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Torilin fromTorilis japonica (Houtt.) DC. Blocks hKv1.5 channel current

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Abstract

Torilin was purified fromTorilis 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, IKUR) 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 IC50 value of 2.51±0.34 μM 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 usedependent manner. These results strongly suggest that torilin is a type of open-channel blocker of the hKv 1.5 channel.

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Authors and Affiliations

  1. Department of Pharmacology, Chonbuk National University Medical School, 561-756, Chonju, Korea

    Yong Geun Kwak, Tian-Ze Ma & Sun-Ah Park

  2. College of Pharmacy, Woosuk University, 565-701, Samrye, Korea

    Dae Keun Kim, Hoon Park & Jae Soon Eun

  3. College of Pharmacy, SungKyunKwan University, 440-746, Suwon, Korea

    Young Hoon Jung

  4. Department of Chemistry, Seonam University, 590-711, Namwon, Korea

    Dong-Jin Yoo

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  1. Yong Geun Kwak
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  2. Dae Keun Kim
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  3. Tian-Ze Ma
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  4. Sun-Ah Park
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  5. Hoon Park
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  7. Dong-Jin Yoo
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  8. Jae Soon Eun
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Correspondence to Jae Soon Eun.

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Kwak, Y.G., Kim, D.K., Ma, TZ. et al. Torilin fromTorilis japonica (Houtt.) DC. Blocks hKv1.5 channel current. Arch Pharm Res 29, 834–839 (2006). https://doi.org/10.1007/BF02973902

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  • DOI: https://doi.org/10.1007/BF02973902

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