2-苯基苯并[b]呋喃类化合物的Pin1抑制活性研究  

Pin1-Inhibitory Activity of 2-Phenylbenzo[b]furans

作　　者：李云萍[1] 成晓东 戴学新[1] 彭莘媚 贺银菊[1] LI Yunping;CHENG Xiaodong;DAI Xuexin;PENG Xinmei;HE Yinju(Qiannan Normal University for Nationalities,Duyun 558000,China)

机构地区：[1]黔南民族师范学院,贵州都匀558000

出　　处：《生物化工》2023年第1期80-82,86,共4页Biological Chemical Engineering

基　　金：黔南民族师范学院校级项目(qnsy2017018);黔南民族师范学院2016年度校级重点实验室、科研团队与产学研基地项目(Qnsyk201603);2018年黔南民族师范学院学科建设能力提升计划项目(QNSYCXYJD2018005)。

摘　　要：本文选取了8个2-苯基苯并[b]呋喃类化合物,以糜蛋白偶联方法检测化合物对Pin1的抑制能力,在50 μmol/L浓度下8个化合物对Pin1酶均有一定的抑制作用,其中化合物b6、b7的抑制作用显著强于阳性对照胡桃醌,IC50值分别达0.658 μmol/L和0.800 μmol/L。以MTT法检测化合物b6、b7对肝癌细胞SK-Hep-1与SNU-423生长抑制活性,化合物b6的IC50值分别为70.40 μmol/L、90.35 μmol/L,化合物b7的IC50值分别为79.83 μmol/L、57.48 μmol/L。本研究获得一些具有较好Pin1抑制活性的2-苯基苯并[b]呋喃类化合物,可为抗肿瘤先导药物的研究提供参考。Eight 2-phenylbenzo[b]furans are selected and Pin1-inhibitory activity of 2-phenylbenzo[b]furans is detected by chymoprotein coupling method.All the 8 compounds are found to inhibit Pin1 enzyme to some extent at the test concentration(50μmol/L).Compounds b6 and b7 possess higher inhibitive effect than that of the positive control Juglone significantly,and the IC50 values of b6 and b7 are up to 0.658µmol/L and 0.800µmol/L.Further,the antitumor activity of b6 and b7 are evatulated on SK-Hep-1 and SNU-423 cell lines with MTT assay.Compounds b6 and b7 show good inhibitory activity on both SK-Hep-1 and SNU-423 cells,among them b6 show IC50 values of 70.40µmol/L and 90.35µmol/L,and b7 show IC50 values of 79.83µmol/L and 57.48µmol/L.2-Phenylbenzo[b]furans equipped satisfactory Pin1-inhibitory activity are found through our study,which provide some reference for designing new leading compounds with antitumor activity.

关 键 词：2-苯基苯并[b]呋喃 Pin1抑制剂 抗肿瘤 

分 类 号：R730.53[医药卫生—肿瘤]