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Thiazolidinedione Derivatives: In Silico, In Vitro, In Vivo, Antioxidant and Anti-Diabetic Evaluation.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2022 Jan 27; Vol. 27 (3). Date of Electronic Publication: 2022 Jan 27. - Publication Year :
- 2022
-
Abstract
- This work aimed to synthesize a new antihyperglycemic thiazolidinedione based on the spectral data. The DFT\B3LYP\6-311G** level of theory was used to investigate the frontier molecular orbitals (FMOs), chemical reactivity and map the molecular electrostatic potentials (MEPs) to explain how the synthesized compounds interacted with the receptor. The molecular docking simulations into the active sites of PPAR- γ and α -amylase were performed. The in vitro potency of these compounds via α -amylase and radical scavenging were evaluated. The data revealed that compounds ( 4 - 6 ) have higher potency than the reference drugs. The anti-diabetic and anti-hyperlipidemic activities for thiazolidine-2,4-dione have been investigated in vivo using the alloxan-induced diabetic rat model along with the 30 days of treatment protocol. The investigated compounds didn't show obvious reduction of blood glucose during pre-treatments compared to diabetic control, while after 30 days of treatments, the blood glucose level was lower than that of the diabetic control. Compounds ( 4 - 7 ) were able to regulate hyperlipidemia levels (cholesterol, triglyceride, high-density lipoproteins and low- and very-low-density lipoproteins) to nearly normal value at the 30th day.
- Subjects :
- Animals
Diabetes Mellitus, Experimental metabolism
Molecular Structure
Rats
Structure-Activity Relationship
alpha-Amylases antagonists & inhibitors
alpha-Amylases chemistry
Diabetes Mellitus, Experimental drug therapy
Free Radical Scavengers chemical synthesis
Free Radical Scavengers chemistry
Free Radical Scavengers pharmacology
Molecular Docking Simulation
Thiazolidinediones chemical synthesis
Thiazolidinediones chemistry
Thiazolidinediones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 27
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 35164095
- Full Text :
- https://doi.org/10.3390/molecules27030830