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 Ki value of 0.05 ± 0.01 μM, while compound 1d showed the lowest inhibition effect against AR with a Ki 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 Ki 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 IC50 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.
Keywords: aldose reductase; bromophenol; enzyme inhibition; α-amylase; α-glucosidase.
© 2018 Deutsche Pharmazeutische Gesellschaft.