Details

Autor(en) / Beteiligte

• Eun, Jae Soon
• Choi, Bok Hee
• Park, Jeong Ah
• Lee, Ggot Im
• Lee, Taek Yul
• Kim, Dae Keun
• Jung, Young Hoon
• Yoo, Dong Jin
• Kwak, Yong Geun

Titel

Open channel block of hKv1.5 by psoralen from Heracleum moellendorffii Hance

Ist Teil von

• Archives of pharmacal research, 2005-03, Vol.28 (3), p.269-273

Ort / Verlag

Korea (South)

Erscheinungsjahr

2005

Quelle

MEDLINE

Beschreibungen/Notizen

• 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 psoralen on a human Kv1.5 potassium channel (hKv1.5) cloned from human heart and stably expressed in Ltk- cells. We found that psoralen inhibited the hKv1.5 current in a concentration-, use- and voltage-dependent manner with an IC50 value of 180 +/- 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.