有机化学 ›› 2014, Vol. 34 ›› Issue (3): 589-595.DOI: 10.6023/cjoc201309010 上一篇    下一篇

研究简报

蒽醌-多胺缀合物的合成及生理活性研究

甘莹, 何利华, 张亚宏, 王建红, 赵瑾   

  1. 河南大学 河南省天然药物与免疫工程重点实验室 开封 475004
  • 收稿日期:2013-09-16 修回日期:2013-10-24 发布日期:2013-11-20
  • 通讯作者: 王建红,赵瑾 E-mail:hdky@henu.edu.cn
  • 基金资助:

    国家自然科学基金(No. 21272056);河南省科技厅(Nos. 112300413224,132300410228)资助项目.

Synthesis and Biological Activity of Anthraquinone-polyamine Derivatives

Gan Ying, He Lihua, Zhang Yahong, Wang Jianhong, Zhao Jin   

  1. Key Laboratory of Natural Medicines and Immunotechnology of Henan Province, Henan University, Kaifeng 475004
  • Received:2013-09-16 Revised:2013-10-24 Published:2013-11-20
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21272056) and the Key Scientific and Technological Projects of Henan Province (Nos. 112300413224, 132300410228).

设计合成7个蒽醌-多胺缀合物,化合物结构经1H NMR,APCI-MS和元素分析确认. 利用MTT(噻唑蓝)法测试7个目标化合物对K562,HepG2,MB231,Hela,HCT-116五种肿瘤细胞的体外细胞毒性,结果表明所合成的化合物对测肿瘤细胞均具有明显的生长抑制作用. DNA结合实验表明11b14c以嵌入方式作用于DNA,使鲱鱼精DNA-EB体系的荧光产生猝灭现象.

关键词: 蒽醌衍生物, 合成, 生理活性, DNA嵌入剂

Seven anthraquinone-polyamine derivatives were designed and synthesized. The structures of the synthesized compounds were confirmed by 1H NMR, APCI-MS and elemental analysis. Prelimilary antitumor activity was invesitgated on K562, HepG2, MB231, Hela and HCT-116 cell lines by MTT (thiazolyl blue) assay. The results indicated that the target compounds obviously exhibited antitumor activity against the tested cell lines. Compounds 11b and 14c can intercalate to DNA with intensively fluorescence quenching in herring sperm DNA-EB system.

Key words: nitrogen mustard derivatives, synthesis, biological activity, DNA intercalator