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

Demir Y., Taslimi P., Ozaslan M. S., Oztaskin N., ÇETİNKAYA Y., GÜLÇİN İ., ...More

ARCHIV DER PHARMAZIE, vol.351, no.12, 2018 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 351 Issue: 12
  • Publication Date: 2018
  • Doi Number: 10.1002/ardp.201800263
  • Journal Name: ARCHIV DER PHARMAZIE
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Keywords: alpha-amylase, alpha-glucosidase, aldose reductase, bromophenol, enzyme inhibition, ALPHA-GLUCOSIDASE INHIBITORS, ALDOSE REDUCTASE INHIBITORS, BIOLOGICAL EVALUATION, CARBONIC-ANHYDRASE, AMYLASE, IDENTIFICATION, ANTIOXIDANT
  • Anadolu University Affiliated: Yes

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), alpha-glucosidase, and alpha-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 mu M, while compound 1d showed the lowest inhibition effect against AR with a K-i value of 1.13 +/- 0.99 mu M. In addition, alpha-amylase from porcine pancreas and alpha-glucosidase from Saccharomyces cerevisiae were used as enzymes. In this study, all compounds were tested for the inhibition of the alpha-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 alpha-glucosidase. Additionally, these compounds were tested against the alpha-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, alpha-glucosidase, and alpha-amylase enzymes as antidiabetic agents.