Zhao Ming-Hong, Yuan Lin, Meng Ling-Yun, Qiu Jian-Ling, Wang Chun-Bin
Department of Oncology, Jianhu People's Hospital, Yancheng, Jiangsu 224700, P.R. China.
Department of Oncology, Yancheng Third People's Hospital, Yancheng, Jiangsu 224001, P.R. China.
Exp Ther Med. 2017 Dec;14(6):5503-5508. doi: 10.3892/etm.2017.5230. Epub 2017 Sep 29.
In the present study, quercetin (QUR)-loaded mixed micelles (QUR-M) were prepared with the aim of improving the physicochemical and anticancer efficacy of QUR in lung cancer cells. The mixed micelles comprised tocopheryl polyethylene glycol 1000 succinate (TPGS) and a 1,2-distearoyl--glycero-3-phosphatidylethanolamine derivative of polyethylene glycol. The nanosized QUR-M exhibited a pH-responsive and controlled release of QUR that is likely to be beneficial in cancer treatment. The results of an MTT assay clearly demonstrated that the anticancer effect of QUR-M in A549 cancer cells was stronger compared with that of free QUR at 24 and 48 h time points. The half-maximal inhibitory concentrations of QUR and QUR-M were observed to be 12.45 and 6.42 µg/ml, respectively. When stained with Hoechst 33342 and observed using a confocal laser scanning microscope, A549 cells treated with QUR-M exhibited severe chromatin condensation and apoptotic body formation of the nuclei. Overall, high intracellular uptake, sustained drug release and the presence of TPGS in the mixed micelles may result in an increased inhibitory effect against cell proliferation and improved therapeutic efficacy in lung cancers.
在本研究中，制备了载有槲皮素（QUR）的混合胶束（QUR-M），目的是改善QUR在肺癌细胞中的物理化学性质和抗癌功效。混合胶束由生育酚聚乙二醇1000琥珀酸酯（TPGS）和聚乙二醇的1,2-二硬脂酰-sn-甘油-3-磷脂酰乙醇胺衍生物组成。纳米尺寸的QUR-M表现出pH响应性和QUR的控释，这可能对癌症治疗有益。MTT试验结果清楚地表明，在24小时和48小时时间点，QUR-M对A549癌细胞的抗癌作用比游离QUR更强。观察到QUR和QUR-M的半数最大抑制浓度分别为12.45和6.42μg/ml。用Hoechst 33342染色并使用共聚焦激光扫描显微镜观察时，用QUR-M处理的A549细胞表现出严重的染色质浓缩和细胞核凋亡小体形成。总体而言，混合胶束中高细胞内摄取、持续药物释放以及TPGS的存在可能导致对细胞增殖的抑制作用增强，并提高肺癌的治疗效果。
