Diarylmethanon, bromophenol and diarylmethane compounds: Discovery of potent aldose reductase, α-amylase and α-glycosidase inhibitors as new therapeutic approach in diabetes and functional hyperglycemia
International Journal of Biological Macromolecules, cilt.119, ss.857-863, 2018 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 119
- Basım Tarihi: 2018
- Doi Numarası: 10.1016/j.ijbiomac.2018.08.004
- Dergi Adı: International Journal of Biological Macromolecules
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.857-863
- Anahtar Kelimeler: Aldose reductase, Bromophenols, Diarylmethanons, α-Amylase, α-Glycosidase
- Bilecik Şeyh Edebali Üniversitesi Adresli: Evet
Özet
Diabetes mellitus (DM) is a chronic metabolic disease in which there are high blood sugar levels over a prolonged period. Aldose reductase (AR) belongs to aldo-keto reductase superfamily and plays a key role in the polyol pathway. α-Glycosidase and α-amylase are important enzymes in glucose metabolism. In this study, AR was purified from purified from cow liver. The enzyme was obtained with 139.17 purification fold and with a specific activity of 1.67 EU/mg protein. Then, it is observed the inhibition effect of diarylmethanons (1a–d), bromophenols (2a–d and 4a–d) and diarylmethanes (3a–d) on aldose reductase, α-glycosidase and α-amylase enzymes. In these series, compound 2a showed lowest inhibitory activity against AR with a Ki value of 1.09 ± 0.29 μM while compound 2d showed highest inhibitory activity against AR with a Ki value of 0.092 ± 0.015 μM. Additionally, α-glycosidase and α-amylase enzymes were easily inhibited by these compounds. All compounds were tested for their inhibition effects against of α-glycosidase enzyme and demonstrated efficient inhibition profiles with Ki values in the range of 14.44 ± 0.88–43.53 ± 9.06 nM, and IC50 values in the range of 11.72–46.11 nM. Also, inhibition of the α-amylase enzyme, which determined an effective inhibition profile with IC50 values, is in the range of 3.84–29.61 nM.