中华医学超声杂志

应用化学 ›› 2010, Vol. 27 ›› Issue (04): 398-403.DOI: 10.3724/SP.J.1095.2010.90334

• 研究论文 • 上一篇    下一篇

N,N-二(8-黄酮甲基)香叶胺类化合物的合成及生理活性

赵瑾1,谢焕许2,刘洪雨2,马红霞2,谢松强3,王超杰1*   

  1. (河南大学1.天然药物与免疫工程重点实验室;2.化学化工学院;3.药学院 开封 475004)
  • 收稿日期:2009-05-08 修回日期:2009-07-22 出版日期:2010-04-10 发布日期:2010-04-10
  • 通讯作者: 王超杰，男，博士，教授; E-mail:wcjsxq@yahoo.com; 研究方向：天然产物和药物化学
  • 基金资助:
    国家自然科学基金资助项目（20872027），河南省科技攻关项目（72102270004）

Synthesis and Cytotoxicity of N,N-Bis(8-flavonmethyl)geranylamine Derivatives

ZHAO Jin1, XIE Huan-Xu2, LIU Hong-Yu2, MA Hong-Xia2, XIE Song-Qiang3, WANG Chao-Jie1*   

  1. (1.Key Laboratory of Natural Medicine and Immune Engineering,Henan University,Kaifeng;
    2.College of Chemistry and Chemical Engineering,Henan University,Kaifeng;
    3.College of Pharmacy,Henan University,Kaifeng 475004)
  • Received:2009-05-08 Revised:2009-07-22 Published:2010-04-10 Online:2010-04-10

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1208

被引次数

1

摘要：

设计合成了4个N,N-二（8-黄酮甲基）香叶胺类化合物，所有目标化合物的结构均经1H NMR、MS和元素分析测试技术确证。采用MTT法考察了目标化合物对K562（白血病细胞）和SMMC7721（肝癌细胞）2种肿瘤细胞的体外抑制活性，结果表明，所测化合物对2种肿瘤细胞都有体外抑制活性，其中N,N-二(3′,4′-二甲氧基-8-黄酮甲基）香叶胺(1c)的活性最好，IC50值分别为5.78和3.85 μmol/L，N,N-二（4′-氟-8-黄酮甲基）香叶胺(1a)和化合物1c对K562（白血病细胞）的体外抑制活性明显优于商品药物美法仑(Melphalan)。以溴化乙锭(EB)为荧光探针测定了化合物1c与鲱魚精DNA有较强的相互作用。

关键词: N,N-二（黄酮甲基）香叶胺, 合成, 生理活性, 荧光探针

Abstract:

Four N,N-bis(8-flavonmethyl)geranylamine derivatives were designed and synthesized. The structures of the synthesized compounds were determined from the results of 1H NMR, MS and elemental analysis. The prelimilary cytotoxicity was evaluated on K562 and SMMC7721 cell lines by MTT assay. The results demonstrated that all compounds possessed antitumor actitity and compound 1c is the best among them with an IC50 value of 5.78 μmol/L or 3.85 μmol/L against K562 or SMMC7721 cell lines, respectively. The in vitro antitumor activities of compounds 1a and 1c against K562 were better than that of the commercial drug Melphalan. The interaction of compound 1c with herring sperm DNA was explored with ethidium bromide(EB) as a fluorescence probe. The result of the study on fluorescence quenching by DNAEB confirms the strong interaction of compound 1c with Herring Sperm DNA.

Key words: N,N-bis(flavonmethyl)geranylamine, synthesis, bioactivity, fluorescence

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