Biological effects of bis-hydrazone compounds bearing isovanillin moiety on the aldose reductase
Yazarlar (8)
Gönül Yapar
Türkiye
Doç. Dr. Hatice Esra DURAN
Kafkas Üniversitesi, Türkiye
Nebih Lolak
Türkiye
Süleyman Akocak
Türkiye
Cüneyt Türkeş
Türkiye
Mustafa Durgun
Türkiye
Mesut Işık
Bilecik Şeyh Edebali Üniversitesi, Türkiye
Şükrü Beydemir
Anadolu Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | BIOORGANIC CHEMISTRY (Q1) | ||
| Dergi ISSN | 0045-2068 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | Türkçe | Basım Tarihi | 12-2021 |
| Cilt / Sayı / Sayfa | 117 / 0 / 105473–0 | DOI | 10.1016/j.bioorg.2021.105473 |
| Makale Linki | http://dx.doi.org/10.1016/j.bioorg.2021.105473 | ||
| Özet |
| Aldose reductase (ALR2), one of the metabolically important enzymes, catalyzes the formation of sorbitol from glucose in the polyol pathway. ALR2 inhibition is required to prevent diabetic complications. In the present study, the novel bis-hydrazone compounds bearing isovanillin moiety (GY1-12) were synthesized, and various chromatographic methods were applied to purify the ALR2 enzyme. Afterward, the inhibitory effect of the synthesized compounds on the ALR2 was screened in vitro. All the novel bis-hydrazones demonstrated activity in nanomolar levels as AR inhibitors with IC and K values in the range of 12.55-35.04 nM, and 13.38-88.21 nM, respectively. Compounds GY-11, GY-7, and GY-5 against ALR2 were identified as the highly potent inhibitors, respectively, and were superior to the standard drug, epalrestat. Moreover, a comprehensive ligand-receptor interactions prediction was performed using ADME-Tox, Glide XP, and MM-GBSA modules of Schrödinger Small-Molecule Drug Discovery Suite to elucidate the novel bis-hydrazone derivatives, potential binding modes versus the ALR2. As a result, these compounds with ALR2 inhibitory effects may be potential alternative agents that can be used to treat or prevent diabetic complications. |
| Anahtar Kelimeler |
| Aldose reductase | Bis-hydrazones | Epalrestat | In silico study | ADME-Tox |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 64 |
| Google Scholar | 75 |