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

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, compound1f showed the maximum inhibition effect against AR with aKi value of 0.05  ± 0.01 μM, while compound1d showed the lowest inhibition effect against AR with aKi value of 1.13  ± 0.99 μM. In addition, α‐amylase from porcine pancreas and α‐glucosidase fromSaccharomyces 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 withKi 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.

Source: Archiv der Pharmazie - November 27, 2018 Category: Drugs & Pharmacology Authors: Yeliz Demir, Parham Taslimi, Muhammet Serhat Ozaslan, Necla Oztaskin, Yasin Çetinkaya, İlhami Gulçin, Şükrü Beydemir, Suleyman Goksu Tags: FULL PAPER Source Type: research