主客体组装构建环糊精修饰基因微载体的研究  

CONSTRUCTION OF CYCLODEXTRIN-MODIFIED POLYPLEXES via HOST-GUEST ASSEMBLY

作　　者：孙婕衎[1] 常皓[1] 陈丽娜[1] 王幽香[1] 计剑[1] 

机构地区：[1]教育部高分子合成与功能构造重点实验室浙江大学高分子科学与工程学系,杭州310027

出　　处：《高分子学报》2012年第12期1429-1433,共5页Acta Polymerica Sinica

基　　金：国家自然科学基金(基金号50873089;21074110);浙江省科技计划项目(项目号2010C31025);中央高校基本科研业务费专项资金(基金号2011QNA4025)资助项目

摘　　要：合成了二茂铁接枝聚乙烯亚胺(PEI-Fc),利用二茂铁与β-环糊精的主客体嵌套作用制备了环糊精修饰聚乙烯亚胺,核磁测定结果显示,每条PEI-Fc链上通过主客体作用嵌套的CD平均为26个.这种基于弱相互作用力的β-环糊精修饰聚乙烯亚胺能有效诱导DNA分子的缔合,在N/P值达到3以上时,可形成表面为正电荷、粒径为150～250 nm的球形粒子.在含10%胎牛血清的DMEM体外细胞培养基中,由于培养基中的蛋白质能够在粒子表面发生静电吸附,PEI-Fc/CD/DNA基因微载体显示出良好的稳定性.HEK293细胞培养结果显示,以表达绿色荧光蛋白的质粒pEGFP为模型,以N/P值为10的PEI/DNA组装体作为对照,N/P值为3、5和10的PEI-Fc/CD/DNA组装体的转染效率均达到对照组的2～3倍,这种基于主客体组装构建的环糊精修饰基因微载体显著提高了基因转染效率。Ferrocene-grafted polyethyleneimine（PEI-Fc） was synthesized via the reaction of ferrocene carboxaldehyde with branched PEI.The graft level of Fc was about 8.35%.Based on the host-guest interaction between ferrocene and β-cyclodextrin（CD）,CD-modified PEI was successfully prepared.1H-NMR spectrum indicated that there were 26 CD molecules per PEI-Fc chain.CD-modified PEI via host-guest interaction showed effective DNA condensation ability.At N/P ratio above 3,the positive nanoparticles with diameter of about 150-250 nm were formed.At the cell culture medium of DMEM with 10% FBS,PEI-Fc/CD/DNA polyplexes showed excellent stability.It was probably due to the electronic adsorption of proteins on the surface of polyplexes.HEK293 cells culture results indicated that the transfection of PEI-Fc/CD/DNA polyplexes at N/P ratio of 3,5 and 10 was almost 2-3 folds of that of PEI polyplexes at N/P ratio of 10.The CD modified PEI via host-guest interactions significantly improved the transfection efficiency.

关 键 词：非病毒基因载体 主客体组装 聚乙烯亚胺 环糊精 

分 类 号：TQ460.1[化学工程—制药化工] O634[理学—高分子化学]