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外消旋辛因 A 作为瞬时受体电位 melastatin 7 通道阻断剂的作用。

The role of waixenicin A as transient receptor potential melastatin 7 blocker.

机构信息

Division of Longevity and Biofunctional Medicine, Pusan National University School of Korean Medicine, Yangsan, Korea.

出版信息

Basic Clin Pharmacol Toxicol. 2013 Feb;112(2):83-9. doi: 10.1111/j.1742-7843.2012.00929.x. Epub 2012 Sep 25.

Abstract

Transient receptor potential melastatin 7 (TRPM7) plays a role in a number of physiological and pharmacological functions in variety of cells. The aim of this study was to clarify the role for TRPM7 channels and the effect of waixenicin A on the pacemaking activity of interstitial cells of Cajal (ICCs) and on the cell viability of the human gastric and breast adenocarcinoma cell lines, AGS and MCF-7, respectively. Waixenicin A decreased the amplitude of pacemaker potentials in cultured ICC clusters and inhibited TRPM7 currents, but had no effect on Ca(2+) -activated Cl(-) conductance (ANO1). Furthermore, waixenicin A was found to inhibit the growth and survival of AGS and MCF-7 cells. These findings indicate that TRPM7 channel modulates intestinal motility and regulates the pathophysiology of human gastric and breast adenocarcinoma cells. These findings suggest that TRPM7 channel be considered a potential target for the treatment of gut motor disorders and gastric and breast cancer.

摘要

瞬时受体电位 melastatin 7(TRPM7)在多种细胞的许多生理和药理学功能中发挥作用。本研究旨在阐明 TRPM7 通道的作用以及 waixenicin A 对起搏活动的影响 Cajal 间质细胞(ICCs)和对人胃腺癌和乳腺癌细胞系 AGS 和 MCF-7 的细胞活力的影响,分别。Waixenicin A 降低了培养的 ICC 簇中起搏电位的幅度,并抑制了 TRPM7 电流,但对 Ca(2+)-激活的 Cl(-)电导(ANO1)没有影响。此外,发现 waixenicin A 抑制了 AGS 和 MCF-7 细胞的生长和存活。这些发现表明,TRPM7 通道调节肠道运动并调节人类胃腺癌和乳腺癌细胞的病理生理学。这些发现表明,TRPM7 通道可被视为治疗肠道运动障碍和胃癌和乳腺癌的潜在靶点。

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