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通过二代和四代聚酰胺-胺树枝状聚合物(G2和G4表示)末端分别修饰苯丙氨酸和色氨酸合成了多种新型聚合物载体,进而考察了其与质粒的组装行为.研究结果显示,Phe-G4和Trp-G4与质粒组装为结构致密的纳米粒子,其中Phe-G4与质粒形成的纳米粒子更加紧密.这一过程是由聚合物载体与质粒间的静电相互作用和结构重排共同驱动的.此外,末端修饰方法显著降低了载体的细胞毒性.细胞转染结果表明,Phe-G4和Trp-G4成功介导质粒pEGFP-CL在COS-7细胞中表达,Phe-G4/pEGFP-CL的转染效率提高到作为阳性对照的脂质体组的4倍以上.因此,Phe-G4载体是一种有应用潜力的新型基因传递系统.
A variety of novel polymeric supports were synthesized by modifying the phenylalanine and tryptophane ends of the second and fourth generation polyamide-amine dendrimers (G2 and G4) respectively, and their assembly behavior with plasmids was also investigated. The results showed that Phe-G4 and Trp-G4 were assembled with the plasmid into densely packed nanoparticles, in which Phe-G4 was more tightly bound to the nanoparticle than the plasmid.This process consisted of the electrostatic interaction between the polymer carrier and the plasmid and Structure rearrangement .In addition, the terminal modification method significantly reduced the cytotoxicity of the vector.Transfection results showed that Phe-G4 and Trp-G4 successfully mediated plasmid pEGFP-CL expression in COS-7 cells, Phe- The transfection efficiency of G4 / pEGFP-CL was increased more than 4-fold as the positive control liposome group.Therefore, the Phe-G4 vector is a novel gene delivery system with potential application.