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目的:检测Bmi1(B lymphoma Mo-MLV insertion region 1)小分子化学抑制剂PTC-209对人舌鳞癌细胞中Bmi1表达的抑制作用,并探讨其对体外人舌鳞癌细胞生物表型的影响。方法:对人舌鳞癌细胞系Cal27予以PTC-209处理,通过蛋白质免疫印迹、实时定量逆转录聚合酶链反应检测PTC-209干预后细胞内Bmi1的表达变化;通过MTT、Transwell、划痕试验等分析PTC-209处理对人舌鳞癌细胞增殖、迁移和侵袭的影响;应用克隆形成、肿瘤球培养、流式分选等实验分析PTC-209对人舌鳞癌细胞系中肿瘤干细胞亚群的影响。结果:PTC-209能显著下调人舌鳞癌细胞中Bmi1的表达,并具有浓度和时间依赖效应(P<0.05);PTC-209体外干预可明显抑制细胞增殖、侵袭和迁移能力,增强细胞对顺铂和5-FU的药物敏感性;PTC-209能显著降低细胞克隆形成率、肿瘤球形成以及ALDH+亚群细胞比例。结论:PTC-209能在体外抑制人舌鳞癌细胞中Bmi1的表达,具有抑制细胞增殖、侵袭迁移和降低肿瘤干细胞亚群比例等抗肿瘤效应。
OBJECTIVE: To detect the inhibitory effect of small molecule chemical inhibitor Bmi1 on the expression of Bmi1 in human tongue squamous cell carcinoma and to investigate its effect on the biological phenotype of human tongue squamous cell carcinoma . Methods: Human tongue squamous cell carcinoma cell line Cal27 was treated with PTC-209. The protein expression of Bmi1 was detected by real-time quantitative reverse transcription-polymerase chain reaction (RT-PCR) after transfection with PTC-209. 209 cells were treated with PTC-209 to study the effect of PTC-209 on the proliferation, migration and invasion of human tongue squamous cell carcinoma cells. The effects of PTC-209 on the proliferation, migration and invasion of human tongue squamous carcinoma cells were analyzed by clonal formation, tumor ball culture and flow cytometry. Impact. Results: PTC-209 significantly down-regulated the expression of Bmi1 in human tongue squamous cell carcinoma cells in a concentration-and time-dependent manner (P <0.05). PTC-209 in vitro could significantly inhibit cell proliferation, invasion and migration, Cisplatin and 5-FU drug sensitivity; PTC-209 can significantly reduce the rate of cell colony formation, tumor ball formation and ALDH + subpopulation cell ratio. Conclusion: PTC-209 can inhibit the expression of Bmi1 in human tongue squamous carcinoma cells in vitro, and has the antitumor effects of inhibiting cell proliferation, invasion and migration and reducing the proportion of tumor stem cell subsets.