4-氨基-2-三氟甲基苯基维甲酸酯诱导MGC80-3分化的研究  

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

作　　者：吴菲[1] 沈爱宗 张圣雨 陈飞虎[2] WU Fei;SHEN Aizong;ZHANG Shengyu;CHEN Feihu(Department of Pharmacy,the First Affiliated Hospital of USTC,Anhui Hefei 230001,China;College of Pharmacy,Anhui Medical University,Anhui Hefei 230002,China)

机构地区：[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

出　　处：《中国药物警戒》2018年第10期577-581,共5页Chinese Journal of Pharmacovigilance

基　　金：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

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 reti nate,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RARαm RNA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RARαm RNA的表达有关。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.

关 键 词：维甲酸 胃癌 增殖 分化 

分 类 号：R965[医药卫生—药理学]