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

作　　者：周双生[1] 薛璇[1] 姜波[1] 鲁传华[1] 田玉鹏[2,3] 蒋明华[3] 

机构地区：[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

出　　处：《化学学报》2011年第19期2335-2340,共6页Acta Chimica Sinica

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)

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.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.

关 键 词：姜黄素 铂(Ⅱ)配合物 合成 抗肿瘤活性 

分 类 号：R284[医药卫生—中药学] O627.8[医药卫生—中医学]