植物来源的蛋白磷酸酶Cdc25C的新抑制剂(英文)  

New Inhibitors of Dual-specificity Protein Phosphatase Cdc25C from Plants

作　　者：贾锐锐[1] 曾广智[1] 谭宁华[1] 范君婷[1,2] 黄火强[1,2] 嵇长久[1,2] 郝小江[1] 赵勤实[1] 李朝明[1] 

机构地区：[1]中国科学院昆明植物研究所植物化学与西部植物资源持续利用国家重点实验室,云南昆明650204 [2]中国科学院研究生院,北京100049

出　　处：《云南植物研究》2008年第5期617-620,共4页Acta Botanica Yunnanica

基　　金：The National Natural Science Foundation of China(30725048);the Foundation of Chinese Academy of Sciences(West LightProgram)

摘　　要：蛋白磷酸酶Cdc25C能够使有丝分裂激酶CDK1/cyclin B去磷酸化,从而促进细胞周期的进程。已经在一些肿瘤细胞中检测到Cdc25C的过量表达,这使得Cdc25C成为肿瘤治疗中的潜在靶标。通过随机筛选,发现了八个Cdc25C的天然新抑制剂(1-8),其IC50值在1.66～75.07μmol/L之间。肿瘤细胞毒试验结果表明,其中四个化合物(化合物3,4,5,7)对十种肿瘤细胞株显示一定的细胞毒活性,其IC50值皆小于10μg/mL。Protein phosphatase Cdc25C dephosphorylates the mitotic kinase CDK1/cyclin B, and then triggers the cell cycle progression. Overexpression of Cdc25C is detected in some cancer cells, which made it to be a potential target for anti-cancer drugs. Through Cdc25C assay, compounds 1-8 were found to be new natural inhibitors against Cdc25C with IC50s of 1.66-75.07 μmol/L. Moreover, 3, 4, 5 and 7 exhibited cytotoxicities on a panel of ten cancer cell lines with IC50 s below 10 μg/mL.

关 键 词：Cdc25C 磷酸酶 天然抑制剂 细胞周期 肿瘤 

分 类 号：R979.1[医药卫生—药品]