化工进展

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叶酸偶联N-季铵化壳聚糖的制备及其基因载体性能

宋宇宁,辛梅华,李明春,周盛全   

  1. 华侨大学材料科学与工程学院,环境友好功能材料教育部工程中心 福建厦门 361021
  • 出版日期:2012-11-05 发布日期:2012-11-07

Synthesis and characterization of folate-conjugated quaternized chitosan as a gene delivery vector

SONG Yuning,XIN Meihua,LI Mingchun,ZHOU Shengquan   

  1. School of Material Science and Engineering, Huaqiao University, Engineering Research Center of Environment-Friendly Functional Materials, Ministry of Education, Xiamen 361021, Fujian, China
  • Online:2012-11-05 Published:2012-11-07

摘要: 首先对壳聚糖进行季铵化改性合成N-季铵化壳聚糖(HTCC),再接枝叶酸基团制备了叶酸偶联N-季铵化壳聚糖(FA-HTCC),用FTIR和1H NMR等对产物进行表征,并对其作为基因载体进行研究。结果表明,合成产物具有较好的水溶性,N/P为4的FA-HTCC/DNA复合物粒径为188 nm、Zeta电位为15.4 mV。与PEI和阳离子脂质体相比,FA-HTCC具有更低的细胞毒性和更高的转染效率。

关键词: 壳聚糖, 季铵化, 叶酸, 基因载体

Abstract: N-[(2-hydroxy-3-trimethylammonium) propyl] chitosan chloride (HTCC) was synthesized by quaternisation and the folate group was conjugated on the N-quarternary ammonium chitosan. The target product was characterized by FTIR and 1H NMR. The result showed that both HTCC and FA-HTCC had good water solubility. Particle size and zeta potential were 188 nm and 15.4 mV at N/P ratio of 4. In contrast with other carriers, FA-HTCC had comparatively high transfection efficiency and low cytotoxicity on Hela cells in vitro.

Key words: chitosan, quaternized, folate, gene delivery