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化学学报
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化学学报 ›› 2011, Vol. 69 ›› Issue (19): 2335-2340. 上一篇    下一篇

研究论文

姜黄素类铂(II)配合物的合成及其抗肿瘤活性

周双生*,1，薛璇1，姜波1，鲁传华1，田玉鹏2,3，蒋明华3   

  1. (1安徽中医学院药学院 合肥 230031)
    (2安徽大学化学化工学院 合肥 230039)
    (3山东大学晶体材料国家重点实验室 济南 250100)
  • 投稿日期:2010-11-21 修回日期:2011-04-25 发布日期:2011-06-01
  • 通讯作者: 周双生 E-mail:zshuangsheng@126.com
  • 基金资助:

    二阶/三阶非线性光学效应配合物的设计合成及其应用探索;姜黄素类铂配合物的合成及其抗肿瘤活性研究;姜黄素衍生物的合成及其光学性质研究

Synthesis and Antitumor Activities of Platinum(II) Complexes of Curcumin Analog

Zhou Shuangsheng*,1 Xue Xuan1 Jiang Bo1, Lu Chuanhua1 Tian Yupeng2,3 Jiang Minghua3   

  1. (1 School of Pharmacy, Anhui College of Traditional Chinese Medicine, Hefei 230031)
    (2 School of Chemistry and Chemical Engineering, Anhui University, Hefei 230039)
    (3 State Key Laboratory of Crystal Materials, Shandong University, Jinan 250100)
  • Received:2010-11-21 Revised:2011-04-25 Published:2011-06-01

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1212

被引次数

26

以乙醇为溶剂, 用自制的姜黄素衍生物(L1～L4)和碘亚铂酸钾为原料, 合成得到了4种姜黄素类铂(II)配合物(A～D), 通过FT-IR、1H NMR、MS、差热热重和元素分析对所有目标化合物进行了结构表征. 应用MTT (3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐)法研究了化合物体外对人肺腺癌A549、子宫颈癌HeLa和乳腺癌MCF-7细胞的抗肿瘤活性, 结果表明这些化合物对上述癌细胞均有较强活性|并用抑瘤率测定了人肺腺瘤(A549)细胞的抑制作用, 体内试验也显示铂(II)配合物A具有抗人肺腺癌瘤(A549)作用. 其中剂量为800 mg•kg－1的抗瘤活性与顺铂相当, 它的半数致死量为945.6 mg•kg－1.

关键词: 姜黄素, 铂(II)配合物, 合成, 抗肿瘤活性

Four kinds of platinum(II) complexes of curcumin analog (A～D) were synthesized by self-made curcumin derivatives (L1～L4) and potassium tetraiodoplatinate(II) as the starting material with ethanol as solvent. Their compositions were characterized by FT-IR, 1H NMR, MS, TG-DTA and elemental analysis. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) was used to study the complexes antitumor activity in vitro against human lung adenocarcinoma cancer cell line (A549), human cervix cancer cell line (Hela) and human breast cancer cell line (MCF-7), the results showed that the complexes had strong antitumor activity against these cell lines. Inhibition of human liver tumor of A549 was examined by antitumor rate, complex A showed inhibition activity on transplanting-tumor growth of A549, 800 mg• kg－1 was as potent as cisplatin, its LD50 was 945.6 mg•kg－1.

Key words: curcumin, platinum(II) complex, synthesis, antitumor activity