羧甲基聚（L-组氨酸）作为一种新型pH敏感多肽以增强多聚体基因递送。

Carboxymethyl poly(L-histidine) as a new pH-sensitive polypeptide to enhance polyplex gene delivery.

作者信息

Asayama Shoichiro, Sudo Miyuki, Nagaoka Shoji, Kawakami Hiroyoshi

机构信息

Department of Applied Chemistry, Tokyo Metropolitan University, Hacioji, Tokyo, Japan.

出版信息

Mol Pharm. 2008 Sep-Oct;5(5):898-901. doi: 10.1021/mp800094b. Epub 2008 Aug 14.

DOI:10.1021/mp800094b

PMID:18700779

Abstract

Carboxymethyl poly( l-histidine) (CM-PLH) as a new pH-sensitive polypeptide has enhanced polyplex gene delivery. Agarose gel retardation assay and zeta potential measurement proved that the anionic CM-PLH at physiological pH coated the PEI/DNA binary complexes. The resulting CM-PLH/PEI/DNA ternary complexes showed the gene expression value 300 times higher than that of the PEI/DNA binary complexes. These results suggest that the synergistic effect of the pH-sensitive imidazole groups at endosomal pH and the anionic carboxymethyl groups at physiological pH in the CM-PLH enhanced polyplex gene delivery.

摘要

羧甲基聚（L-组氨酸）（CM-PLH）作为一种新型的pH敏感多肽，增强了多聚体基因递送。琼脂糖凝胶阻滞试验和ζ电位测量证明，在生理pH值下呈阴离子性的CM-PLH包被了PEI/DNA二元复合物。所得的CM-PLH/PEI/DNA三元复合物的基因表达值比PEI/DNA二元复合物高300倍。这些结果表明，CM-PLH中内体pH值下的pH敏感咪唑基团与生理pH值下的阴离子羧甲基基团的协同作用增强了多聚体基因递送。