GLP-1受体激动的高通量筛选及作用机制研究
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2007年3月5日
作者:殷菲 (重庆)摘要:目的 筛选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(GLP-1);激动剂;京尼平苷
Screening of Agonist for Glucagon-Like Peptide-1 Receptor and its Effect in PC12 cells
Yin Fei, Zheng Xuxu, Jing Jiajia, Xiao He, Liu Jianhui
(Research Center of Pharmaceutical Chemistry & Chemical Biology, Chongqing Technology and Business University, Chongqing, 400067, China)
ABSTRACT:OBJECTIVE To acquire the agonist for glucagon-like peptide-1 receptor, and check its function. METHODS Natural products are collected to screen in the stable cell line of GLP-1 receptor, and the active component was identified in the PC12 cells. RESULTS Geniposide is a novel agonist for GLP-1 receptor, which induces the neuronal differentiation of PC12 cells via mitogen-activated protein kinase pathway, and prevents PC12 cells from oxidative damage induced by hydrogen peroxide. CONCLUSION Geniposide has the similar function with the agonist for GLP-1 receptor, including neurotrophic and neuroprotective effects. ......
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