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以二氢吡唑为先导的新型化合物靶向hTERT 抑制 SMMC-7721的增殖

何旭 黄成 孟晓明 刘新华 李俊

安徽医科大学学报Issue(8):1053-1057,5.
安徽医科大学学报Issue(8):1053-1057,5.

以二氢吡唑为先导的新型化合物靶向hTERT 抑制 SMMC-7721的增殖

Novel compound containing dihydropyrazole moiety inhibits the proliferation of SMMC-7721 by targeting hTERT

何旭 1黄成 2孟晓明 3刘新华 1李俊2

作者信息

  • 1. 安徽医科大学药学院
  • 2. 安徽医科大学肝病研究所
  • 3. 安徽省高校产业共性技术研究院,合肥 230032
  • 折叠

摘要

Abstract

Objective To investigate the inhibitory effect of novel compound containing dihydropyrazole moiety on the proliferation of SMMC-7721 by targeting hTERT melittin. Methods The inhibition rate of proliferation of cells treated with novel compounds was measured by MTT assay. And the novel compounds’ effect on cell cycle was test-ed by flow cytometry cell cycle experiment. Telomerase activity was determined through modified Telomeric Repeat Amplification Protocol (TRAP) assays. The protein expression level of hTERT was observed by Western blot. Re-sults Compared with the heterocyclic compounds, novel compound containing dihydropyrazole moiety had obvious inhibitory effect on the proliferation of cell lines, especially on the human hepatoma cell line SMMC-7721. The re-sult of flow cytometric cell cycle analysis showed that the number of cells in S phase was markedly increased. After the treatment with novel compound containing dihydropyrazole moiety, the results of modified TRAP assays predic-ted that the telomerase activity was inhibited. And the results of western blot showed that the protein expression level of hTERT decreased obviously. Conclusion Novel compound containing dihydropyrazole moiety inhibits the prolif-eration of SMMC-7721 and makes them arrested at S phase. This initial discovery is mainly achieved through the inhibition of telomerase activity by targeting hTERT.

关键词

二氢吡唑/香豆素/人肝癌细胞株 SMMC-7721/增殖抑制/hTERT

Key words

dihydropyrazole/coumarin/human hepatoma cell line SMMC-7721/proliferation inhibition/hTERT

分类

医药卫生

引用本文复制引用

何旭,黄成,孟晓明,刘新华,李俊..以二氢吡唑为先导的新型化合物靶向hTERT 抑制 SMMC-7721的增殖[J].安徽医科大学学报,2015,(8):1053-1057,5.

基金项目

安徽省科技攻关计划项目(编号:1301042212) (编号:1301042212)

安徽医科大学学报

OA北大核心CSTPCD

1000-1492

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