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血根碱通过毒蕈碱受体介导的 PKC-CPI-17 通路对分散肠平滑肌细胞的抑制作用。

Inhibitory effect of sanguinarine on PKC-CPI-17 pathway mediating by muscarinic receptors in dispersed intestinal smooth muscle cells.

机构信息

College of Veterinary Medicine, Hunan Agricultural University, Changsha, Hunan 410128, China.

出版信息

Res Vet Sci. 2013 Dec;95(3):1125-33. doi: 10.1016/j.rvsc.2013.07.022. Epub 2013 Aug 29.

DOI:10.1016/j.rvsc.2013.07.022
PMID:23993687
Abstract

This study investigated the inhibitory effects of sanguinarine (SA) on PKC-CPI-17 pathway in rat intestinal smooth muscle cells (ISMC). Previous studies indicate that the inhibitory effects of SA on ISMC contraction are possibly mediated by the Ca(2+) influx. ISMC was treated with 1 μM SA for 24h remarkably inhibited the mRNA expression of m2 and m3 receptors. ISMC treated with 1 or 3 μM SA for 30 min significantly decreased the mRNA expression of PKC-δ, PKC-ε, PKC-η, and CPI-17. 1 μM SA could markedly inhibit carbachol (CCh)-mediated increase PKC-δ, PKC-η, and CPI-17 mRNA but had no effect in PKC-ε.Treatment of ISMC with SA (1 μM, 30 min) caused a decrease in protein expression of PKC-δ. However, the expression of CPI-17 was significantly inhibited in a time-dependent manner. These results demonstrate that the inhibitory effect of SA is coupled with alteration of PKC-mediated signal transduction and intracellular Ca(2+) concentration.

摘要

本研究探讨了血根碱(SA)对大鼠肠平滑肌细胞(ISMC)PKC-CPI-17 通路的抑制作用。先前的研究表明,SA 对 ISMC 收缩的抑制作用可能是通过 Ca2+内流介导的。用 1μM SA 处理 ISMC 24 小时可显著抑制 m2 和 m3 受体的 mRNA 表达。用 1 或 3μM SA 处理 30 分钟可显著降低 PKC-δ、PKC-ε、PKC-η 和 CPI-17 的 mRNA 表达。1μM SA 可显著抑制 CCh 介导的 PKC-δ、PKC-η 和 CPI-17 mRNA 的增加,但对 PKC-ε 无影响。用 SA(1μM,30 分钟)处理 ISMC 可导致 PKC-δ 蛋白表达减少。然而,CPI-17 的表达在时间上受到显著抑制。这些结果表明,SA 的抑制作用与 PKC 介导的信号转导和细胞内 Ca2+浓度的改变有关。

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