Inhibitory Effect of Fisetin on α-Glucosidase Activity: Kinetic and Molecular Docking Studies

被引：19

作者：

Shen, Beiyun ^{[1
]}

Shangguan, Xinchen ^{[1
]}

Yin, Zhongping ^{[1
]}

Wu, Shaofu ^{[1
]}

Zhang, Qingfeng ^{[1
]}

Peng, Wenwen ^{[2
]}

Li, Jingen ^{[1
]}

Zhang, Lu ^{[3
]}

Chen, Jiguang ^{[1
,2
]}

机构：

[1] Jiangxi Agr Univ, Coll Food Sci & Engn, Jiangxi Key Lab Nat Prod & Funct Food, Nanchang 330045, Jiangxi, Peoples R China

[2] Jiangxi Agr Univ, Coll Agr, Lab Phytochem & Plant Derived Pesticides, Nanchang 330045, Jiangxi, Peoples R China

[3] Jiangxi Agr Univ, Coll Forestry, Collaborat Innovat Ctr Jiangxi Typ Trees Cultivat, Nanchang 330045, Jiangxi, Peoples R China

来源：

MOLECULES | 2021年 / 26卷 / 17期

关键词：

alpha-glucosidase inhibition; fisetin; diabetes; molecular docking; IN-VITRO; BIOLOGICAL EVALUATION; INTERACTION MECHANISM; DERIVATIVES; CONSTITUENTS; FLAVONOIDS; DISCOVERY; OXIDATION; LUTEOLIN; INSIGHTS;

D O I：

10.3390/molecules26175306

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：

The inhibition of alpha-glucosidase is a clinical strategy for the treatment of type 2 diabetes mellitus (T2DM), and many natural plant ingredients have been reported to be effective in alleviating hyperglycemia by inhibiting alpha-glucosidase. In this study, the alpha-glucosidase inhibitory activity of fisetin extracted from Cotinus coggygria Scop. was evaluated in vitro. The results showed that fisetin exhibited strong inhibitory activity with an IC50 value of 4.099 x 10(-4) mM. Enzyme kinetic analysis revealed that fisetin is a non-competitive inhibitor of alpha-glucosidase, with an inhibition constant value of 0.01065 +/- 0.003255 mM. Moreover, fluorescence spectrometric measurements indicated the presence of only one binding site between fisetin and alpha-glucosidase, with a binding constant (lgKa) of 5.896 L center dot mol(-1). Further molecular docking studies were performed to evaluate the interaction of fisetin with several residues close to the inactive site of alpha-glucosidase. These studies showed that the structure of the complex was maintained by Pi-Sigma and Pi-Pi stacked interactions. These findings illustrate that fisetin extracted from Cotinus coggygria Scop. is a promising therapeutic agent for the treatment of T2DM.

引用

页数：11

共 45 条

[1]

Alberti KGMM, 1998, DIABETIC MED, V15, P539, DOI 10.1002/(SICI)1096-9136(199807)15:7<539::AID-DIA668>3.0.CO

[2]

2-S

[3] Fisetin protects against streptozotocin-induced diabetic cardiomyopathy in rats by suppressing fatty acid oxidation and inhibiting protein kinase R [J].

AlTamimi, Jozaa Z. ;

BinMowyna, Mona N. ;

AlFaris, Nora A. ;

Alagal, Reham I. ;

El-Kott, Attalla F. ;

Al-Farga, Ammar M. .

SAUDI PHARMACEUTICAL JOURNAL, 2021, 29 (01) :27-42

[4]

[Anonymous], 2019, IDF DIABETES ATLAS, V9th

[5] Synthesis and biological evaluation of new benzimidazole-1,2,3-triazole hybrids as potential α-glucosidase inhibitors [J].

Asemanipoor, Nafise ;

Mohammadi-Khanaposhtani, Maryam ;

Moradi, Shahram ;

Vahidi, Mahbobeh ;

Asadi, Mehdi ;

Faramarzi, Mohammad Ali ;

Mahdavi, Mohammad ;

Biglar, Mahmood ;

Larijani, Bagher ;

Hamedifar, Haleh ;

Hajimiri, Mir Hamed .

BIOORGANIC CHEMISTRY, 2020, 95

[6] α-Glucosidase and α-amylase inhibitory activities of Nepalese medicinal herb Pakhanbhed (Bergenia ciliata, Haw.) [J].

Bhandari, Megh Raj ;

Jong-Anurakkun, Nilubon ;

Hong, Gao ;

Kawabata, Jun .

FOOD CHEMISTRY, 2008, 106 (01) :247-252

[7] α-Glucosidase inhibitory effect of anthocyanins from Cinnamomum camphora fruit: Inhibition kinetics and mechanistic insights through in vitro and in silico studies [J].

Chen, Ji-guang ;

Wu, Shao-fu ;

Zhang, Qing-feng ;

Yin, Zhong-ping ;

Zhang, Lu .

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 2020, 143 :696-703

[8] Fisetin Alleviates Hepatic and Adipocyte Fibrosis and Insulin Resistance in Diet-Induced Obese Mice [J].

Choi, Myung-Sook ;

Choi, Ji-Young ;

Kwon, Eun-Young .

JOURNAL OF MEDICINAL FOOD, 2020, 23 (10) :1019-1032

[9] Isolation and characterization of α-glucosidase inhibitory constituents from Rhodiola crenulata [J].

Chu, Yung-Hung ;

Wu, Shih-Hsiung ;

Hsieh, Jung-Feng .

FOOD RESEARCH INTERNATIONAL, 2014, 57 :8-14

[10] Evaluation of collagenase, elastase and tyrosinase inhibitory activities of Cotinus coggygria Scop. through in vitro and in silico approaches [J].

Deniz, Fatma Sezer Senol ;

Salmas, Ramin Ekhteiari ;

Emerce, Esra ;

Cankaya, Iffet Irem Tatli ;

Yusufoglu, Hasan Soliman ;

Orhan, Ilkay Erdogan .

SOUTH AFRICAN JOURNAL OF BOTANY, 2020, 132 :277-288

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