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  

Screening of Agonist for Glucagon-Like Peptide-1 Receptor and Its Effect on PC12 Cells

作　　者：殷菲[1] 邓小红[1] 景佳佳[1] 郑旭煦[1] 刘建辉[1] 

机构地区：[1]重庆工商大学药物化学与化学生物学研究中心

出　　处：《中国药学杂志》2007年第1期24-27,共4页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(30600813);重庆市科委重点基础项目资助(CSTC;2004BA5015)

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。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.

关 键 词：胰高血糖素样肽1 激动剂 京尼平苷 

分 类 号：R963[医药卫生—微生物与生化药学]