新一代降血糖药—肠促胰素

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.

New Hypoglycemic Agents-Incretins

Incretins are gut hormones,which stimulate insulin secretion after meal,including glucose-dependent insulinotropic peptide(GIP)and glucagon-like peptide-1(GLP-1).They can contribute to glucose homeostasis by stimulation of insulin secretion,suppression of glucagon secretion(both in a glucose dependent manner),slowing of gastric emptying,and induction of satiety.However,because they are easily degradated by Dipeptidyl peptidase-Ⅳ(DPP-Ⅳ)and the short biological half-life,incretins are not practical for diabetes therapy.So peoples gone in for researching on DPP-Ⅳ inhibitors and GLP-1 analogues.Author of this article makes an outline of the incretins’ current situation and the development of drug depending on incretins.