GPR41稳定细胞株的建立及受体激动剂筛选

Establishment of GPR41 stable cell line and agonist screening of GPR41 receptor

构建GPR41稳定细胞株,从RNA、蛋白水平验证了GPR41的表达并利用cAMP和钙流检测验证了GPR41的生物活性.实验结果表明,该细胞株可以用于筛选受体激动剂.从海藻来源的黄曲霉中提取到的次级代谢产物用于筛选GPR41的激动剂.实验结果还表明,2-吡喃酮类化合物(37号)在1μmol/L浓度条件下即可具有GPR41受体激动活性.这是首次报道2-吡喃酮类化合物具有GPR41受体激动活性.

In this study,a stable GPR41 receptor cell model was established.The GPR41 expression was detected by RT-PCR and western blot,while the function of GPR41 was confirmed by cAMP and Ca assays.These results have shown that we have successfully established GPR41 cell line which can be used for screening the agonists of the receptor in vitro.GPR41 receptor binding activity was tested by cAMP assay using secondary metabolites extracted from gulf seaweed aflatoxin c-f-3 in Putian Fujian.The results have also shown that the No.37 compound,a new compound belonging to 2-Pyrones,has GPR41 receptor agonist activity with high affinity.This is the first report on 2-Pyrones with GPR41 receptor agonist activity.