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利用转铁蛋白受体介导的内吞作用,使转铁蛋白-阿霉素复合物(Tf-DOX)靶向作用于肿瘤细胞具有深远意义.文章利用荧光光谱确定了阿霉素对转铁蛋白具有荧光猝灭作用,且为静态猝灭.利用激光共聚焦显微镜观察到Tf-DOX可以靶向进入活的人肝癌细胞(HepG2)内,且5h时位于细胞质,24h时DOX解离进入细胞核.而同样条件,单独阿霉素5h已进入细胞核.利用流式细胞仪法检测了Tf-DOX进入细胞的转运机理,结果表明Tf-DOX是通过网格蛋白(Clathrin)介导、转铁蛋白受体决定的内吞机制进入细胞,具有温度、能量依赖性.体外培养条件下,利用MTT比色法检测Tf-DOX对HepG2细胞活力的影响,结果表明转铁蛋白-阿霉素体系保持较好的活性,相对单独阿霉素对细胞的杀伤力较强.这些结果表明转铁蛋白-阿霉素复合物具有明显的生物效应和潜在的生物医药价值.
Using transferrin receptor-mediated endocytosis, targeting transferrin-doxorubicin complex (Tf-DOX) to tumor cells is of far-reaching significance.In this paper, the fluorescence spectra of doxorubicin The protein was quenched by fluorescence and quenched statically.Using confocal laser scanning microscopy, Tf-DOX could be targeted into HepG2 cells and located in the cytoplasm at 5h, and dissociated into the nucleus at 24h .In the same condition, doxorubicin alone entered into the nucleus 5h.The flow cytometry was used to detect the transport mechanism of Tf-DOX into cells, the results showed that Tf-DOX was mediated by Clathrin, Receptor endocytosis mechanism into the cells, with temperature, energy dependence.In vitro culture conditions, the use of MTT colorimetric assay Tf-DOX HepG2 cell viability, the results show that the transferrin - doxorubicin system to maintain more than Good activity, relative to single doxorubicin cytotoxicity stronger.These results show that the transferrin - doxorubicin complex has obvious biological effects and potential biomedical value.