Article ; Online: Discovery of anthraquinones as DPP-IV inhibitors: Structure-activity relationships and inhibitory mechanism.
2023 Volume 168, Page(s) 105549
Abstract: Dipeptidyl peptidase IV (DPP-IV) is an integrated type II transmembrane protein that reduces endogenous insulin contents and increases plasma glucose levels by hydrolyzing glucagon-like peptide-1 (GLP-1). Inhibition of DPP-IV regulates and maintains ... ...
Abstract | Dipeptidyl peptidase IV (DPP-IV) is an integrated type II transmembrane protein that reduces endogenous insulin contents and increases plasma glucose levels by hydrolyzing glucagon-like peptide-1 (GLP-1). Inhibition of DPP-IV regulates and maintains glucose homeostasis, making it an attractive drug target for the treatment of diabetes II. Natural compounds have tremendous potential to regulate glucose metabolism. In this study, we examined the DPP-IV inhibitory activity of a series of natural anthraquinones and synthetic structural analogues on DPP-IV using fluorescence-based biochemical assays. The inhibitory efficiency differed among anthraquinone compounds with different structures. Alizarin (7), aloe emodin (11), emodin (13) emerged the outstanding inhibitory potential for DPP-IV with IC |
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MeSH term(s) | Humans ; Dipeptidyl-Peptidase IV Inhibitors/pharmacology ; Dipeptidyl-Peptidase IV Inhibitors/chemistry ; Dipeptidyl-Peptidase IV Inhibitors/therapeutic use ; Diabetes Mellitus, Type 2/drug therapy ; Molecular Docking Simulation ; Emodin/pharmacology ; Emodin/therapeutic use ; Molecular Structure ; Hypoglycemic Agents/pharmacology ; Structure-Activity Relationship ; Dipeptidyl Peptidase 4/chemistry ; Dipeptidyl Peptidase 4/metabolism |
Chemical Substances | Dipeptidyl-Peptidase IV Inhibitors ; Emodin (KA46RNI6HN) ; Hypoglycemic Agents ; Dipeptidyl Peptidase 4 (EC 3.4.14.5) |
Language | English |
Publishing date | 2023-05-25 |
Publishing country | Netherlands |
Document type | Journal Article |
ZDB-ID | 412385-2 |
ISSN | 1873-6971 ; 0367-326X |
ISSN (online) | 1873-6971 |
ISSN | 0367-326X |
DOI | 10.1016/j.fitote.2023.105549 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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