Controlling the mechanism of trypsin inhibition by the numbers of α-cyclodextrins and carboxyl groups in carboxyethylester-polyrotaxanes

被引：36

作者：

Eguchi, M ^{[1
]}

Ooya, T ^{[1
]}

Yui, N ^{[1
]}

机构：

[1] Japan Adv Inst Sci & Technol, Sch Mat Sci, Tatsunokuchi, Ishikawa 9231292, Japan

来源：

JOURNAL OF CONTROLLED RELEASE | 2004年 / 96卷 / 02期

关键词：

polyrotaxanes; calcium binding; trypsin inhibition;

D O I：

10.1016/j.jconrel.2004.02.013

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Carboxyethylester-polyrotaxanes (CEE-polyrotaxanes) with the various number of CEE-modified alpha-cyclodextrins (CEE-alpha-CDs) were synthesized, and the effects of the number of CEE-alpha-CDs on calcium binding and trypsin inhibition were investigated. Calcium binding affinity was dependent on the density of the CEE groups accompanied with the number of alpha-CD threading in the CEE-polyrotaxanes. The high number of CEE-alpha-CDs leads to greater inhibition of trypsin activity than poly(acrylic acid), which is mainly due to the good calcium binding affinity. The CEE-polyrotaxane with the smallest number of CEE-alpha-CDs temporally interacted with trypsin, which was well correlated with the inhibition and recovery of trypsin activity. Therefore, the number of CEE-alpha-CDs in the CEE-polyrotaxanes can control the inhibition mechanism of trypsin activity. (C) 2004 Elsevier B.V. All rights reserved.

引用

页码：301 / 307

页数：7

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