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.