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Screening inhibitory effects of selected flavonoids on human recombinant aldose reductase enzyme:in vitroandin silicostudy
- Publication Year :
- 2022
- Publisher :
- Taylor & Francis Ltd, 2022.
-
Abstract
- Aldose reductase (AR) is the first enzyme of the polyol pathway that has physiological importance under hyperglycaemic conditions. The article has been focussed on AR enzyme inhibition by selected compounds. For this purpose, thein vitroinhibitory effects of various compounds on commercially available recombinant human AR (rAR) enzyme activity were investigated. The IC(50)values of compounds on rAR inhibition effect were found for 6-hydroxy flavone, syringic acid, diosmetin, 6-fluoroflavone, 7-hydroxy-4 '-nitroisoflavone, myricetin as 2.05, 2.97, 15.75, 16.1, 49.5, and 63 mu M, respectively. 6-Hydroxy flavone and syringic acid competitively inhibited rAR with respect to the NADPH with K(i)values 0.509 +/- 0.036 and 0.842 +/- 0.012 mu M. In addition, docking studies were performed to evaluate the potential enzyme binding positions of the compounds. Ourin vitroandin silicoresults indicated that the 6-hydroxy flavone may be a good lead compound in the development of AR inhibitors to prevent diabetic complications.<br />Agri Ibrahim Cecen University Scientific Research [SYO.18.003]<br />This study was financially supported by Agri Ibrahim Cecen University Scientific Research [Project number: SYO.18.003].
- Subjects :
- Physiology
Aldose reductase
030209 endocrinology & metabolism
Pathogenesis
03 medical and health sciences
chemistry.chemical_compound
Lens
0302 clinical medicine
Polyol pathway
Ellagic Acid
Physiology (medical)
Dietary Flavonoids
flavonoid
Polyol Pathway
chemistry.chemical_classification
Glycation
biology
Toxicity
Prevention
Phenolic-Compounds
General Medicine
Syringic acid
Diosmetin
Enzyme assay
inhibition
Enzyme binding
Enzyme
chemistry
Biochemistry
In-Vitro
030220 oncology & carcinogenesis
docking
biology.protein
Myricetin
phenolic
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....9f679aacdffd6dab3c9504e1811c43b8