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林产化学与工业 ›› 2015, Vol. 35 ›› Issue (2): 1-7.doi: 10.3969/j.issn.0253-2417.2015.02.001

• 研究报告 •    下一篇

脱氢枞基苯甲酰腙衍生物与DNA作用及抗癌活性研究

徐武双1, 黄志向1, 高炜琳1, 张洁1, 龙剑英2, 刘庆波2, 费宝丽1   

  1. 1. 南京林业大学 化学工程学院, 江苏 南京 210037;
    2. 南京林业大学 理学院, 江苏 南京 210037
  • 收稿日期:2014-09-01 出版日期:2015-04-25 发布日期:2015-04-24
  • 通讯作者: 费宝丽(1971-),女,黑龙江齐齐哈尔人,副教授,博士,主要从事功能配合物和林产配位化学的研究;E-mail:baolifei@yahoo.com。 E-mail:baolifei@yahoo.com
  • 作者简介:徐武双(1989-),男,江苏苏州人,硕士生,主要从事功能配合物和林产配位化学的研究;E-mail:1030034532@qq.com
  • 基金资助:
    南京林业大学引进高层次留学回国人员科研基金(163030031);江苏省普通高校研究生科研创新计划(CXLX13_517)

DNA Binding and Anticancer Properties of Dehydroabietyl Benzoylhydrazone Derivatives

XU Wu-shuang1, HUANG Zhi-xiang1, GAO Wei-lin1, ZHANG Jie1, LONG Jian-ying2, LIU Qing-bo2, FEI Bao-li1   

  1. 1. College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China;
    2. College of Science, Nanjing Forestry University, Nanjing 210037, China
  • Received:2014-09-01 Online:2015-04-25 Published:2015-04-24

摘要: 以脱氢枞酸为原料,合成了脱氢枞基-2-羟基苯甲酰腙(4)和脱氢枞基-2-羟基-5-溴苯甲酰腙(6),并用IR、元素分析、1H NMR 和MS进行了表征。运用黏度分析、紫外吸收光谱和荧光光谱等方法研究了鲑鱼精DNA与46的相互作用,结果表明, 46是以插入模式与DNA发生作用,且4的结合能力强于6。采用MTT 法探究该类化合物对人体癌细胞的抑制作用,结果表明:在浓度25和50 μmol/L下,46对4种肿瘤细胞HeLa,MCF-7,HL-60和HepG-2都表现出较高的抑制活性,抑制率为73.9%~92.3%,均接近或超过临床上使用的顺铂(抑制率为66.3%~92.7%)。

关键词: 脱氢枞酸, 脱氢枞基苯甲酰腙, DNA, 抗癌活性

Abstract: Dehydroabietyl-2-hydroxy benzoylhydrazone (4) and dehydroabietyl-2-hydroxy-5-bromo benzoylhydrazone (6) were synthesized from dehydroabietic acid and characterized by IR, 1H NMR, MS spectra and elemental analysis . Their interactions with Salmon sperm DNA were investigated by viscosity analysis, UV, and fluorescence spectrometry, etc. The experimental results showed that they were bound to DNA by intercalation and the binding ability of 4 is stronger than that of 6. The anticancer experiments by MTT method indicated that the compounds has high growth inhibitory activities on the selected cancer cells (HeLa, MCF-7, HL-60, and HepG-2) with the inhibitory rates of 73.9%-92.3% at the concentrations of 25 and 50 μmol/L. Their anticancer activities were all close to or greater than that of Cisplatin (66.3%-92.7%)

Key words: dehydroabietic acid, dehydroabietyl benzoylhydrazone, DNA, anticancer

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