Synthesis and inhibitory activity of euparin derivatives as potential dual inhibitors against α-glucosidase and protein tyrosine phosphatase 1B (PTP1B).
Chalcone
Diabetes
Euparin
Molecular docking
PTP1B
α-Glucosidase
Journal
Fitoterapia
ISSN: 1873-6971
Titre abrégé: Fitoterapia
Pays: Netherlands
ID NLM: 16930290R
Informations de publication
Date de publication:
Sep 2023
Sep 2023
Historique:
received:
11
03
2023
revised:
19
06
2023
accepted:
23
06
2023
medline:
21
8
2023
pubmed:
27
6
2023
entrez:
26
6
2023
Statut:
ppublish
Résumé
Diabetes mellitus is a serious threat to human life and health. The α-glucosidase and protein tyrosine phosphatase 1B (PTP1B) were important targets for the treatment of type 2 diabetes mellitus. In this paper, euparin, a natural product from Eupatorium chinense possessed extensive pharmacological activities, was selected as the lead compound. It was derived into chalcone compounds with high efficiency, and the inhibitory activities of these 30 products on α-glucosidase and PTP1B were tested. The results showed that compounds 12 and 15 had good inhibitory activities against both enzymes. The IC
Identifiants
pubmed: 37364700
pii: S0367-326X(23)00171-5
doi: 10.1016/j.fitote.2023.105596
pii:
doi:
Substances chimiques
Glycoside Hydrolase Inhibitors
0
Enzyme Inhibitors
0
alpha-Glucosidases
EC 3.2.1.20
euparin
46YA021ENM
Protein Tyrosine Phosphatase, Non-Receptor Type 1
EC 3.1.3.48
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
105596Informations de copyright
Copyright © 2023 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest Authors declare no competing financial interest.