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

Yeliz Demir¹, Parham Taslimi¹, Muhammet Serhat Ozaslan¹

¹Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.

Archiv Der Pharmazie

|November 28, 2018

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 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

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