraction of Heracleum moellendorffii Hance. We examined the effects of psor-alen on a human Kv1.5 potassium channel (hKv1.5) cloned from human heart and stably expressed in Uk- cells. We found that psoralen inhibited the hKv1.5 current in a concentration-, use- and voltage-dependent manner with an IC $_{50}$ value of 180 $\pm$ 21 nM at +60 mV. Psoralen accelerated the inactivation kinetics of the hKv1.5 channel, and it slowed the deactivation kinetics of the hKv1.5 current resulting in a tail crossover phenomenon. These results indicate that psoralen acts on the hKv1.5 channel as an open channel blocker. Furthermore, psoralen prolonged the action potential duration of rat atrial muscles in a dose-dependent manner. Taken together, the present results strongly suggest that psoralen may be an ideal antiarrhythmic drug for atrial fibrillation.

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  • 이 논문을 인용한 문헌 (4)

    1. 2006. "" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, 29(10): 834~839     
    2. 2006. "" The journal of applied pharmacology : the official journal of the Korean Society of Applied Pharmacology, 14(2): 102~105     
    3. 2007. "" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, 30(2): 155~160     
    4. 2011. "" Biomolecules & therapeutics, 19(1): 33~37     

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