title: The inhibitory effect of Isoflavones isolated from Caesalpinia pulcherrima on aldose reductase in STZ induced diabetic rats.
abstract: Increased aldose reductase activity has been implicated in the development of retinopathy due to accumulation of intracellular sugar alcohol, i.e., sorbitol. In this study, the compounds isolated from the Caesalpinia pulcherrima, have been examined for its inhibitory effects on aldose reductase (AR), which plays a major role in diabetic retinopathy. 3,6,7,4',5'-Pentamethoxy-5,3'-dihydroxyflavone (Compound 2) has shown significant inhibition of rat retina AR with an IC50 value of 16.24±0.046μM in a non-competitive manner. Molecular docking study results are steady with the pattern of AR inhibition by Compound 2 and its specificity. The supplementation of Compound 2 suppresses sorbitol accumulation in retina by decreased AR activity in STZ induced diabetic rat in dose dependent manner. Besides this, rats fed with Compound 2 have shown improved levels of antioxidant enzymes. This study revealed that Compound 2 has pharmacologically active component with a potential to inhibit rat retina AR and affecting the delaying process of diabetic retinopathy in STZ induced diabetic rats.
authors.affiliation: Department of Zoology, Osmania University, Hyderabad 500 007, India.
authors.forename: Munipally Praveen
authors.initials: MP
authors.lastname: Kumar
authors.affiliation: Department of Zoology, Osmania University, Hyderabad 500 007, India.
authors.forename: Venu
authors.initials: V
authors.lastname: Sankeshi
authors.affiliation: National Institute of Nutrition, Hyderabad 500 007, India.
authors.forename: R Ravindar
authors.initials: RR
authors.lastname: Naik
authors.affiliation: Indian Institute of Chemical Technology (IICT), Hyderabad 500 007, India.
authors.forename: P
authors.initials: P
authors.lastname: Thirupathi
authors.affiliation: Indian Institute of Chemical Technology (IICT), Hyderabad 500 007, India.
authors.forename: Biswanath
authors.initials: B
authors.lastname: Das
authors.affiliation: Department of Zoology, Osmania University, Hyderabad 500 007, India. Electronic address: rajutn57@gmail.com.
authors.forename: T N
authors.initials: TN
authors.lastname: Raju
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000201:enzymology*; D003930:Diabetic Retinopathy / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D007887:Fabaceae / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D007529:Isoflavones / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008297:Male; D062105:Molecular Docking Simulation; D051381:Rats; D012160:Retina / Q000201:enzymology; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared; D013311:Streptozocin
chemical_list: D004791:Enzyme Inhibitors; D007529:Isoflavones; D013311:Streptozocin; D000449:Aldehyde Reductase
keywords: Aldose reductase; Aldose reductase inhibitors; Diabetic retinopathy; Enzyme kinetics and molecular docking; Oxidative stress