Pharmaceutical Research Center, School of Pharmacy, Mashhad University of Medical Sciences, P.O. Box 91775-1365, Mashhad, Iran.
Int J Biol Macromol. 2013 Sep;60:18-27. doi: 10.1016/j.ijbiomac.2013.05.001. Epub 2013 May 13.
Conjugation of various arginine-rich peptide sequences to vectors based on 10 kDa polyethylenimine (PEI) and its hydrophobic derivative (hexanoate-PEI) was investigated as a strategy for improving pDNA and siRNA transfection activities. Six different arginine-histidine (RH) sequences and two arginine-serine (RS) sequences with a range of R/H ratios were designed and coupled to PEI and hexanoate-PEI. All arginine-rich peptide derivatives of PEI significantly enhanced luciferase gene expression compared to PEI 10 kDa alone. Hexanoate-PEI derivatives exhibited higher transfection activity than underivatized PEI vectors. Improved transfection activity may have resulted at least in part from use of higher vector/DNA ratios made possible by reduced cytotoxicity of vectors, and to use of vectors with higher molecular weights. Vectors that were the most efficient in pDNA delivery and transfection were also the most effective in siRNA delivery and protein expression knock down.
将各种富含精氨酸的肽序列与基于 10 kDa 聚乙二烯亚胺（PEI）及其疏水衍生物（己酸酯-PEI）的载体缀合，作为提高 pDNA 和 siRNA 转染活性的策略进行了研究。设计了六个不同的精氨酸-组氨酸（RH）序列和两个具有不同 R/H 比的精氨酸-丝氨酸（RS）序列，并将其与 PEI 和己酸酯-PEI 偶联。与单独的 10 kDa PEI 相比，所有富含精氨酸的 PEI 衍生物均显著增强了荧光素酶基因的表达。己酸酯-PEI 衍生物的转染活性高于未衍生的 PEI 载体。转染活性的提高至少部分归因于载体细胞毒性降低，使得更高的载体/DNA 比成为可能，并且使用了更高分子量的载体。在 pDNA 传递和转染中效率最高的载体，在 siRNA 传递和蛋白质表达抑制方面也是最有效的。
