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

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.