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.
出处
《化学学报》
SCIE
CAS
CSCD
北大核心
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)