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

Demır Y., Taslımı P., Ozaslan M. S., Öztaşkın N., Çetinkaya Y., Gülçin İ., ...Daha Fazla

ARCHIV DER PHARMAZIE, cilt.351, sa.12, 2018 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 351 Sayı: 12
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1002/ardp.201800263
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Anahtar Kelimeler: alpha-amylase, alpha-glucosidase, aldose reductase, bromophenol, enzyme inhibition, ALPHA-GLUCOSIDASE INHIBITORS, ALDOSE REDUCTASE INHIBITORS, BIOLOGICAL EVALUATION, CARBONIC-ANHYDRASE, AMYLASE, IDENTIFICATION, ANTIOXIDANT
  • Atatürk Üniversitesi Adresli: Evet

Özet

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.