journal6 ›› 2008, Vol. 29 ›› Issue (2): 106-111.

• 医学 • 上一篇    下一篇

5,4’-二-正辛烷氧基-7-二氟亚甲基异黄酮抑制人乳腺癌细胞生长和诱导凋亡的作用

  

  1. (1.南华大学附属第一医院,湖南　衡阳 421001；2.南华大学肿瘤研究所,湖南 衡阳 421001)
  • 出版日期:2008-03-25 发布日期:2012-05-25
  • 作者简介:郑芳(1982-)，女，湖南汨罗人，南华大学附属第一医院硕士研究生，主要从事肿瘤内科研究.

Inhibition of Growth and Induction of Apoptosis in Human Breast Cancer Cell Line by 5,4’-Di-n-octoxyl- 7-gem-Difluoromethylene-Genistein  in  Vitro

  1. (1.The first Affiliated Hospital of Nanhua University,Hengyang 421001,Hunan China;2.Cancer Research Institute of Nanhua University,Hengyang 421001,Hunan China)
  • Online:2008-03-25 Published:2012-05-25

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摘要：目的 探讨金雀异黄素（Genistein,Gen）衍生物5,4’-二-正辛烷氧基-7-二氟亚甲基异黄酮（5,4’-Di-n- octoxyl-7-gem-difluoromethylene-genistein，DOdFMG）体外抑制人乳腺癌细胞系MCF-7细胞生长和诱导凋亡作用及机制，以寻找具有开发前景的肿瘤治疗新候选药物.方法 体外培养人乳腺癌细胞系（MCF-7）细胞，分别应用不同浓度的DOdFMG处理人乳腺癌细胞系（MCF-7）细胞，软琼脂克隆形成法测定DOdFMG对体外培养MCF-7细胞的锚定非依赖性增殖及生长作用的影响；PI染色流式细胞计分析（FCM）法检测DOdFMG对MCF-7细胞诱导凋亡影响.western blotting法检测蛋白激酶CK2，NF-KB蛋白表达和活性的变化，初步探讨DOdFMG抗乳腺癌作用的分子机制.结果 DOdFMG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.DOdFMG诱导人MCF-7细胞凋亡.Western Blot分析结果显示：DOdFMG 3.0，10.0，30.0 μmol/L处理人乳腺癌MCF-7细胞24 h后，比较于空白对照组，蛋白激酶CK2的表达下调12.50%，41.50%，67.30%，NF-KB的表达下调20.50%，51.47%，71.93%.DOdFMG 30.0 μmol/L分别处理6，12，24 h后，比较于空白对照组，蛋白激酶CK2的表达下调27.73％，44.8％，65.2％，NF-KB的表达下调20.50%，49.83%，69.93%.这表明DOdFMG以时间－剂量依赖方式引起蛋白激酶CK2、NF-KB下调，与先导化合物Gen比较，DOdFMG更为有效（P<0.05）.结论 DOdFMG显著抑制人乳腺癌细胞系（MCF-7）细胞增殖及生长；DOdFMG可诱导人乳腺癌细胞系（MCF-7）细胞凋亡；抑制蛋白激酶CK2，下调NF-κB的表达可能是DOdFMG诱导凋亡的分子机制之一.

关键词： 乳腺癌, 金雀异黄素, 5, 4&rsquo, -二-正辛烷氧基-7-二氟亚甲基异黄酮, 蛋白激酶CK2

Abstract: PURPOSE  To investigate the effect and mechanism of the Genistein derivative 5,4’-Di-n-octoxyl-7-gem-difluoromethylene-genistein(DOdFMG) 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   Soft ager-colon assay was used to test colon formation inhibitory effect of MCF-7 by DOdFMG.PI stain flow cytometry(FCM) was used to analyse the apoptosis  after being treated with DOdFMG.Western blotting assay was used to detect the effect of DOdFMG on the CK2 and NF-κB protein expression level of breast cells.Results: DOdFMG significantly inhibited proliferation and growth of MCF-7 cells in dose-dependent manner.DOdFMG significantly induced apoptosis. Western-blotting analysis indicated that after exposures to DOdFMG3.0,10.0,30.0μmol/L for 24h,the protein expressions of CK2 were down-regulated by 12.50%,41.50%,67.30%，the protein expressions of NF-κB were down-regulated by 20.50%,51.47%,71.93% respectively in comparison with the control group.After MCF-7 cells were treated with DOdFMG at 30.0 μmol/L for 6,12 and 24 h,the protein expressions of CK2 were down-regulated by 27.73％,44.8％,65.2％，the protein expressions of NF-κB were down-regulated by 20.5%,49.83%,69.93%  respectively in comparison with the control group.These showed that the expressions of CK2，NF-κB were decreased in a time and dose-dependent manner  after treatment with various concentrations of DOdFMG..In comparison with the lead compound Gen,DOdFMG was more effective.CONCLUSION DOdFMG possesses a significant inhibitory effect on the cell proliferation and growth of human breast carcinoma cell(MCF-7) in vitro  DOdFMG significantly induced apoptosis of human breast cancer （MCF-7 ） cell line.The mechanism might be associate
d with down-regulation of ck2 and NF-κB.

Key words: breast cancer, Genistein, 5,4&rsquo, -Di-n-octoxyl-7-gem-Difluoromethylene-genistein, CK2

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