胰高血糖素样肽1与糖尿病的治疗

中国临床药理学与治疗学 ›› 2008, Vol. 13 ›› Issue (11): 1298-1303.

胰高血糖素样肽1与糖尿病的治疗

卢守四¹, 俞蕴莉¹, 刘晓东¹, 杨永革²

¹中国药科大学药物代谢动力学重点实验室, 南京 210009, 江苏;
²淇县人民医院, 鹤壁 456750, 河南

收稿日期:2008-09-22 修回日期:2008-11-12 出版日期:2008-11-26 发布日期:2020-10-14
通讯作者: 刘晓东,男, 教授, 博士生导师, 研究方向:创新药物的药代动力学, 药物转运与血脑屏障, 中药及天然产物的药物代谢动力学。Tel:025-83271006 E-mail: xdliu@cpu.edu.cn
作者简介:卢守四, 男, 硕士研究生, 主管药师, 研究方向:药物代谢动力学。Tel:025-8327-1006 E-mail: lss3965388@163.com
基金资助:
国家自然科学基金(30873123)

Effect of glucagon-like peptide-1 for the treatment of diabetes mellitus

LU Shou-si¹, YU Yun-li¹, LIU Xiao-dong¹, YANG Yong-ge²

¹Key Lab of Drug Metabolism &Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Jiangsu, China;
²Qixian People’s Hospital, Hebi 456750, Henan, China

Received:2008-09-22 Revised:2008-11-12 Online:2008-11-26 Published:2020-10-14

摘要/Abstract

摘要： 胰高血糖素样肽1(glucagon-like peptide-1,GLP-1) 是由肠道L 细胞分泌的一种重要的肠促胰岛素激素, 其在体内的主要生理作用有刺激胰岛素的分泌和释放、抑制胰高血糖素的分泌、促进胰腺β 细胞的增殖并抑制其凋亡、抑制胃的排空、促进饱食感的产生等。GLP-1 对糖尿病和肥胖具有很好的治疗前景。由于GLP-1 在体内很快被二肽酰基肽酶Ⅳ降解, 血浆半衰期很短, 因而限制了其临床应用。现已发现了促进GLP-1 分泌的物质, 开发了多种GLP-1 的衍生物和二肽酰基肽酶Ⅳ抑制剂, 为开发新型糖尿病治疗药物开辟了新的天地。

关键词: 胰高血糖素样肽-1, 糖尿病, 衍生物

Abstract: Glucagon-like peptide-1(GLP-1) is one of the key incretins secreted by L-cell in intestine. The bioactivities of GLP-1 in vivo includes the enhancement of glucose-dependent insulin secretion and insulin dilivery, suppression of glucagon secretion, promotion of β-cell proliferation and differentiation, inhibition of gastric emptying and appetite. Studies demonstrated that GLP-1 might be used as a new drug for the treatment of diabetes mellitus and obesity in future. However, GLP-1 is quickly degradated by DPP-IV in vivo and its plasma half-life is short, thus the studies of DPP-IV inhibitors are another aspect for durg development. At present, several GLP-1 derivates and DPP-Ⅳ inhibitors may have important application perspective as new therapeutic agents in the treatment of diabetes mellitus and obesity.

Key words: glucagon-like peptide-1, diabetes mellitus, derivate

中图分类号:

R587.1

卢守四, 俞蕴莉, 刘晓东, 杨永革. 胰高血糖素样肽1与糖尿病的治疗[J]. 中国临床药理学与治疗学, 2008, 13(11): 1298-1303.

LU Shou-si, YU Yun-li, LIU Xiao-dong, YANG Yong-ge. Effect of glucagon-like peptide-1 for the treatment of diabetes mellitus[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2008, 13(11): 1298-1303.

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