Chitooligosaccharides as a novel β-secretase inhibitor

被引：42

作者：

Byun, HG

Kim, YT

Park, PJ

Lin, XL

Kim, SK ^{[1
]}

机构：

[1] Pukyong Natl Univ, Dept Chem, Pusan 608737, South Korea

[2] Oklahoma Med Res Fdn, Funct Proteom Lab, Oklahoma City, OK 73104 USA

[3] Konkuk Univ, Dept Biotechnol, Chungju 380701, South Korea

来源：

CARBOHYDRATE POLYMERS | 2005年 / 61卷 / 02期

关键词：

Alzheimer's disease; beta-secretase inhibitor; chitooligosaccharide (COS);

D O I：

10.1016/j.carbpol.2005.05.003

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Nine kinds of hetero-chitooligosaccharides (hetero-COSs) with different degrees of deacetylation and molecular weights were prepared using an ultrafiltration (UF) membrane reactor system. In addition, their sulfated derivatives were also synthesized by a method using trimethylamine-sulfur trioxide to investigate the functional group of COSs on beta-secretase inhibitory activity. 90-MMWCOSs-I, which are 90% deacetylated COSs passed through the 5 kDa membrane but not passed through the 3 kDa membrane, exhibited the highest P-secretase inhibitory activity (25-42 mu M) based on molecular weight of 3 and 5 kDa. The inhibition pattern of the inhibitor was found to be a noncompetitive by Dixon plot, and K-i of 90-MMWCOSs-I was 3.8,7-6.47 mu M. Therefore, the data of this research suggest that 90-MMWCOSs-I is a good candidate target molecule to inhibit beta-secretase. (C) 2005 Elsevier Ltd. All rights reserved.

引用

页码：198 / 202

页数：5

共 28 条

[1] Untangling Alzheimer's disease with β-secretase inhibitors [J].