Acta Chimica Sinica ›› 2007, Vol. 65 ›› Issue (19): 2181-2186. Previous Articles     Next Articles

Original Articles

聚乙二醇嵌段树枝状聚赖氨酸共聚物的合成及其基因载体研究

崔亮1,2, 李洋2, 侯小东3, 宫文娟3, 徐宇虹*,1, 曹阿民*,2   

  1. (1上海交通大学药学院 上海 200237)
    (2中国科学院上海有机化学研究所 上海 200032)
    (3上海交通大学化学化工学院 上海 200237)
  • 投稿日期:2007-04-18 修回日期:2007-05-29 发布日期:2007-10-14
  • 通讯作者: 徐宇虹, 曹阿民

Studies on the Synthesis of Poly(ethylene glycol)-b-dendritic Poly(l-lysine)s and Their Application as Gene Carriers

CUI Liang1; LI Yang2; HOU Xiao-Dong3; GONGWen-Juan3; XU Yu-Hong*,1; CAO A-Min*,2   

  1. (1 School of Pharmacy, Shanghai Jiaotong University, Shanghai 200237)
    (2 Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032)
    (3 School of Chemistry and Chemical Engineering, Shanghai Jiaotong Univer-sity, Shanghai 200237)
  • Received:2007-04-18 Revised:2007-05-29 Published:2007-10-14
  • Contact: XU Yu-Hong; CAO A-Min

New water-soluble diblock poly(ethylene glycol)-b-dendritic poly(l-lysine) with diverse den-dritic generations were molecularly designed and synthesized with well-defined structures. The chemical structures of the diblock cationic copolymers were characterized by 1H NMR. Furthermore, agarose gel electrophoresis and fluorescence titration assays were implemented to evaluate the plasmid DNA (pDNA) binding affinities of the synthesized new block copolymers, indicating higher DNA binding affinities of the diblock copolymers with 4 and 5 generation (PLL). Moreover, the dynamic light scattering was applied to characterize the polyplexes nanoparticles of the cationic carrier/pDNA, indicating the water-soluble PEG-b-dendritic PLL and pDNA could complex to form stable “core-shell” structure nanoparticles, and the biocompatible PEG shell could possibly decrease cytotoxicity of the complexed polyplexes nanoparticle during cell gene transfection. Therefore, these new structural diblock cationic macromolecules may be further developed as potential gene carriers with high efficacy.

Key words: PEG-b-dendritic PLL, cationic gene carrier, agarose gel electrophoresis, fluorescence titration, polyplex nanoparticles