顺铂与DMPIBPA合用体外抗肿瘤作用研究  

Study on anti-tumor activity of combined application of cisplatin and DMPIBPA in vitro

作　　者：李佳军[1] 马军[1] 田玉顺[1] 

机构地区：[1]延边大学药学院,吉林延吉133002

出　　处：《药学研究》2016年第3期133-135,共3页Journal of Pharmaceutical Research

基　　金：国家自然科学基金(No.81260226)

摘　　要：目的合成Z-2-(3,5-二甲氧苯基)-3-(4-异丁氧苯基)丙烯腈(DMPIBPA)并初步研究与顺铂(DDP)联合应用时的抗癌活性。方法以3,5二甲氧基苯甲酸为原料合成DMPIBPA,后用DDP、DMPIBPA及DDP+DMPIBPA分别处理人结肠癌细胞(HCT116)及人正常肝细胞(L-02)细胞,其细胞增殖的抑制程度用四唑盐(MTT)比色法测定。结果在HCT116细胞中,100μmol·L^(-1) DMPIBPA(抑制率为35.3%±5.0%)与250μmol·L^(-1) DDP(抑制率为28.9%±1.3%)联合应用时其抑制率为65.4%±2.0%,明显强于单用,而在L-02细胞中仅为36.2%±0.5%。结论联合应用DDP及DMPIBPA时对HCT116细胞有选择性协同增殖抑制活性,而对L-02无作用。Objective To synthesize Z -2 -(3,5 -dimethoxyphenyl -3 -)4 -isobutoxyphenyl)acrylonitrile (DMPIBPA)and preliminarily study the anti -tumor activities of combined application of DMPIBPA with cisplatin(DDP). Methods DMPIBPA was synthesized with 3,5 -dimethoxybenzoic acid as a starting material and HCT116 and L -02 cells were treated with DDP,DMPIBPA and DDP +DMPIBPA,respectively,and the proliferation inhibitory effects were de-termined by MTT assays.Results In HCT116 cells,inhibition ratio of DMPIBPA(100 μmol·L -1 )was 35.3% ±5.0%, and the inhibition ratio of DDP (250 μmol · L -1 ) was 28.9% ±1.3%.When combined use of DMPIBPA (100μmol·L -1 )with DDP(250 μmol·L -1 ),the inhibition ratio was 65.4% ±2.0% in HCT116 cells but was only 36.2%±0.5% in L -02 cells.The growth inhibition activity of combined application of DMPIBPA and DDP significantly stronger than either one compound in HCT116 cells.Conclusion When combined use of DDP and DMPIBPA,it expressed selective and synergistic inhibition effect on HCT116 cells but had not any effect on L -02 cells.

关 键 词：白藜芦醇衍生物 顺铂 联合用药 抗癌活性 四唑盐比色法 

分 类 号：R979.1[医药卫生—药品]