A new biological prospective for the 2-phenylbenzofurans as inhibitors of α-glucosidase and of the islet amyloid polypeptide formation.
Amyloid
/ chemistry
Benzofurans
/ chemistry
Blood Glucose
/ drug effects
Diabetes Mellitus, Type 2
/ metabolism
Glycoside Hydrolase Inhibitors
/ chemistry
Humans
Hydroxylation
Hypoglycemic Agents
/ pharmacology
Islet Amyloid Polypeptide
/ metabolism
Molecular Docking Simulation
Prospective Studies
alpha-Amylases
/ antagonists & inhibitors
alpha-Glucosidases
/ metabolism
2-phenylbenzofuran, molecular docking
Islet amyloid polypeptide
α-Glucosidase
Journal
International journal of biological macromolecules
ISSN: 1879-0003
Titre abrégé: Int J Biol Macromol
Pays: Netherlands
ID NLM: 7909578
Informations de publication
Date de publication:
01 Feb 2021
01 Feb 2021
Historique:
received:
28
07
2020
revised:
01
12
2020
accepted:
15
12
2020
pubmed:
22
12
2020
medline:
23
4
2021
entrez:
21
12
2020
Statut:
ppublish
Résumé
In this study, we have investigated a series of hydroxylated 2-phenylbenzofurans compounds for their inhibitory activity against α-amylase and α-glucosidase activity. Inhibitors of carbohydrate degrading enzymes seem to have an important role as antidiabetic drugs. Diabetes mellitus is a wide-spread metabolic disease characterized by elevated levels of blood glucose. The most common is type 2 diabetes, which can lead to severe complications. Since the aggregates of islet amyloid polypeptide (IAPP) are common in diabetic patients, the effect of compounds to inhibit amyloid fibril formation was also determined. All the compounds assayed showed to be more active against α-glucosidase. Compound 16 showed the lowest IC
Identifiants
pubmed: 33347933
pii: S0141-8130(20)35287-9
doi: 10.1016/j.ijbiomac.2020.12.117
pii:
doi:
Substances chimiques
Amyloid
0
Benzofurans
0
Blood Glucose
0
Glycoside Hydrolase Inhibitors
0
Hypoglycemic Agents
0
Islet Amyloid Polypeptide
0
alpha-Amylases
EC 3.2.1.1
alpha-Glucosidases
EC 3.2.1.20
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
428-435Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.