中国药物警戒 ›› 2018, Vol. 15 ›› Issue (10): 577-581.

• 基础与临床研究 •    下一篇

4-氨基-2-三氟甲基苯基维甲酸酯诱导MGC80-3分化的研究

吴菲1, 沈爱宗1, 张圣雨1, 陈飞虎2*   

  1. 1中国科学技术大学附属第一医院药剂科,安徽 合肥230001;
    2安徽医科大学药学院,安徽 合肥 230032
  • 收稿日期:2018-06-12 修回日期:2018-11-27 出版日期:2018-10-20 发布日期:2018-11-27
  • 通讯作者: 陈飞虎,男,教授,博士生导师,分子药理学。E-mail：cfhchina@sohu.com
  • 作者简介:吴菲,女,硕士,主管药师,临床药学。
  • 基金资助:
    十二五国家“重大新药创制”科技重大专项项目（2011ZX09401-021）：企业创新药物孵化基地建设

Effects of 4-Amino-2-Trifluoromethyl-Phenyl Retinate on the Differentiation of MGC80-3

WU Fei1, SHEN Aizong1, ZHANG Shengyu1, CHEN Feihu2*   

  1. 1Department of Pharmacy, the First Affiliated Hospital of USTC, Anhui Hefei 230001, China;
    2College of Pharmacy, Anhui Medical University, Anhui Hefei 230002, China
  • Received:2018-06-12 Revised:2018-11-27 Online:2018-10-20 Published:2018-11-27

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摘要： 目的 分析了解新型维甲酸类化合物4-氨基-2-三氟甲基苯基维甲酸酯（4-amino-2-trifluoromethyl-phenyl retinate,ATPR）对胃癌细胞株MGC80-3的作用。方法 MGC80-3细胞经ATPR处理后,MTT法研究其抑制增殖能力;倒置相差显微镜下吉姆萨染色观察细胞形状变化;紫外分光光度计法检测细胞分化标志酶ALP、LDH的活性;流式细胞仪监测细胞周期变化情况;RT-PCR检测经ATPR处理后细胞株RARα mRNA的表达变化情况。结果 ATPR能够显著抑制MGC80-3的增殖,且呈浓度依赖性;细胞形态向正常细胞分化;ALP、LDH酶活性减弱;G0/G1期细胞表达量上升,S期减少,细胞周期被抑制在G0/G1期;RARα的表达量增多。结论 ATPR可以抑制MGC80-3细胞的增殖,能够诱导其向正常细胞分化,其作用机制可能与上调RARα mRNA的表达有关。

关键词: 维甲酸, 胃癌, 增殖, 分化

Abstract: Objective To analyze the effects of 4-amino-2-trifluoromethyl phenyl retinate(ATPR) on gastric cancer cell line MGC80-3. Methods Cell proliferation was assessed by MTT assay before and after the treatment with ATPR. The morphologic changes were observed after Giemsa under inverted phase contrast microscope. The activity of enzyme ALP and LDH was detected by ultraviolet spectrophotometer. The cell cycle was analyzed by flow cytometry. RT-PCR was used to analyze the expression of RARα mRNA after the treatment with ATPR. Results ATPR had inhibitory effects on the proliferation ability of MGC80-3. It promoted the growth differentiation. The growth of MGC80-3 cells was inhibited in a dose-dependent manner after the treatment with ATPR. The cell morphology differentiated into normal cells. It can cause the decrease of the activity of ALP and LDH. In addition, the number of G0/G1 phase was increased, and the S phase was decreased, the cell growth was inhibited in G0/G1 phase. The expression of RARα was increased. Conclusion ATPR had inhibitory effects on the proliferation of MGC80-3 cells and could induce its differentiation to normal cells, the mechanism of which might be related to the up-regulation of RARα mRNA.

Key words: retinoic acid, gastric cancer, proliferation, differentiation

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