Jun Yong Joo, Kim Jung Hee, Choi Su Jin, Lee Hwa Jeong, Jun Moo Jin, Sohn Youn Soo
Division of Nano Science BK 21, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea.
Bioorg Med Chem Lett. 2007 Jun 1;17(11):2975-8. doi: 10.1016/j.bmcl.2007.03.069. Epub 2007 Mar 25.
In order to develop a new gene delivery vector, a novel cationic poly(organophosphazene) was synthesized by stepwise nucleophilic substitutions of poly(dichlorophosphazene) with a hydrophilic methoxy-poly(ethylene glycol) (MPEG) as a shielding group and a branched tetra(L-lysine), LysLys(LysEt)(2), as a cationic moiety. The cationic polymer has shown to form a polyplex by DNA condensation and very low in vitro cytotoxicity probably due to the shielding effect of MPEG, which provides a basis for improving the low gene transfection yield of cationic polyphosphazenes.
为了开发一种新的基因传递载体，通过用亲水性甲氧基聚乙二醇（MPEG）作为屏蔽基团和支链四（L-赖氨酸）LysLys（LysEt）（2）作为阳离子部分对聚（二氯磷腈）进行逐步亲核取代，合成了一种新型阳离子聚（有机磷腈）。该阳离子聚合物已显示通过DNA缩合形成多聚体，并且由于MPEG的屏蔽作用，其体外细胞毒性非常低，这为提高阳离子聚磷腈的低基因转染率提供了基础。
