AI Article Synopsis
- Type 2 diabetes is a major global health issue, costing over 800 billion USD annually, prompting the search for better anti-diabetic treatments, including coumarins with potential glucose-lowering effects.
- The study focuses on designing and testing new 7-hydroxy coumarin derivatives for their hypoglycemic activity, utilizing in-silico methods to investigate their pharmacological potential against type 2 diabetes.
- Results showed that the synthesized coumarin derivatives displayed strong molecular interactions with the GLP-1 receptor and confirmed their chemical structures, indicating promising hypoglycemic effects worth further exploration.
Article Abstract
Background: Worldwide, type 2 diabetes mellitus accounts for a considerable burden of disease, with an estimated global cost of >800 billion USD annually. For this reason, the search for more effective and efficient therapeutic anti-diabetic agents is continuing. Recent studies support the search for coumarins or related compounds with potential blood glucose-lowering properties.
Aim: The study aims to design, synthesize and evaluate the hypoglycemic activity of a new class of 7-hydroxy coumarin derivatives.
Objective: To explore and establish the in-silico-driven pharmacological role of a new class of 7- hydroxy coumarin derivatives as the therapeutic strategies against type 2 diabetes mellitus.
Methods: A new class of 7-hydroxy coumarin derivatives was designed by assessment of their physicochemical properties and molecular docking against the Glucagon-like peptide-1 (GLP-1) receptor. Two novel series of 30 compounds were synthesized. The chemical structures of all the synthesized analogues have been elucidated by spectral studies of IR, H-NMR, and mass spectroscopy. After considering the molecular docking score and their physicochemical properties, the compounds were screened out for the evaluation of their hypoglycemic potential. The compounds were investigated for their hypoglycemic activity using a streptozotocin (STZ) induced diabetic model and an oral glucose tolerance test (OGTT) method at different dose levels.
Results: The molecular docking studies of synthesized derivatives reveal significant molecular interaction with the various amino acid residues of the GLP-1 receptor. IR spectral analysis revealed a strong band of -NH stretching in the range of 3406.7-3201.61 cm and one strong band for the lactone carbonyl group of the coumarin ring in the range of 1722.0-1703.5 cm, confirming the chemical structure of all produced compounds. The synthesized coumarin analogues with the best docking score exhibited remarkable hypoglycemic potential as assessed by the STZ model and the OGTT method.
Conclusion: Coumarin derivatives explored a good structure-activity relationship (SAR) and produced significant hypoglycemic potential.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2174/0929866529666220829090810 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Design, synthesis and antiviral evaluation of triazole-linked 7-hydroxycoumarin-monoterpene conjugates as inhibitors of RSV replication.
RSC Med Chem
December 2024
Department of Medicinal Chemistry, N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry 9, Akademika Lavrentieva Ave. 630090 Novosibirsk Russia
Respiratory syncytial virus (RSV) is the leading cause of acute lower respiratory infections in babies across the world. Irrespective of progress in the development of RSV vaccines, effective small molecule drugs are still not available on the market. Based on our previous data we designed and synthesized triazole-linked coumarin-monoterpene hybrids and showed that they are indeed effective in inhibiting the RSV replication.
View Article and Find Full Text PDFSupramolecular Control of the Photoisomerization of a Coumarin-Based Photoswitch.
ACS Omega
December 2024
Department of Physical Chemistry and Materials Science, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem rkp. 3, 1111 Budapest, Hungary.
The complex formation of the cationic stilbene-type photoswitch CP with the anionic macrocycles carboxylato-pillar[5]arene (WP5) and carboxylato-pillar[6]arene (WP6) has been investigated in aqueous solution by optical spectroscopic, NMR and isothermal calorimetric experiments and theoretical calculations. Subsequently, the photoisomerization reactions of the supramolecular complexes formed have been studied. CP consists of a 7-diethylamino-coumarin fluorophore and an -methylpyridinium unit, which are connected via an ethene bridge.
View Article and Find Full Text PDFA comprehensive investigation of Clerodendrum Infortunatum Linn. using LC-QTOF-MS/MS metabolomics as a promising anti-alzheimer candidate.
Sci Rep
January 2025
Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.
Alzheimer's disease (AD) poses a global health challenge, demanding innovative approaches for effective treatments. Clerodendrum infortunatum Linn. (Lamiaceae) is a shrub traditionally used as a medicinal plant to treat inflammation, skin diseases, and bronchitis.
View Article and Find Full Text PDFUltrasound-assisted extraction and value of active substances in Muxu.
Ultrason Sonochem
January 2025
Key Laboratory of Carbohydrate Science and Engineering, Chongqing Key Laboratory of Inorganic Functional Materials, Chongqing Normal University, Chongqing 401331, PR China. Electronic address:
This article reviews the latest research progress on ultrasound-assisted extraction of active substances from Muxu, including polysaccharides, polyphenols, leaf proteins, anthocyanins, total flavonoids, and total saponins, in order to provide theoretical references for the extraction of active substances from Muxu. At the same time, its medicinal value, feeding value, ecological value, edible value, and ornamental value were analyzed and summarized. Flavonoids, saponins, and polysaccharides in the bioactive substances of Muxu have good effects on improving animal productivity, enhancing immune function, and improving animal health.
View Article and Find Full Text PDFIndole and Coumarin Derivatives Targeting EEF2K in Aβ Folding Reporter Cells.
J Neurochem
January 2025
Department of Neurology, Chang Gung Memorial Hospital, Chang Gung University College of Medicine, Taoyuan, Taiwan.
Misfolding and accumulation of amyloid-β (Aβ) in the brains of patients with Alzheimer's disease (AD) lead to neuronal loss through various mechanisms, including the downregulation of eukaryotic elongation factor 2 (EEF2) protein synthesis signaling. This study investigated the neuroprotective effects of indole and coumarin derivatives on Aβ folding and EEF2 signaling using SH-SY5Y cells expressing Aβ-green fluorescent protein (GFP) folding reporter. Among the tested compounds, two indole (NC009-1, -6) and two coumarin (LM-021, -036) derivatives effectively reduced Aβ misfolding and associated reactive oxygen species (ROS) production.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!