Inhibitory effect of phloretin on α-glucosidase: Kinetics, interaction mechanism and molecular docking

被引：179

作者：

Han, Lin ^{[1
,2
]}

Fang, Chun ^{[1
]}

Zhu, Ruixue ^{[1
]}

Peng, Qiang ^{[1
]}

Li, Ding ^{[3
]}

Wang, Min ^{[1
]}

机构：

[1] Northwest A&F Univ, Coll Food Sci & Engn, Yangling 712100, Shanxi, Peoples R China

[2] Chongqing Three Gorges Univ, Coll Life Sci & Engn, Chongqing 404100, Peoples R China

[3] Northwest A&F Univ, Coll Sci, Yangling 712100, Peoples R China

来源：

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES | 2017年 / 95卷

关键词：

Phloretin; α -glucosidase; Inhibitory mechanisms; BOVINE SERUM-ALBUMIN; IN-VITRO; ACID; POLYPHENOLS; DERIVATIVES; PHLORHIZIN; KAEMPFEROL; PHTHALATE; AMYLASE; BINDING;

D O I：

10.1016/j.ijbiomac.2016.11.089

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

As the aglycone of phloridzin, phloretin belongs to dihydrochalcone with antioxidant, anti-inflammatory and antimicrobial activities. In this study, multispectroscopic techniques and molecular docking analysis were used to investigate the inhibitory activity and mechanisms of phloretin on alpha-glucosidase. The results showed that phloretin reversibly inhibited alpha-glucosidase in a mixed-type manner and the value of IC50 was 31.26 mu g L-1. The intrinsic fluorescence of alpha-glucosidase was quenched by the interactions with phloretin through a static quenching mechanism and spontaneously formed phloretin-alpha-glucosidase complex by the driving forces of van der Waals force and hydrogen bond. Atomic force microscope (AFM) studies and FT-IR measurements suggested that the interactions could change the micro-environments and conformation of the enzymes and the molecular docking analysis displayed the exact binding site of phloretin on alpha-glucosidase. These results indicated that phloretin is a strong alpha-glucosidase inhibitor, thus could be contribute to the improvement of diabetes mellitus. (C) 2016 Elsevier B.V. All rights reserved.

引用

页码：520 / 527

页数：8

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