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

Masaru Eguchi; Tooru Ooya; Nobuhiko Yui

doi:10.1016/j.jconrel.2004.02.013

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

J Control Release. 2004 Apr 28;96(2):301-7. doi: 10.1016/j.jconrel.2004.02.013.

Authors

Masaru Eguchi¹, Tooru Ooya, Nobuhiko Yui

Affiliation

¹ School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Tatsunokuchi, Ishikawa 923-1292, Japan.

PMID: 15081220
DOI: 10.1016/j.jconrel.2004.02.013

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anthracenes / chemistry*
Calcium / chemistry
Polycyclic Compounds / chemistry*
Structure-Activity Relationship
Time Factors
Trypsin / chemistry
Trypsin Inhibitors / chemistry*
alpha-Cyclodextrins / chemistry*

Substances

Anthracenes
Polycyclic Compounds
Trypsin Inhibitors
alpha-Cyclodextrins
carboxyethylester-polyrotaxane
Trypsin
Calcium