GLP-1受體激動(dòng)的高通量篩選及作用機(jī)制研究
http://www.www.srpcoatings.com
2007年3月5日
作者:殷菲 (重慶)摘要:目的 篩選GLP-1受體激動(dòng)劑,并進(jìn)行初步的作用機(jī)制研究。方法 建立穩(wěn)定的GLP-1受體激動(dòng)劑高通量篩選模型,從天然藥物中篩選活性成分;在PC12細(xì)胞中驗(yàn)證GLP-1受體激動(dòng)劑的功能及作用機(jī)制。結(jié)果 經(jīng)過(guò)篩選、鑒定,京尼平苷是一種新的GLP-1受體激動(dòng)劑,能夠通過(guò)MAPK信號(hào)通路誘導(dǎo)PC12細(xì)胞分化,對(duì)抗過(guò)氧化氫誘導(dǎo)的PC12細(xì)胞氧化損傷,提高神經(jīng)細(xì)胞活力。結(jié)論 京尼平苷具有與GLP-1受體激動(dòng)劑類似的神經(jīng)營(yíng)養(yǎng)和神經(jīng)保護(hù)功能。
關(guān)鍵詞:胰高血糖素樣肽1(GLP-1);激動(dòng)劑;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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