肿瘤靶向性聚酰胺-胺型树枝状高分子基因载体的合成及性能研究  

Synthesis and Characterization of Polyamidoamine Dendrimers Conjugating Transferrin as Tumor-targeted Gene Carriers

作　　者：石楠[1,2] 张悦[1] 王燕铭[1] 

机构地区：[1]南开大学药学院,天津300071 [2]南开大学化学科学学院,天津300071

出　　处：《南开大学学报（自然科学版）》2012年第6期7-11,共5页Acta Scientiarum Naturalium Universitatis Nankaiensis

基　　金：国家自然科学基金(50803029)

摘　　要：通过二硫键可逆地将转铁蛋白偶联在以季戊四醇衍生物为核的第5代聚酰胺-胺型树枝状大分子(G5PDPAMAM)载体表面上,合成出肿瘤靶向性基因载体G5PDPAMAM-dsTf.系统研究了该载体介导绿色荧光蛋白质粒pEFGP-C1转染不同细胞的性能.结果表明,相比于G5PD PAMAM对癌细胞MCF-7和HepG2的转染效率,G5PDPAMAM-dsTf的转染性能均有不同程度的提高,显示出较好的肿瘤靶向性.同时,游离转铁蛋白的拮抗实验也证明了G5PD PAMAM-dsTf可以通过癌细胞表面的转铁蛋白受体TFR介导进入细胞.In an attempt to investigate the effect of transferrin conjugation on the transfection ability of the G5 PD PAMAM/DNA complexes,a tumor-targeted gene carriers,indicated as G5 PD PAMAM-Tf was synthesized by conjugating transferrin via reversible disulfide linkage on PAMAM surface.The important parameters for the physico-chemical properties of this delivery system were investigated and the transfection efficiencies of G5 PD PAMAM-Tf were also evaluated in different cell lines.The results showed that transferrin modification could enhance the delivery of pEGFP-C1 into tumor cells MCF-7 and HepG2.Meanwhile,the addition of free transferrin could significantly decrease the transfection efficiencies of G5 PD PAMAM-Tf in tumor cells,which indicated that the cellular uptake of such vectors is mainly based on transferrin receptor-mediated endocytosis.

关 键 词：聚酰胺-胺型(PAMAM)高分子 非病毒基因载体 转铁蛋白 肿瘤靶向性 

分 类 号：Q819[生物学—生物工程]