Sürdürülebilir Kalkınma Amaçları
Yazarlar
Yayınlar
- MakaleAçık Erişim2024Scopus SJRQ2Antioxidant properties and aldose reductase inhibitory potency of Viscum album L. extracts: experimental and computational insights
Akyüz, Bilal; Şengül, Bülent
This study systematically investigates the antioxidant capacity and inhibitory impact of Viscum album L. plant extracts on the aldose reductase (AR) enzyme through a combined approach of in vitro and in silico methods. Various sections derived from distinct plant parts were examined, revealing potent inhibitory potential. Notably, the methanol extract sourced from the plant’s stem displayed remarkable efficacy with an IC50 value of 0.156 µM. Total phenolic content and antioxidant capacity analyses were conducted, highlighting variations across plant parts and solvent types. Qualitative and quantitative phenolic compound content in the extracts was elucidated by LC-MS/MS analysis, revealing higher levels of quinic acid, fumaric acid, and chlorogenic acid. Molecular docking studies further substantiated the inhibitory roles of key compounds like chlorogenic acid and fumaric acid, elucidating their interactions with specific amino acid residues within the AR enzyme’s active site and shedding light on the underlying mechanisms. Collectively, this study underscores Viscum album L. extracts as promising candidates for aldose reductase modulation. By merging experimental and computational techniques, the study presents a holistic understanding of natural compound interactions, potentially influencing drug development and herbal therapeutics.
AtıfScopus4WoS4OpenAlex4
İncele - MakaleYalnız künye2024Scopus SJRQ3Exploring the Potential of Isoindole-1,3-Dione Derivatives as Novel Inhibitors of Aldose Reductase: An In Silico and In Vitro Insight into Therapeutic Strategies for Diabetic Complications
Şengül, Bülent; Gündoğdu, Özlem; Kilinç, Namık; Kishali, Nurhan
This study explores the potential of isoindole-1,3-dione derivatives as novel inhibitors of aldose reductase (AR), focusing on their in silico and in vitro effects for therapeutic strategies against diabetic complications. Aldose reductase, a critical enzyme in the polyol pathway, plays a significant role in glucose metabolism and has been linked to diabetic complications. In this comprehensive study, isoindole-1,3-dione derivatives were synthesized and evaluated for their inhibitory effects on the recombinant human AR enzyme. The compounds’ inhibitory activities were measured both in vitro and through in silico techniques, employing molecular docking and free binding energy calculations and ADME studies. The newly synthesized compounds demonstrated varied inhibitory effects, with ethyl and phenyl substituents at specific positions enhancing inhibitory activity. Notably, compounds with carboxylic acid derivatives exhibited potent inhibitory effects, especially compound 6 with an IC50 value of 1.649 μM. In conclusion, this study provides valuable insights into the inhibitory potential of isoindole-1,3-dione derivatives against AR, suggesting their potential therapeutic application in mitigating diabetic complications. The combination of experimental and computational approaches offers a comprehensive understanding of the compounds’ interaction mechanisms and pharmacokinetic profiles, supporting their further exploration as antidiabetic agents.
- MakaleAçık Erişim2017Scopus SJRQ1Inhibition behaviours of some phenolic acids on rat kidney aldose reductase enzyme: an in vitro study
Alim, Zuhal; Kilinç, Namik; Şengül, Bülent; Beydemir, Şükrü
Aldose reductase (AR) inhibitors have vital importance in the treatment and prevention of diabetic complications. In this study, rat kidney AR was purified 19.34-fold with a yield of 3.49% and a specific activity of 0.88 U/mg using DE-52 Cellulose anion exchange chromatography, gel filtration chromatography and 2′5′ ADP Sepharose-4B affinity chromatography, respectively. After purification, the in vitro inhibition effects of some phenolic acids (tannic acid, chlorogenic acid, sinapic acid, protocatechuic acid, 4-hydroxybenzoic acid, p-coumaric acid, ferulic acid, vanillic acid, syringic acid, α-resorcylic acid, 3-hydroxybenzoic acid and gallic acid) were investigated on purified enzyme. We determined IC50, Ki values and inhibition types of these phenolic acids. As a result, tannic and chlorogenic acid had a strong inhibition effect. On the other hand, gallic acid had a weak inhibition effect. In this study, all phenolic acids except for chlorogenic acid and p-coumaric acid showed non-competitive inhibition effects on rat kidney AR.
AtıfScopus61WoS60OpenAlex64
İncele - MakaleYalnız künye2017Scopus SJRQ2Mechanism of capsaicin inhibition of aldose reductase activity
Alim, Zuhal; Kilinc, Namık; Sengul, Bulent; Beydemir, Sukru
Aldose reductase (AR) inhibitors play a vital importance as a potential therapeutic and preventive medicine when it comes to hyperglycemia associated diabetic complications. Additionally, capsaicin is used as a food additive and a drug in a number of diverse clinical trials. The aim of this study is to determine the in vitro inhibition behavior of capsaicin on AR enzyme activity, which was obtained from different rat tissues (heart, kidney, liver, and brain). We showed that AR was inhibited by capsaicin in the micromolar range and noncompetitive manner in all of the tissues. Ki values of capsaicin were found to be 8.87, 264, 535, and 597, respectively, in heart AR, kidney AR, liver AR, and brain AR. In conclusion, capsaicin may be an effective molecule when used in low concentrations to prevent diabetic complications associated with the polyol pathway.
AtıfScopus21WoS19OpenAlex24İncele