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目的:研究叶酸(FA)偶联纳米紫杉醇对卵巢癌的体外治疗效果,并初步探讨其作用机制。方法:共孵育法制备FA偶联纳米紫杉醇,荧光显微镜和流式细胞仪定性和定量测定其对SKOV3细胞的靶向作用,绘制细胞生长曲线;噻唑蓝法、流式细胞术及电子显微镜下观察FA偶联纳米紫杉醇对SKOV3细胞和SKOV3/TAX细胞的体外杀伤效应。结果:(1)FA偶联纳米紫杉醇的粒径为(140.5±10.3)nm,包封率为97%;(2)FA偶联纳米紫杉醇在FA受体(FR)介导下对SKOV3细胞有靶向杀伤作用,并且随时间延长,细胞内药物浓度逐渐增加;(3)FA偶联纳米紫杉醇对SKOV3细胞及SKOV3/TAX细胞的药效显著强于纳米紫杉醇,SKOV3/TAX细胞对FA偶联纳米紫杉醇的耐药指数有下降趋势。结论:FA偶联纳米紫杉醇可能利用FR为作用靶点,将药物主动靶向肿瘤细胞,提高药物在肿瘤细胞内的分布。其抗肿瘤疗效优于传统的紫杉醇。
Objective: To study the effect of folic acid (FA) coupled with paclitaxel on ovarian cancer in vitro and its possible mechanism. METHODS: FA-conjugated nanpaclitaxel was prepared by co-incubation. The targeting effect of FA on SKOV3 cells was determined by fluorescence microscopy and flow cytometry. The cell growth curve was drawn. The growth curves were observed by flow cytometry and electron microscopy In Vitro Cytotoxicity of FA-Coupled Nano-Paclitaxel to SKOV3 and SKOV3 / TAX Cells. Results: (1) The particle size of FA-conjugated nanpaclitaxel was (140.5 ± 10.3) nm and the entrapment efficiency was 97%. (2) FA-conjugated nanpaclitaxel (3) The effect of FA-conjugated nanpaclitaxel on SKOV3 cells and SKOV3 / TAX cells was significantly stronger than that of paclitaxel, and the SKOV3 / TAX cells were positively associated with FA Drug resistance index of nano-paclitaxel has a downward trend. CONCLUSION: FA-conjugated nanpaclitaxel may use FR as a target, actively target drugs to tumor cells and improve the distribution of drugs in tumor cells. Its anti-tumor effect is superior to the traditional paclitaxel.