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胰高血糖素样肽1受体激动的高通量筛选及作用机制研究
引用本文:殷菲,邓小红,景佳佳,郑旭煦,刘建辉. 胰高血糖素样肽1受体激动的高通量筛选及作用机制研究[J]. 中国药学杂志, 2007, 42(1): 24-27
作者姓名:殷菲  邓小红  景佳佳  郑旭煦  刘建辉
作者单位:1. 重庆工商大学,药物化学与化学生物学研究中心,重庆,400067;重庆工商大学,环境与生物工程学院,重庆,400067
2. 重庆工商大学,药物化学与化学生物学研究中心,重庆,400067
基金项目:国家自然科学基金;重庆市科委重点基础项目
摘    要: 目的筛选胰高血糖素样肽1(GLP-1)受体激动剂,并进行初步的作用机制研究。方法建立稳定的GLP-1受体激动剂高通量筛选模型,从天然药物中筛选活性成分;在PC12细胞中验证GLP-1受体激动剂的功能及作用机制。结果经过筛选、鉴定,京尼平苷是一种新的GLP-1受体激动剂,能够通过MAPK信号通路诱导PC12细胞分化,对抗过氧化氢诱导的PC12细胞氧化损伤,提高神经细胞活力。结论京尼平苷具有与GLP-1受体激动剂类似的神经营养和神经保护功能。

关 键 词:胰高血糖素样肽1  激动剂  京尼平苷
文章编号:1001-2494(2007)01-0024-04
收稿时间:2006-11-12;
修稿时间:2006-11-12

Screening of Agonist for Glucagon-Like Peptide-1 Receptor and Its Effect on PC12 Cells
YIN Fei, DENG Xiao-hong, JING Jia-jia, ZHENG Xu-xu, LIU Jian-hui. Screening of Agonist for Glucagon-Like Peptide-1 Receptor and Its Effect on PC12 Cells[J]. Chinese Pharmaceutical Journal, 2007, 42(1): 24-27
Authors:YIN Fei   DENG Xiao-hong   JING Jia-jia   ZHENG Xu-xu   LIU Jian-hui
Affiliation:a.Research Center of Pharmaceutical Chemistry & Chemical Biology,b.College of Enviroment and Bioengineering,Chongqing Technology and Business University,Chongqing 400067,China
Abstract:OBJECTIVE To screen the agonist for glucagon-like peptide-1 receptor,and evaluate its neuronal activity. METHODS Natural products were collected to screen in the stable cell line of GLP-1 receptor ,and the active component was identified in the PC12 cells. RESULTS Geniposide was a novel agonist for GLP-1 receptor,which induced the neuronal differentiation of PC12 cells via mitogen-activated protein kinase pathway,and prevented PC12 cells from oxidative damage induced by hydrogen peroxide. CONCLUSION Geniposide has the similar function as the agonist for GLP-1 receptor,including neurotrophic and neuroprotective effects.
Keywords:glucagon-like peptide-l   agonist   geniposide
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