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肠促胰素"(incretins)是肠道在进餐后分泌的激素,能促进胰岛素的分泌,包括葡萄糖依赖性胰岛素释放肽(GIP)和胰高糖素样肽(GLP-1)。二者可通过葡萄糖依赖的方式促进胰岛素分泌、抑制胰高血糖素分泌以及延缓胃排空、增强饱腹感等作用维持体内血糖的稳定。但由于天然的肠促胰素易被二肽基肽酶Ⅳ(DPP-Ⅳ)降解,半衰期短,无法用于临床治疗。因此,人们致力于研发可以用于糖尿病治疗的DPP-Ⅳ抑制剂和GLP-1类似物。本文就肠促胰素的研究现状及以肠促胰素为基础的降血糖药物的开发情况做一概述。
The incretins, which are hormones secreted by the gut after meal, promote the secretion of insulin, including glucose-dependent insulin-releasing peptide (GIP) and glucagon-like peptide (GLP-1) Glucose-dependent manner can promote insulin secretion, inhibition of glucagon secretion and delay gastric emptying, enhance satiety and other effects of maintaining the stability of the body’s blood sugar.But due to natural incretin is susceptible to dipeptidyl peptidase IV (DPP-IV) degradation, short half-life, can not be used for clinical treatment.Therefore, people are committed to the development of DPP-IV inhibitors and GLP-1 analogues can be used for the treatment of diabetes.In this paper, An overview is given of the development of hypoglycemic agents based on incretin.