常见肝癌细胞系的转铁蛋白受体表达差异分析及主动靶向载体效率比较

转铁蛋白受体1(transferrin receptor 1,TfR1)可介导细胞内吞过程，从而摄取与之特异结合的纳米颗粒，因此成为许多主动靶向型纳米载体的靶点。研究表明，肝癌细胞存在TfR1高表达现象，可作为肿瘤治疗纳米药物递送系统的关键性靶点。体外评价是TfR1靶向纳米载体的重要研究环节，然而肝癌细胞模型种类繁多，其TfR1表达水平可能存在一定差异。选择了几种常见的肝癌细胞系，包括HepG2、Hep3B、MHCC97-H以及Huh-1,分别从mRNA水平以及蛋白水平测定了细胞系TfR1的表达情况，考察了转铁蛋白(Tf)以及转铁蛋白核酸适配体(transferrin nucleic acid aptamer, Tf-APT)对不同细胞的亲和效率。同时，制备了包载紫杉醇的TfR1靶向脂质体，并考察其对不同细胞系的细胞生长抑制作用。结果表明，4种肝癌细胞系在mRNA水平以及蛋白水平均存在TfR1的表达差异；同时，体外抗肿瘤结果显示，不同肝癌细胞系对紫杉醇-TfR1靶向脂质体的敏感性也存在显著不同。

Expression of transferrin receptor in hepatocellular carcinoma cell lines and comparison of the efficiency of targeting drug carrier

Transferrin receptor 1 (TfR1) can mediate cell endocytosis and thus absorb nanoparticles that specifically bind to it, so it has become the target of many active targeted nanoparticles. Studies have shown that hepatoma cells have high expression of TfR1, which can be used as a key target for tumor therapy nano-drug delivery system. In vitro evaluation is an important part of TfR1 targeting nano-carriers. However, there are many kinds of liver cancer cell models, and there may be some differences in their TfR1 expression levels. In this study, some common hepatoma cell lines, including HepG2, Hep3B, MHCC97-H and Huh-1, were selected to determine the expression of TfR1 at mRNA level and protein level. The affinity efficiency of transferrin (Tf) and transferrin nucleic acid aptamer (Tf-APT) to different cells were also investigated. Paclitaxel-loaded TfR1 targeted liposomes were prepared and their inhibitory effects on cell growth of different cell lines were investigated. The results showed that there were differences in the expression of TfR1 in five hepatoma cell lines at mRNA level and protein level, as well as the sensitivity to paclitaxel-TfR1 targeted liposomes.