微波辅助点击聚合合成聚（ε-赖氨酸）类似物聚合物。

Chemosynthesis of poly(ε-lysine)-analogous polymers by microwave-assisted click polymerization.

机构信息

State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Graduate School of the Chinese Academy of Sciences, Renmin Str. 5625, Changchun 130022, P. R. China.

出版信息

Biomacromolecules. 2011 Mar 14;12(3):737-46. doi: 10.1021/bm1013662. Epub 2011 Feb 8.

DOI:10.1021/bm1013662

PMID:21302898

Abstract

Poly(ε-lysine) (ε-PL)-analogous click polypeptides with not only similar α-amino side groups but also similar main chain to ε-PL were chemically synthesized for the first time through click polymerization from aspartic (or glutamic)-acid-based dialkyne and diazide monomers. With microwave-assisting, the reaction time of click polymerization was compressed into 30 min. The polymers were fully characterized by NMR, ATR-FTIR, and SEC-MALLS analysis. The deprotected click polypeptides had similar pK(a) value (7.5) and relatively low cytotoxicity as ε-PL and could be used as substitutes of ε-PL in biomedical applications, especially in endotoxin selective removal. Poly(ethylene glycol) (PEG)-containing alternating copolymers with α-amino groups were also synthesized and characterized. After deprotection, the polymers could be used as functional gene vector with PEG shadowing system and NCA initiator to get amphiphilic graft polymers.

摘要

聚（ε-赖氨酸）（ε-PL）类似物点击多肽不仅具有相似的α-氨基侧基，而且与 ε-PL 的主链也相似，通过从天冬氨酸（或谷氨酸）-基二炔和叠氮单体的点击聚合，首次在化学上合成。通过微波辅助，点击聚合的反应时间被压缩到 30 分钟。通过 NMR、ATR-FTIR 和 SEC-MALLS 分析对聚合物进行了充分的表征。脱保护的点击多肽具有相似的 pK(a)值（7.5）和相对较低的细胞毒性，与 ε-PL 相似，可以在生物医学应用中用作 ε-PL 的替代品，特别是在内毒素选择性去除方面。还合成并表征了含有 α-氨基的聚乙二醇（PEG）交替共聚物。脱保护后，聚合物可用作具有 PEG 屏蔽系统和 NCA 引发剂的功能基因载体，以获得两亲性接枝聚合物。