6,8-二-三氟甲基-7-乙酰氧基白杨素的抗肺癌作用

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。

The Antitumor Effect of 6,8-ditrifluoromethy -7-acetoychrysin in Human Lung Cancer

Objective To investigate the therapeutic effect of 6,8ditrifluoromethy-7-acetoychrysin(dFMAChR) in human lung cancer.Methods The antitumor effect of dFMAChR in lung cancer in vitro,were determined by MTT assay,Plate clone-formation method,flow cytometry(FCM) using PI stainin and DNA fragment method.Human lung carcinoma xenograft in nude mouse model was established to investigate the anti-lung cancer effect of dFMAChR in vivo.Effect of dFMAChR on p-Akt,and caspase-3 protein expression of A549 cells was detected by western blotting.Results Assays in vitro showed dFMAChR inhibited the growh of A549 cells,and significantly induced apoptosis in a concentration-dependent.Therapeutic trial with human lung carcinoma xenograft in nude mouse model indicated that dFMAChR significantly inhibited the growth of human lung carcinoma xenografts in Balb/c-nu mice.Western-blotting analysis indicated protein level of p-Akt was increased and expression of Caspase-3 was enhanced after treatment with dFMAChR in a concentration-dependent manner.Conclusion dFMAChR possess therapeutic action in human lung cancer,and its mechanism may be associated with inhibition of p-Akt signaling and activation of Caspase-3.