Antidiabetic potential: In vitro inhibition effects of bromophenol and diarylmethanones derivatives on metabolic enzymes

Abstract

Aldose reductase converts glucose to sorbitol in the polyol pathway. It is an important enzyme to prevent diabetic complications. In this study, we studied the inhibitory effects of bromophenol derivatives on aldose reductase (AR), α-glucosidase, and α-amylase enzymes. In the bromophenols series, compound 1f showed the maximum inhibition effect against AR with a K i value of 0.05 ± 0.01 μM, while compound 1d showed the lowest inhibition effect against AR with a K i value of 1.13 ± 0.99 μM. In addition, α-amylase from porcine pancreas and α-glucosidase from Saccharomyces cerevisiae were used as enzymes. In this study, all compounds were tested for the inhibition of the α-glucosidase enzyme and demonstrated efficient inhibition profiles with K i values in the range of 43.62 ± 5.28 to 144.37 ± 16.37 nM against α-glucosidase.Additionally, these compounds were tested against the α-amylase enzyme, which determined an effective inhibition profile with IC 50 values in the range of 9.63-91.47 nM. These compounds can be selective inhibitors of AR, α-glucosidase, and α-amylase enzymes as antidiabetic agents. K E Y W O R D S α-amylase, α-glucosidase, aldose reductase, bromophenol, enzyme inhibition Arch Pharm Chem Life Sci. 2018;351:e1800263.wileyonlinelibrary.com/journal/ardp AR activity was assayed according to previous studies and it measured the decrease of NADPH at 340 nm spectrophotometrically. [45,46] | Enzyme purificationEnzyme purification procedures were done according to previous studies. [47,48] | Protein determinationThe protein concentration was measured according to the Bradford method by using with Coomassie Brilliant Blue G-250. [49] 4.2.7 | SDS polyacrylamide gel electrophoresisAfter the enzyme purification, the purity degree of the enzyme was controlled according to Laemmli's method [50] by using 3-8% batch sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). The electrophoresis process was carried out according to our previous papers. [51][52][53] The gel was stained with the silver staining method and photographed after staining. CONFLICT OF INTERESTThe authors declare that there are no conflicts of interest. ORCIDParham Taslimi

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