» Articles » PMID: 38185713

Flavonoids As Dual-target Inhibitors Against α-glucosidase and α-amylase: a Systematic Review of in Vitro Studies

Overview
Publisher Springer
Specialty Biology
Date 2024 Jan 7
PMID 38185713
Authors
Affiliations
Soon will be listed here.
Abstract

Diabetes mellitus remains a major global health issue, and great attention is directed at natural therapeutics. This systematic review aimed to assess the potential of flavonoids as antidiabetic agents by investigating their inhibitory effects on α-glucosidase and α-amylase, two key enzymes involved in starch digestion. Six scientific databases (PubMed, Virtual Health Library, EMBASE, SCOPUS, Web of Science, and WHO Global Index Medicus) were searched until August 21, 2022, for in vitro studies reporting IC values of purified flavonoids on α-amylase and α-glucosidase, along with corresponding data for acarbose as a positive control. A total of 339 eligible articles were analyzed, resulting in the retrieval of 1643 flavonoid structures. These structures were rigorously standardized and curated, yielding 974 unique compounds, among which 177 flavonoids exhibited inhibition of both α-glucosidase and α-amylase are presented. Quality assessment utilizing a modified CONSORT checklist and structure-activity relationship (SAR) analysis were performed, revealing crucial features for the simultaneous inhibition of flavonoids against both enzymes. Moreover, the review also addressed several limitations in the current research landscape and proposed potential solutions. The curated datasets are available online at https://github.com/MedChemUMP/FDIGA .

Citing Articles

Flavonoids as Natural Anti-Inflammatory Agents in the Atopic Dermatitis Treatment.

Zawawi N, Ahmad H, Madatheri R, Fadilah N, Maarof M, Fauzi M Pharmaceutics. 2025; 17(2).

PMID: 40006628 PMC: 11859288. DOI: 10.3390/pharmaceutics17020261.


BuZhong YiQi Formula Alleviates Postprandial Hyperglycemia in T2DM Rats by Inhibiting α-Amylase and α-Glucosidase In Vitro and In Vivo.

Zeng X, Wang L, Wang M, Hu Z, Li X, Fei G Pharmaceuticals (Basel). 2025; 18(2).

PMID: 40006017 PMC: 11858844. DOI: 10.3390/ph18020201.


A multidimensional study for design of phytochemical profiling, antioxidant potential, and enzyme inhibition effects of ışgın () as an edible plant.

Tel A, Aslan K, Yilmaz M, Gulcin I Food Chem X. 2025; 25:102125.

PMID: 39974533 PMC: 11838142. DOI: 10.1016/j.fochx.2024.102125.


Enzyme (α-Glucosidase, α-Amylase, PTP1B & VEGFR-2) Inhibition and Cytotoxicity of Fluorinated Benzenesulfonic Ester Derivatives of the 5-Substituted 2-Hydroxy-3-nitroacetophenones.

Olomola T, Nkoana J, More G, Gildenhuys S, Mphahlele M Int J Mol Sci. 2024; 25(22).

PMID: 39595931 PMC: 11594133. DOI: 10.3390/ijms252211862.


Exploring the 3,5-Dibromo-4,6-dimethoxychalcones and Their Flavone Derivatives as Dual α-Glucosidase and α-Amylase Inhibitors with Antioxidant and Anticancer Potential.

Nkoana J, Mphahlele M, More G, Choong Y Antioxidants (Basel). 2024; 13(10).

PMID: 39456508 PMC: 11505200. DOI: 10.3390/antiox13101255.


References
1.
Islam M, Jung H, Sohn H, Kim H, Choi J . Potent α-glucosidase and protein tyrosine phosphatase 1B inhibitors from Artemisia capillaris. Arch Pharm Res. 2013; 36(5):542-52. DOI: 10.1007/s12272-013-0069-7. View

2.
Wu S, Tian L . A new flavone glucoside together with known ellagitannins and flavones with anti-diabetic and anti-obesity activities from the flowers of pomegranate (Punica granatum). Nat Prod Res. 2018; 33(2):252-257. DOI: 10.1080/14786419.2018.1446009. View

3.
Swilam N, Nawwar M, A Radwan R, Mostafa E . Antidiabetic Activity and In Silico Molecular Docking of Polyphenols from L. subsp. Aegyptiaca (Willd.) Koehne Waste: Structure Elucidation of Undescribed Acylated Flavonol Diglucoside. Plants (Basel). 2022; 11(3). PMC: 8840488. DOI: 10.3390/plants11030452. View

4.
Zhang X, Liu Z, Bi X, Liu J, Li W, Zhao Y . Flavonoids and its derivatives from Callistephus chinensis flowers and their inhibitory activities against alpha-glucosidase. EXCLI J. 2016; 12:956-66. PMC: 4904746. View

5.
Gao H, Kawabata J . alpha-Glucosidase inhibition of 6-hydroxyflavones. Part 3: Synthesis and evaluation of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs and 6-aminoflavones as alpha-glucosidase inhibitors. Bioorg Med Chem. 2005; 13(5):1661-71. DOI: 10.1016/j.bmc.2004.12.010. View