α-amino acid pendant polymers as endosomal pH-responsive gene carriers

Takuya Wada, Arihiro Kano, Naohiko Shimada, Atsushi Maruyama

研究成果: ジャーナルへの寄稿学術誌査読

9 被引用数 (Scopus)

抄録

In order to prepare gene carriers responsive to an endosomal pH, amino groups of linear poly(allylamine) (PAA) or poly(L-lysine) (PLL) were coupled with a-carboxyl groups of α-amino acids (Gly, His, Lys, Arg, and Orn). Acid-base titration indicated that Lys-, Arg-, and Orn-pendant polymers had both strongly basic groups and endoso-mal pH-responsive α-amino groups. These polymers, like PAA and PLL, formed stable complexes with DNA. Lys-, Arg-, and Orn-pendant polymers were effective transfection reagents independent of the backbone polymers. The pH-responsive α-amino groups enhanced transfection activity as shown by the observation that acetylation of the α-amino group resulted in a considerable loss in transfection activity. These results strongly suggested a lysosomo-tropic activity of the α-amino groups. Among the α-amino acid-pendant polymers tested, the Orn-pendant polymer exhibited the highest transfection activity/toxicity index. Since PLL with α-amino acid-pendants is composed of naturally occurring amino acids, it is expected to be biodegradable, and these reagents have promise as gene carriers.

本文言語英語
ページ(範囲)302-308
ページ数7
ジャーナルMacromolecular Research
20
3
DOI
出版ステータス出版済み - 3月 1 2012

All Science Journal Classification (ASJC) codes

  • 化学工学(全般)
  • 有機化学
  • ポリマーおよびプラスチック
  • 材料化学

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