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有机化学
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有机化学 ›› 2005, Vol. 25 ›› Issue (08): 944-948. 上一篇    下一篇

研究论文

大黄素衍生物的合成及细胞毒性研究

陆豫，黄志纾*，谭嘉恒，丁岩，卜宪章
安林坤，马林，符立梧，古练权   

  1. (1中山大学药学院 广州 510080)
    (2中山大学化学与化工学院 广州 510275)
    (3江西中德联合研究院 南昌 330047)
    (4中山大学肿瘤防治中心 广州 510060)
  • 收稿日期:2004-08-05 修回日期:2005-02-28 发布日期:2005-07-30
  • 通讯作者: 黄志纾

Synthesis and Cytotoxicity of Emodin Derivatives

LU Yu,HUANG Zhi-Shu*,TAN Jia-Heng,DING Yan,BU Xian-Zhang
AN Lin-Kun,MA Lin,FU Li-Wu,GU Lian-Quan   

  1. (1 School of Pharmaceutical Science, Sun Yat-Sen University, Guangzhou 510080)
    (2 School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275)
    (3 Jiangxi China-Germany Joint Research Institute, Nanchang 330047)
    (4 Cancer Center, Sun Yat-Sen University, Guangzhou 510060)
  • Received:2004-08-05 Revised:2005-02-28 Published:2005-07-30
  • Contact: HUANG Zhi-Shu

PDF

2466

被引次数

80

以天然大黄素为母体, 经化学修饰得到一系列新的含氮衍生物6～14. 通过1H NMR, IR, MS和元素分析确定了结构. 选择口腔底癌(KB)和乳腺癌(MFC-7)两种人癌细胞株, 采用标准MTT法测定了这类大黄素衍生物的细胞毒性. 研究表明大多数衍生物都有较强的抗癌活性, 其中位置异构体7a和7b的混合物表现出最强的活性, 与母体大黄素相比较, 活性分别提高了174倍(KB)和133倍(MFC-7).

关键词: 大黄素衍生物, 合成, 细胞毒性

A series of new emodin derivatives 6～14 containing nitrogen atoms have been synthesized. Their structures were established by 1H NMR, IR, MS spectra and elemental analyses. The cytotoxicity bioassays of these new emodin derivatives were carried out using the standard MTT method, and most of emodin derivatives showed potent cytotoxicity. The mixture of positional isomers 7a and 7b demonstrated the strongest cytotoxicity activity against the cell line of KB and MCF-7.

Key words: synthesis, emodin derivative, cytotoxicity