α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure–activity relationship study
Open accessAbstract
α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme’s activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of α-glucosidase, based on in vitro structure–activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A- and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC50 much lower than the one found for the most widely prescribed α-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.
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Flavonoids may possess strong inhibitory activities on the intestinal alpha-glucosidase enzyme, delaying the absorption of glucose and flattening postprandial hyperinsulinemic/hyperglycemic excursions.
“In addition to this, several in vitro studies have confirmed that flavonoids may possess strong inhibitory activities on the intestinal α-glucosidase enzyme that catalyzes the cleavage of glucose from disaccharides, thereby delaying the absorption of glucose and flattening postprandial hyperinsulinemic/hyperglycemic excursions [61,62].”
From Mediterranean diet nutrients to turn the tide against insulin resistance and related diseases (2020) · cites this paper as [62]
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Flagged first, then by citations
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“In addition to this, several in vitro studies have confirmed that flavonoids may possess strong inhibitory activities on the intestinal α-glucosidase enzyme that catalyzes the cleavage of glucose from disaccharides, thereby delaying the absorption of glucose and flattening postprandial hyperinsulinemic/hyperglycemic e…”
BackgroundFlavonoids as Antiobesity Agents: A Review
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Self-citation
- Authors
- Proença, C., Freitas, M., Ribeiro, D., Oliveira, E. F. T., Sousa, J. L. C., Tomé, S. M., Ramos, M. J., Silva, A. M. S., Fernandes, P. A., & Fernandes, E.
- Affiliations
- Universidade do Porto (PT)
- University of Aveiro (PT)
- Corresponding author
- Fernandes, Pedro A.
- Fernandes, Eduarda
- ORCID
- Venue
- Journal of Enzyme Inhibition and Medicinal Chemistry
- Publisher
- Informa UK Limited
- Published
- 2017-01-01
- Volume
- 32
- Issue
- 1
- Pages
- 1216-1228
- ISSN
- 1475-6366 (ISSN-L)
- 1475-6374
- PMC
- PMC6009965
- OpenAlex
- W2759298922
- Cited by
- 432
- References
- 67
- Citations by year
- 2026: 56 · 2025: 41 · 2024: 52 · 2023: 51 · 2022: 76 · 2021: 63 · 2020: 55 · 2019: 24 · 2018: 14
- FWCI
- 20.01
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Journal of Enzyme Inhibition and Medicinal Chemistry (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Figshare (submittedVersion, cc-by)
- Figshare (cc-by)
- Funders
- Fundação para a Ciência e Tecnologia and Ministério da Educação e Ciência
- European Union funds (PT2020 UID/MULTI/04378/2013 – POCI/01/0145/FEDER/007728, FCT UID/QUI/00062/2013, NORTE-01–0145-FEDER-000024)
- Programa Operacional Competitividade e Internacionalização (PTDC/QEQ-QAN/1742/2014 – POCI-01–0145-FEDER-016530)
- FCT (SFRH/BD/116005/2016)
- Fundo Social Europeu
- Ministério da Ciência, Tecnologia e Ensino Superior
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Bioactive natural compounds
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Keywords
- α-glucosidase inhibition, flavonoids, structure-activity relationship, type 2 diabetes, acarbose, catechol groups, enzyme inhibition kinetics, molecular docking, antidiabetic drugs
- MeSH terms
- alpha-Glucosidases, Computer Simulation, Dose-Response Relationship, Drug, Flavonoids, Saccharomyces cerevisiae, Structure-Activity Relationship, Molecular Structure, Acarbose, Molecular Docking Simulation, Glycoside Hydrolase Inhibitors
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