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通过靶向辣椒素受体刺激降钙素基因相关肽释放:一种潜在的胃黏膜保护策略。

Stimulation of calcitonin gene-related peptide release through targeting capsaicin receptor: a potential strategy for gastric mucosal protection.

机构信息

Department of Pharmacology, School of Pharmaceutical Sciences, Central South University, 110 Xiang-Ya Road, Changsha, 410078, China.

出版信息

Dig Dis Sci. 2013 Feb;58(2):320-5. doi: 10.1007/s10620-012-2362-6. Epub 2012 Aug 24.

DOI:10.1007/s10620-012-2362-6
PMID:22918689
Abstract

Calcitonin gene-related peptide (CGRP) is a predominant neurotransmitter from capsaicin-sensitive sensory nerves, which are widely distributed in the gastrointestinal system. These sensory nerves are reported to be involved in the protection of gastric mucosa against damage by various stimuli, and CGRP is a potential mediator in this process. In addition to increase in gastric mucosal blood flow, the beneficial effects of CGRP on gastric mucosa include inhibition of gastric acid secretion, prevention of cellular apoptosis and oxidative injury. The synthesis and release of CGRP is regulated by the capsaicin receptor which is known as transient receptor potential vanilloid subfamily member 1 (TRPV1) and the agonists of TRPV1 have the potential for gastric mucosal protection. So far, multiple TRPV1 agonists, including capsaicin, capsiate, anandamide and rutaecarpine are reported to exert beneficial effects on gastric mucosal injury induced by various stimuli. Therefore, the TRPV1/CGRP pathway represents a novel target for therapeutic intervention in human gastric mucosal injury.

摘要

降钙素基因相关肽(CGRP)是一种主要的神经递质,来源于辣椒素敏感的感觉神经,这些神经在胃肠道中广泛分布。这些感觉神经被报道参与了胃黏膜对各种刺激损伤的保护作用,而 CGRP 是这个过程中的一个潜在介质。除了增加胃黏膜血流外,CGRP 对胃黏膜的有益作用还包括抑制胃酸分泌、防止细胞凋亡和氧化损伤。CGRP 的合成和释放受辣椒素受体(也称为瞬时受体电位香草酸亚型 1(TRPV1))的调节,而 TRPV1 的激动剂具有胃黏膜保护的潜力。到目前为止,多种 TRPV1 激动剂,包括辣椒素、辣椒碱、花生四烯酸酰胺和吴茱萸碱,被报道对各种刺激引起的胃黏膜损伤具有有益作用。因此,TRPV1/CGRP 途径代表了人类胃黏膜损伤治疗干预的一个新靶点。

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