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Tytuł:
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Screening of in vitro and in silico α-amylase, α-glucosidase, and lipase inhibitory activity of oxyprenylated natural compounds and semisynthetic derivatives.
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Autorzy:
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Faraone I; Department of Science, University of Basilicata, via dell'Ateneo Lucano 10, 85100, Potenza, Italy; SpinoffBioActiPlant s.r.l., via dell'Ateneo Lucano 10, 85100, Potenza, Italy.
Russo D; Department of Science, University of Basilicata, via dell'Ateneo Lucano 10, 85100, Potenza, Italy; SpinoffBioActiPlant s.r.l., via dell'Ateneo Lucano 10, 85100, Potenza, Italy.
Genovese S; Department of Pharmacy, University Gabriele D'Annunzio of Chieti-Pescara, Via dei Vestini 31, 66100, Chieti Scalo, CH, Italy.
Milella L; Department of Science, University of Basilicata, via dell'Ateneo Lucano 10, 85100, Potenza, Italy. Electronic address: .
Monné M; Department of Science, University of Basilicata, via dell'Ateneo Lucano 10, 85100, Potenza, Italy.
Epifano F; Department of Pharmacy, University Gabriele D'Annunzio of Chieti-Pescara, Via dei Vestini 31, 66100, Chieti Scalo, CH, Italy. Electronic address: .
Fiorito S; Department of Pharmacy, University Gabriele D'Annunzio of Chieti-Pescara, Via dei Vestini 31, 66100, Chieti Scalo, CH, Italy.
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Źródło:
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Phytochemistry [Phytochemistry] 2021 Jul; Vol. 187, pp. 112781. Date of Electronic Publication: 2021 Apr 28.
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Publication: 2003- : London : Elsevier
Original Publication: 1961-2003: Oxford : Pergamon Press.
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MeSH Terms:
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alpha-Amylases*
alpha-Glucosidases*
Computer Simulation ; Glycoside Hydrolase Inhibitors/pharmacology ; Lipase ; Molecular Docking Simulation
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Contributed Indexing:
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Keywords: Metabolic syndrome; Molecular docking; Oxyprenylated natural compounds; Pancreatic lipase inhibition; Semisynthetic compounds; α‐amylase inhibition; α‐glucosidase inhibition
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Substance Nomenclature:
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0 (Glycoside Hydrolase Inhibitors)
EC 3.1.1.3 (Lipase)
EC 3.2.1.1 (alpha-Amylases)
EC 3.2.1.20 (alpha-Glucosidases)
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Entry Date(s):
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Date Created: 20210430 Date Completed: 20210525 Latest Revision: 20210525
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Update Code:
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20240105
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DOI:
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10.1016/j.phytochem.2021.112781
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PMID:
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33930668
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Metabolic syndrome has several characteristic manifestations, including insulin resistance and dyslipidaemia, that demand therapeutic approaches, such as the inhibition of enzymes involved in nutrient absorption and digestion.This study aimed to evaluate the potential pharmacological use of natural compounds widespread in the plant kingdom and their semisynthetic compounds against target enzymes. Twenty-three oxyprenylated natural compoundswere investigated for their ability to inhibit α-amylase, α-glucosidase, and pancreatic lipase enzymes by in vitro assays. Moreover, in silico molecular docking was performed to analyse their binding capabilities into 3D structures. Farnesyloxyferulic acid, geranyloxyvanillic acid, nelumal A, and geranyloxyferulic acid showed the highest inhibition activity in all three in vitro enzyme assays. Moreover, in silico molecular docking of these four compounds was used to analyse their possible binding in 3D structures of the investigated enzymes. The results indicate that these compounds have considerable therapeutic potential for the treatment of metabolic syndrome, and further studies are warranted for their pharmacological development.
(Copyright © 2021 Elsevier Ltd. All rights reserved.)
