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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      
Yazarlar
Parham Taslimi
Türkiye
Doç. Dr. Hatice Esra DURAN
Türkiye
Yeliz Demir
Ardahan Üniversitesi, Türkiye
Necla Öztaşkın
Türkiye
Ahmet Maraş
Atatürk Üniversitesi, Türkiye
İlhami Gülçin
Atatürk Üniversitesi, Türkiye
Şükrü Beydemir
Anadolu Üniversitesi, Türkiye
Süleyman Göksu
Atatürk Üniversitesi, Türkiye
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 K value of 1.09 ± 0.29 μM while compound 2d showed highest inhibitory activity against AR with a K 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 K values in the range of 14.44 ± 0.88-43.53 ± 9.06 nM, and IC values in the range of 11.72-46.11 nM. Also, inhibition of the α-amylase enzyme, which determined an effective inhibition profile with IC values, is in the range of 3.84-29.61 nM.
Anahtar Kelimeler
alpha-Amylase,alpha-Glycosidase,Aldose reductase,Bromophenols,Diarylmethanons
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı International Journal of Biological Macromolecules
Dergi ISSN 0141-8130
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce
Basım Tarihi 11-2018
Cilt No 119
Sayfalar 857 / 863
Doi Numarası 10.1016/j.ijbiomac.2018.08.004
Makale Linki https://linkinghub.elsevier.com/retrieve/pii/S0141813018328460