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Antidiabetic potential: In vitro inhibition effects of bromophenol and diarylmethanones derivatives on metabolic enzymes
Author(s) -
Demir Yeliz,
Taslimi Parham,
Ozaslan Muhammet Serhat,
Oztaskin Necla,
Çetinkaya Yasin,
Gulçin İlhami,
Beydemir Şükrü,
Goksu Suleyman
Publication year - 2018
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201800263
Subject(s) - aldose reductase , chemistry , enzyme , ic50 , polyol pathway , amylase , sorbitol , aldehyde reductase , biochemistry , aldose reductase inhibitor , polyol , non competitive inhibition , in vitro , stereochemistry , organic chemistry , polyurethane
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 IC 50 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.