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姜黄素类铂(Ⅱ)配合物的合成及其抗肿瘤活性

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

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【作者】 周双生薛璇姜波鲁传华田玉鹏蒋明华

【Author】 Zhou,Shuangsheng,a Xue,Xuana Jiang,Boa Lu,Chuanhuaa Tian,Yupengb,c Jiang,Minghuac (a School of Pharmacy,Anhui College of Traditional Chinese Medicine,Hefei 230031)(b School of Chemistry and Chemical Engineering,Anhui University,Hefei 230039) (c State Key Laboratory of Crystal Materials,Shandong University,Jinan 250100)

【机构】 安徽中医学院药学院安徽大学化学化工学院山东大学晶体材料国家重点实验室

【摘要】 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.

【Abstract】 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 com-plexes’ 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 mgo kg-1 was as potent as cisplatin,its LD50 was 945.6 mgokg-1.

【基金】 国家自然科学基金(No.21071001);安徽省级高校自然科学研究重点项目(No.KJ2010A222);现代中药安徽省工程技术研究中心项目;安徽中医学院自然科学研究重点项目(No.2011zr005A)
  • 【文献出处】 化学学报 ,Acta Chimica Sinica , 编辑部邮箱 ,2011年19期
  • 【分类号】R284;O627.8
  • 【被引频次】7
  • 【下载频次】520
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