双亲水星形共聚物的合成、表征及其作为转染试剂的评价：星形结构的影响
Synthesis, characterization, and evaluation as transfection reagents of double-hydrophilic star copolymers: effect of star architecture.
作者信息
Georgiou Theoni K, Vamvakaki Maria, Phylactou Leonidas A, Patrickios Costas S
机构信息
Department of Chemistry, University of Cyprus, P.O. Box 20537, 1678 Nicosia, Cyprus, Department of Materials Science and Technology, University of Crete, P.O. Box 2208, 710 03 Heraklion, Crete, Greece.
出版信息
Biomacromolecules. 2005 Nov-Dec;6(6):2990-7. doi: 10.1021/bm050307w.
Five star polymers of the ionizable hydrophilic 2-(dimethylamino)ethyl methacrylate (DMAEMA) and the nonionic hydrophilic methoxy hexa(ethylene glycol) methacrylate (HEGMA) were prepared by group transfer polymerization (GTP) using ethylene glycol dimethacrylate (EGDMA) as coupling agent. In particular, four isomeric star copolymers, one heteroarm, two star block and one statistical star, with 90% mol DMAEMA and 10% mol HEGMA, plus one star homopolymer of DMAEMA with degrees of polymerization of the arms equal to 20 were synthesized. The polymers were characterized in terms of their molar masses (MMs) and compositions using gel permeation chromatography (GPC) and proton nuclear magnetic resonance (1H NMR) spectroscopy, respectively. The hydrodynamic diameters in water indicated some aggregation for all the star polymers except for the statistical copolymer star, while the pK values of the DMAEMA units were around 7 for all star polymers. All the star polymers were evaluated for their ability to transfect human cervical HeLa cancer cells with the modified plasmid pRLSV40 bearing the enhanced green fluorescent protein (EGFP) as the reporter gene. All four star copolymers showed decreased toxicity compared to that of the DMAEMA star homopolymer for the same amounts of star polymer tested. The star block copolymer with outer DMAEMA blocks exhibited the highest overall transfection efficiency, 11%, compared to that of all the star polymers examined in this study. This efficiency was the same as that of the commercially available transfection reagent SuperFect.
以乙二醇二甲基丙烯酸酯（EGDMA）为偶联剂，通过基团转移聚合（GTP）制备了可电离亲水性甲基丙烯酸2-(二甲基氨基)乙酯（DMAEMA）和非离子亲水性甲基丙烯酸甲氧基六（乙二醇）酯（HEGMA）的五星聚合物。特别地，合成了四种异构体星形共聚物、一种杂臂、两种星形嵌段和一种统计星形共聚物，其中DMAEMA的摩尔含量为90%，HEGMA的摩尔含量为10%，外加一种臂聚合度等于20的DMAEMA星形均聚物。分别使用凝胶渗透色谱（GPC）和质子核磁共振（1H NMR）光谱对聚合物的摩尔质量（MMs）和组成进行了表征。水中的流体力学直径表明，除统计共聚物星形外，所有星形聚合物都有一定程度的聚集，而所有星形聚合物中DMAEMA单元的pK值约为7。以携带增强型绿色荧光蛋白（EGFP）作为报告基因的修饰质粒pRLSV40评估了所有星形聚合物转染人宫颈HeLa癌细胞的能力。在测试的相同量的星形聚合物中，所有四种星形共聚物的毒性均低于DMAEMA星形均聚物。与本研究中检测的所有星形聚合物相比，具有外部DMAEMA嵌段的星形嵌段共聚物表现出最高的总体转染效率，为11%。该效率与市售转染试剂SuperFect相同。
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