Oxidation-Responsive OEGylated Poly-L-cysteine and Solution Properties Studies

被引：96

作者：

Fu, Xiaohui ^{[1
]}

Ma, Yinan ^{[1
]}

Shen, Yong ^{[1
]}

Fu, Wenxin ^{[1
]}

Li, Zhibo ^{[1
]}

机构：

[1] Chinese Acad Sci, Inst Chem, BNLMS, Beijing 100190, Peoples R China

来源：

BIOMACROMOLECULES | 2014年 / 15卷 / 03期

关键词：

SECONDARY STRUCTURE ANALYSES; DIBLOCK COPOLYMERS; BIOMEDICAL APPLICATIONS; POLYMERIC VESICLES; COIL TRANSITION; DRUG-RELEASE; L-GLUTAMATES; CONFORMATION; POLYPEPTIDES; TEMPERATURE;

D O I：

10.1021/bm5000554

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The oxidation-responsive behaviors of OEGylated poly-L-cysteine homopolypeptides, that is, poly(L-EG(x)MA-C)(n), were investigated. These poly-L-cysteine derivatives adopted mixed conformation in water, in which the beta-sheet accounted for a significant proportion. Upon oxidation, the thioethers in polypeptide side chains were converted to polar sulfone groups, which triggered the secondary structure transition from beta-sheet preferred conformation to random coil. Accordingly, the increase of side-chain polarity together with conformation changes increased samples' water solubility and cloud point temperature. Using mPEG(45)-NH2 as macroinitiator, we synthesized PEG(45)-b-poly(L-EG(2)MA-C)(22) diblock copolymer via ring-opening polymerization (ROP) of L-EG(2)MA-C N-carboxyanhydride (NCA). The PEG(45)-b-poly(L-EG(2)MA-C)(22) was able to self-assemble into spherical micelles in aqueous solution, and the micelles could undergo an oxidation-triggered disassembly due to the oxidation-responsive thioethers. Such a new class of oxidation-responsive polypeptides might provide a promising platform to construct inflammation targeting drug delivery systems.

引用

页码：1055 / 1061

页数：7