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Plant Diversity ›› 2008, Vol. 30 ›› Issue (05): 617-620.DOI: 10.3724 SP.J.1143.2008.07295

• 研究论文 • 上一篇    下一篇

植物来源的蛋白磷酸酶Cdc25C 的新抑制剂

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   

  1. 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
  • 收稿日期:2007-12-14 出版日期:2008-10-25 发布日期:2008-10-25

New Inhibitors of Dual-specificity Protein Phosphatase Cdc25C from Plants

JIA Rui-Rui1 , ZENG Guang-Zhi1 , TAN Ning-Hua1, FAN Jun-Ting1 , 2 ,
HUANG Huo-Qiang1 , 2 , JI Chang-Jiu1 , 2 , HAO Xiao-Jiang1 ,
ZHAO Qin-Shi1 , LI Chao-Ming1   

  1. 1 State Key Laboratory of Phytochemistry and Plant Resources in West China , Kunming Institute of Botany , Chinese Academy
    of Sciences, Kunming 650204 , China ; 2 Graduate School of the Chinese Academy of Sciences , Beijing 100049 , China
  • Received:2007-12-14 Online:2008-10-25 Published:2008-10-25

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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。

关键词: Cdc25C, 磷酸酶, 天然抑制剂, 细胞周期, 肿瘤

Abstract: 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 IC50 s 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 10μg/mL.

Key words: Cdc25C

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