Inhibitory evaluation of oligonol on α-glucosidase, protein tyrosine phosphatase 1B, cholinesterase, and β-secretase 1 related to diabetes and Alzheimer's disease

被引：15

作者：

Choi, Jae Sue ^{[1
]}

Bhakta, Himanshu Kumar ^{[1
]}

Fujii, Hajime ^{[2
]}

Min, Byung-Sun ^{[3
]}

Park, Chan Hum ^{[3
]}

Yokozawa, Takako ^{[4
]}

Jung, Hyun Ah ^{[5
]}

机构：

[1] Pukyong Natl Univ, Dept Food & Life Sci, Busan 608737, South Korea

[2] Amino Up Chem Co Ltd, Sapporo, Hokkaido, Japan

[3] Catholic Univ Daegu, Coll Pharm, Gyeongbuk 712702, South Korea

[4] Toyama Univ, Grad Sch Sci & Engn Res, Toyama 9308555, Japan

[5] Chonbuk Natl Univ, Dept Food Sci & Human Nutr, Jeonju 561756, South Korea

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2016年 / 39卷 / 03期

关键词：

Oligonol; Anti-diabetic activity; Anti-Alzheimer activity; Kinetics; LYCHEE FRUIT; OXIDATIVE STRESS; INSULIN ACTION; DAMAGE; ACETYLCHOLINESTERASE; POLYPHENOLS; TOXICITY; MELLITUS;

D O I：

10.1007/s12272-015-0682-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Oligonol is a low-molecular-weight form of polyphenol that is derived from lychee fruit extract and contains catechin-type monomers and oligomers of proanthocyanidins. This study investigates the anti-diabetic activities of oligonol via alpha-glucosidase and human recombinant protein tyrosine phosphatase 1B (PTP1B) assays, as well as its anti-Alzheimer activities by evaluating the ability of this compound to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-site amyloid precursor protein cleaving enzyme 1 (BACE1). Oligonol exhibited potent concentration-dependent anti-diabetic activities by inhibiting alpha-glucosidase and PTP1B with IC50 values of 23.14 A mu g/mL and 1.02 A mu g/mL, respectively. Moreover, a kinetics study revealed that oligonol inhibited alpha-glucosidase (K (i) = 22.36) and PTP1B (K (i) = 8.51) with characteristics typical of a mixed inhibitor. Oligonol also displayed potent concentration-dependent inhibitory activity against AChE and BChE with IC50 values of 4.34 A mu g/mL and 2.07 A mu g/mL, respectively. However, oligonol exhibited only marginal concentration-dependent BACE1 inhibitory activity with an IC50 value of 130.45 A mu g/mL. A kinetics study revealed mixed-type inhibition against AChE (K (i) = 4.65) and BACE1 (K (i) = 58.80), and noncompetitive-type inhibition against BChE (K (i) = 9.80). Furthermore, oligonol exhibited dose-dependent inhibitory activity against peroxynitrite (ONOO-)-mediated protein tyrosine nitration. These results indicate that oligonol has strong preventative potential in diabetes mellitus and in Alzheimer's disease.

引用

页码：409 / 420

页数：12

共 49 条

[31] Treatment with oligonol, a low-molecular polyphenol derived from lychee fruit, attenuates diabetes-induced hepatic damage through regulation of oxidative stress and lipid metabolism [J].