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KMID : 0043320060290100834
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Archives of Pharmacal Research
2006 Volume.29 No. 10 p.834 ~ p.839
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Torilin from Torilis japonica (Houtt.) DC. Blocks hKv1.5 Channel Current
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Kwak Yong-Geun
Kim Dae-Keun
Ma Tian-Ze
Park Seon-Ah
Park Hoon
Jung Young-Hoon
Yoo Dong-Jin
Eun Jae-Soon
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Abstract
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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, 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 hKv1.5 channel.
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KEYWORD
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hKv1.5 channel blocker, Torilin, Torilis japonica (Houtt.) DC
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