7-二氟亚甲基-5-烯丙基黄酮抑制人乳腺癌细胞生长和诱导凋亡的作用

Inhibition of Growth and Induction of Apoptosis in Human Breast Cancer Cell by 7-difluorinmethylene-5-allyl Flavone

目的:探讨白杨素(Chrysin,5,7-二羟基黄酮,ChR)衍生物7-二氟亚甲基-5-烯丙基黄酮(7-difluorinmethylene-5-allyl flavone,DFMeAlChR)在体外抑制人乳腺癌细胞系MCF-7细胞生长和诱导细胞凋亡的作用及机制,以期获得高效、低毒的乳腺癌治疗新型候选药物.方法:应用软琼脂克隆形成法检测不同浓度的DFMeAlChR体外对人乳腺癌细胞系(MCF-7)细胞的锚定非依赖性增殖及生长作用的影响;采用WesternBlot分析不同浓度的DFMeAlChR对人乳腺癌细胞系(MCF-7)细胞蛋白激酶CK2,β-Catenin,NF-KB蛋白表达及活性的影响.结果:DFMeAlChR对体外培养MCF-7细胞具有抑制增殖及生长作用,呈剂量依赖性.Western Blot分析结果表明DFMeAlChR以时间-剂量依赖方式引起蛋白激酶CK2、β-Catenin、NF-KB下调,与先导化合物ChR比较,DFMeAlChR更为有效(P<0.05).图3,参11.

PURPOSE PURPOSE To investigate the effect and mechanism of the Chrysin derivative 7-difluorinmethylene-5-allyl flavone（DFMeAlChR） on the growth and apoptosis of human breast cancer（MCF-7） cells line in vitro.and provide a molecular mechanism of this effect so as to find a new candidate for tumor chemotherapy.METHODS The antitumor effect of DFMeAlChR in human breast cancer in vitro,were determined by Soft ager-colon assay.Effect of DFMeAlChR on the CK2,β-Catenin and NF-κB protein expression of MCF-7 cells was detected by western blotting.Results： DFMeAlChR significantlu inhibited proliferation and growh of MCF-7 cells in dose-dependent manner.Western-blotting analysis showed that the expressions of CK2,β-Catenin,NF-κB were decreased in a time and dose-dependent manner after treatment with various concentrations of DFMeAlChR.In comparison with the lead compound Gen,DFMeAlChRwas more effective.3tabs.,11refs.