摘要
胰高血糖素样肽-1(GLP-1)作为肠促胰素的一种,是治疗Ⅱ型糖尿病的重要靶点之一,具有促进胰岛素分泌、抑制胰高血糖素分泌、延迟胃排空等作用。GLP-1治疗效果明显,用药安全性高,但体内循环时间短,易被清除,因此,需要对GLP-1进行修饰,以达到延长药物作用时间、提高生物利用度、增强用药安全性等目的。对GLP-1及其生理学作用进行了简单介绍,对GLP-1治疗Ⅱ型糖尿病的作用机理及GLP-1类似物的研究现状进行概述,重点比较不同GLP-1类药物经过不同修饰,在药动学、药效学等方面体现的差异,分析GLP-1类药物在临床应用中存在的问题,并针对现有问题讨论未来长效GLP-1类似物的发展方向。
Glucagon like peptide-1(GLP-1)as an incretin is one of the most important targets in the treatment of type 2 diabetes mellitus(T2DM)with the effects of insulin and glucagon secretion and gastric emptying.In spite of advanced therapeutic effects and high safety,it has disadvantages of short circulation time and quick enzymatic digestion.Therefore,long-acting GLP-1 analogues need to be developed to prolong circulation time,improve bioavailability and enhance safety.In this review,GLP-1 and its physiological function were introduced,the mechanism of GLP-1 in T2DM treatment and GLP-1 analogues research were summarized,the differences in pharmacokinetics and pharmacodynamics of GLP-1 analogues were discussed,and the problems of GLP-1 analogues in clinical application were analyzed.The prospective development of long-acting GLP-1 analogues was discussed.
作者
蒋镜清
符玲
谈梦璐
陈圣福
JIANG Jing-qing;FU Ling;TAN Meng-lu;CHEN Sheng-fu(College of Chemical and Biological Engineering,Zhejiang University,Hangzhou 310027,China)
出处
《高校化学工程学报》
EI
CAS
CSCD
北大核心
2020年第6期1327-1338,共12页
Journal of Chemical Engineering of Chinese Universities
基金
国家自然科学基金(21674092,21474085)。
