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

共 43 条

[21] Discovery of novel α-glucosidase inhibitors based on the virtual screening with the homology-modeled protein structure [J].

Park, Hwangseo ;

Hwang, Kyo Yeol ;

Oh, Kyung Hwan ;

Kim, Young Hoon ;

Lee, Jae Yeon ;

Kim, Keun .

BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (01) :284-292

[22]

Peng X, 2016, FOOD FUNCT, V7, P982, DOI [10.1039/C5FO00992H, 10.1039/c5fo00992h]

[23] Inhibitory kinetics and mechanism of kaempferol on α-glucosidase [J].

Peng, Xi ;

Zhang, Guowen ;

Liao, Yijing ;

Gong, Deming .

FOOD CHEMISTRY, 2016, 190 :207-215

[24] The antioxidant activity of phloretin: the disclosure of a new antioxidant pharmacophore in flavonoids [J].

Rezk, BM ;

Haenen, GRMM ;

van der Vijgh, WJF ;

Bast, A .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2002, 295 (01) :9-13

[25] Inhibition of Oxidation of Aqueous Emulsions of Omega-3 Fatty Acids and Fish Oil by Phloretin and Phloridzin [J].

Rupasinghe, H. P. Vasantha ;

Yasmin, Afsana .

MOLECULES, 2010, 15 (01) :251-257

[26] Binding interaction of sorafenib with bovine serum albumin: Spectroscopic methodologies and molecular docking [J].

Shi, Jie-Hua ;

Chen, Jun ;

Wang, Jing ;

Zhu, Ying-Yao ;

Wang, Qi .

SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY, 2015, 149 :630-637

[27] Interaction of erucic acid with bovine serum albumin using a multi-spectroscopic method and molecular docking technique [J].

Shu, Yang ;

Xue, Weiwei ;

Xu, Xiaoying ;

Jia, Zhimin ;

Yao, Xiaojun ;

Liu, Shuwen ;

Liu, Lihong .

FOOD CHEMISTRY, 2015, 173 :31-37

[28] DETERMINATION OF PROTEIN SECONDARY STRUCTURE BY FOURIER-TRANSFORM INFRARED-SPECTROSCOPY - A CRITICAL-ASSESSMENT [J].

SUREWICZ, WK ;

MANTSCH, HH ;

CHAPMAN, D .

BIOCHEMISTRY, 1993, 32 (02) :389-394

[29] Inhibition of α-glucosidase and α-amylase by flavonoids [J].

Tadera, K ;

Minami, Y ;

Takamatsu, K ;

Matsuoka, T .

JOURNAL OF NUTRITIONAL SCIENCE AND VITAMINOLOGY, 2006, 52 (02) :149-153

[30] Novel Insights into the Inhibitory Mechanism of Kaempferol on Xanthine Oxidase [J].

Wang, Yajie ;

Zhang, Guowen ;

Pan, Junhui ;

Gong, Deming .

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 2015, 63 (02) :526-534

← 1 2 3 4 5 →