Torilin from Torilis japonica (Houtt.) DC. blocks hKv1.5 channel current

Geun Kwak Yong; Keun Kim Dae; Tian Ze Ma; Sun Ah Park; Hoon Park; Hoon Jung Young; Dong Jin Yoo; Soon Eun Jae

doi:10.1007/BF02973902

Torilin from Torilis japonica (Houtt.) DC. blocks hKv1.5 channel current

Geun Kwak Yong
, Keun Kim Dae
, Tian Ze Ma
, Sun Ah Park
, Hoon Park
, Hoon Jung Young
, Dong Jin Yoo
, Soon Eun Jae^*

^*Corresponding author for this work

Department of Medicine

Research output: Contribution to journal › Journal article › peer-review

12 Scopus citations

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 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 use-dependent manner. These results strongly suggest that torilin is a type of open-channel blocker of the hKv1.5 channel.

Original language	English
Pages (from-to)	834-839
Number of pages	6
Journal	Archives of Pharmacal Research
Volume	29
Issue number	10
DOIs	https://doi.org/10.1007/BF02973902
State	Published - 2006.10.31

Keywords

hKv1.5 channel blocker
Torilin
Torilis japonica (Houtt.) DC

Quacquarelli Symonds(QS) Subject Topics

Medicine
Engineering - Petroleum
Pharmacy & Pharmacology
Chemistry

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10.1007/BF02973902

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@article{5eb3aae90d4246ee8ca4fd830da1a47f,

title = "Torilin from Torilis japonica (Houtt.) DC. blocks hKv1.5 channel current",

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 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 use-dependent manner. These results strongly suggest that torilin is a type of open-channel blocker of the hKv1.5 channel.",

keywords = "hKv1.5 channel blocker, Torilin, Torilis japonica (Houtt.) DC",

author = "Yong, \{Geun Kwak\} and Dae, \{Keun Kim\} and Ma, \{Tian Ze\} and Park, \{Sun Ah\} and Hoon Park and Young, \{Hoon Jung\} and Yoo, \{Dong Jin\} and Jae, \{Soon Eun\}",

year = "2006",

month = oct,

day = "31",

doi = "10.1007/BF02973902",

language = "English",

volume = "29",

pages = "834--839",

journal = "Archives of Pharmacal Research",

issn = "0253-6269",

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TY - JOUR

T1 - Torilin from Torilis japonica (Houtt.) DC. blocks hKv1.5 channel current

AU - Yong, Geun Kwak

AU - Dae, Keun Kim

AU - Ma, Tian Ze

AU - Park, Sun Ah

AU - Park, Hoon

AU - Young, Hoon Jung

AU - Yoo, Dong Jin

AU - Jae, Soon Eun

PY - 2006/10/31

Y1 - 2006/10/31

N2 - 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 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 use-dependent manner. These results strongly suggest that torilin is a type of open-channel blocker of the hKv1.5 channel.

AB - 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 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 use-dependent manner. These results strongly suggest that torilin is a type of open-channel blocker of the hKv1.5 channel.

KW - hKv1.5 channel blocker

KW - Torilin

KW - Torilis japonica (Houtt.) DC

UR - https://www.scopus.com/pages/publications/33751311984

U2 - 10.1007/BF02973902

DO - 10.1007/BF02973902

M3 - Journal article

C2 - 17121176

AN - SCOPUS:33751311984

SN - 0253-6269

VL - 29

SP - 834

EP - 839

JO - Archives of Pharmacal Research

JF - Archives of Pharmacal Research

IS - 10

ER -

Torilin from Torilis japonica (Houtt.) DC. blocks hKv1.5 channel current

Abstract

Keywords

Quacquarelli Symonds(QS) Subject Topics

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