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姜黄素能有效阻断Kv1.4钾通道。

Curcumin potently blocks Kv1.4 potassium channels.

作者信息

Liu Haiyan, Danthi Sanjay J, Enyeart John J

机构信息

Department of Neuroscience, The Ohio State University, College of Medicine and Public Health, Columbus, OH 43210-1239, USA.

出版信息

Biochem Biophys Res Commun. 2006 Jun 16;344(4):1161-5. doi: 10.1016/j.bbrc.2006.04.020.

Abstract

Curcumin, a major constituent of the spice turmeric, is a nutriceutical compound reported to possess therapeutic properties against a variety of diseases ranging from cancer to cystic fibrosis. In whole-cell patch-clamp experiments on bovine adrenal zona fasciculata (AZF) cells, curcumin reversibly inhibited the Kv1.4K+ current with an IC50 of 4.4 microM and a Hill coefficient of 2.32. Inhibition by curcumin was significantly enhanced by repeated depolarization; however, this agent did not alter the voltage-dependence of steady-state inactivation. Kv1.4 is the first voltage-gated ion channel demonstrated to be inhibited by curcumin. Furthermore, these results identify curcumin as one of the most potent antagonists of these K+ channels identified thus far. It remains to be seen whether any of the therapeutic actions of curcumin might originate with its ability to inhibit Kv1.4 or other voltage-gated K+ channel.

摘要

姜黄素是香料姜黄的主要成分,是一种营养化合物,据报道具有针对从癌症到囊性纤维化等多种疾病的治疗特性。在对牛肾上腺束状带(AZF)细胞进行的全细胞膜片钳实验中,姜黄素可逆性抑制Kv1.4 K+电流,IC50为4.4微摩尔,希尔系数为2.32。重复去极化可显著增强姜黄素的抑制作用;然而,该药物并未改变稳态失活的电压依赖性。Kv1.4是首个被证明受姜黄素抑制的电压门控离子通道。此外,这些结果表明姜黄素是迄今为止所确定的这些K+通道最有效的拮抗剂之一。姜黄素的任何治疗作用是否可能源于其抑制Kv1.4或其他电压门控K+通道的能力,仍有待观察。

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