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目的:研究6,8-二-三氟甲基-7-乙酰氧基白杨素(dFMAChR)的抗肺癌作用。方法:MTT比色法、平皿克隆形成法、PI染色流式细胞术(FCM)及DNA断片法检测dFMAChR体外抗肺癌作用;人肺癌(A549)裸鼠异种移植瘤模型治疗实验观察dFMAChR体内抗肺癌作用。Western Blot分析dFMAChR对人肺癌A549细胞pAkt、Caspase3蛋白表达及活性的影响。结果:dFMAChR抑制体外培养A549细胞生长,呈浓度依赖性;dFMAChR能有效诱导A549细胞凋亡;dFMAChR对人肺癌裸鼠异种移植瘤的生长具有抑制作用,呈剂量依赖性;dFMAChR处理的A549细胞pAkt蛋白表达下调,Caspase3蛋白表达上调,呈浓度依赖性。结论:dFMAChR具有抗肺癌作用,其机制可能与抑制pAkt信号传导,激活Caspase3有关。
Objective: To study the anti-lung cancer effect of 6,8-di-trifluoromethyl-7-acetoxy chrysin (dFMAChR). METHODS: MTT colorimetric assay, plate cloning method, PI staining flow cytometry (FCM) and DNA fragmentation method were used to detect the anti-lung cancer effect of dFMAChR in vitro; human lung cancer (A549) xenograft model in nude mice was treated with dFMAChR in vivo against lung cancer. effect. The effect of dFMAChR on the expression and activity of pAkt and Caspase3 protein in human lung cancer A549 cells was analyzed by Western Blot. Results: dFMAChR inhibited the growth of A549 cells in vitro in a concentration-dependent manner; dFMAChR could effectively induce apoptosis in A549 cells; dFMAChR inhibited the growth of human lung cancer xenografts in a dose-dependent manner; dFMAChR treated A549 cells pAkt The protein expression was down-regulated, and the expression of Caspase3 protein was up-regulated in a concentration-dependent manner. Conclusion: dFMAChR has anti-lung cancer effect, and its mechanism may be related to inhibition of pAkt signaling and activation of caspase3.