Controlling the mechanism of trypsin inhibition by the numbers of alpha-cyclodextrins and carboxyl groups in carboxyethylester-polyrotaxanes.
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.
Eguchi
Masaru
M
School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Tatsunokuchi, Ishikawa 923-1292, Japan.
Ooya
Tooru
T
Yui
Nobuhiko
N
D000873:Anthracenes / Q000737:chemistry*; D002118:Calcium / Q000737:chemistry; D011083:Polycyclic Compounds / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013997:Time Factors; D014357:Trypsin / Q000737:chemistry; D014361:Trypsin Inhibitors / Q000737:chemistry*; D047391:alpha-Cyclodextrins / Q000737:chemistry*
D000873:Anthracenes; D011083:Polycyclic Compounds; D014361:Trypsin Inhibitors; D047391:alpha-Cyclodextrins; C466718:carboxyethylester-polyrotaxane; D014357:Trypsin; D002118:Calcium