Choi Y H, Liu F, Kim J S, Choi Y K, Park J S, Kim S W
Department of Chemistry, Seoul National University, South Korea.
J Control Release. 1998 Jun;54(1):39-48. doi: 10.1016/s0168-3659(97)00174-0.
A new series of gene carriers, polyethylene glycol (PEG)-grafted poly-L-lysine (PLL, mol. wt. = 25000) with three different PEG-grafted ratios (5, 10 and 25 mole%, which means 5, 10 and 25% of epsilon-amino group of PLL was modified by PEG), was synthesized. These new gene carriers, named comb-shaped PEG-g-PLL copolymer, showed a 5- to 30-fold increase in transfection efficiency compared to PLL alone on a human carcinoma cell line. It is likely that Hep G2 cells were transfected by plasmid DNA/PEG-g-PLL complexes through an endocytosis mechanism due to the fact that chloroquine increased transfection efficiency. Although Lipofectin, a cationic lipid formulation, showed slightly higher transfection efficiency than PEG-g-PLL in Hep G2 cells, our designed PEG-g-PLL demonstrated lower cytotoxicity, early gene expression and maintenance of gene expression for up to 96 h.
合成了一系列新的基因载体，即聚乙二醇（PEG）接枝的聚-L-赖氨酸（PLL，分子量 = 25000），其具有三种不同的PEG接枝率（5、10和25摩尔％，这意味着PLL的ε-氨基的5、10和25％被PEG修饰）。这些新的基因载体，称为梳状PEG-g-PLL共聚物，在人癌细胞系上与单独的PLL相比，转染效率提高了5至30倍。由于氯喹提高了转染效率，Hep G2细胞很可能是通过内吞机制被质粒DNA/PEG-g-PLL复合物转染的。尽管阳离子脂质制剂Lipofectin在Hep G细胞中显示出比PEG-g-PLL略高的转染效率，但我们设计的PEG-g-PLL表现出较低的细胞毒性、早期基因表达以及长达96小时的基因表达维持。
