Wang Yong-Qiang, Sun Yun-Xia, Hong Xin-Lin, Zhang Xian-Zheng, Zhang Gao-Yong
Department of Chemistry, Wuhan University, Wuhan 430072, China.
Mol Biosyst. 2010 Jan;6(1):256-63. doi: 10.1039/b915718b. Epub 2009 Oct 6.
A series of poly(methyl methacrylate)-graft-oligoamines (PMMA-g-oligoamines), including PMMA-g-DETA, PMMA-g-TETA and PMMA-g-TEPA, were synthesized through aminolysis of the PMMA with diethylenetriamine, triethylenetetramine and tetraethylenepentamine. Agarose gel retardation assay indicated that PMMA-g-oligoamines had good binding capability with plasmid DNA, and the binding capability increased with increasing length of oligoamines and content of nitrogen (N%). The results of particle size, zeta potential and morphology observation further showed that the PMMA-g-oligoamines could condense DNA efficiently and the PMMA-g-oligoamine/DNA complexes were uniform nanospheres. The in vitro cell viability indicated that PMMA-g-oligoamines were less toxic than 25 kDa PEI, though the cytotoxicity of PMMA-g-oligoamines increased slightly with increasing length of oligoamines as well as the N% of PMMA-g-oligoamines. The transfection efficiency of PMMA-g-oligoamines/DNA complexes in 293 T and HeLa cells demonstrated that PMMA-g-oligoamines could transfect cells efficiently with increasing the length of oligoamines, especially PMMA-g-TEPA with highest N%, and showed similar transfection capability as 25 kDa PEI. The cellular uptake study showed that the distribution of YOYO-1 labeled DNA in the cytoplasm and nuclei increased gradually with increasing length of oligoamines.
通过用二乙烯三胺、三乙烯四胺和四乙烯五胺对聚甲基丙烯酸甲酯（PMMA）进行氨解反应，合成了一系列聚甲基丙烯酸甲酯接枝低聚胺（PMMA-g-oligoamines），包括PMMA-g-DETA、PMMA-g-TETA和PMMA-g-TEPA。琼脂糖凝胶阻滞试验表明，PMMA-g-oligoamines与质粒DNA具有良好的结合能力，且结合能力随着低聚胺长度的增加和氮含量（N%）的增加而增强。粒径、zeta电位和形态观察结果进一步表明，PMMA-g-oligoamines能够有效地凝聚DNA，且PMMA-g-oligoamine/DNA复合物为均匀的纳米球。体外细胞活力表明，PMMA-g-oligoamines的毒性低于25 kDa的聚乙烯亚胺（PEI），尽管PMMA-g-oligoamines的细胞毒性也随着低聚胺长度以及PMMA-g-oligoamines的N%的增加而略有增加。PMMA-g-oligoamines/DNA复合物在293 T细胞和HeLa细胞中的转染效率表明，随着低聚胺长度的增加，PMMA-g-oligoamines能够有效地转染细胞，尤其是N%最高的PMMA-g-TEPA，其转染能力与25 kDa的PEI相似。细胞摄取研究表明，随着低聚胺长度的增加，YOYO-1标记的DNA在细胞质和细胞核中的分布逐渐增加。
