Sürdürülebilir Kalkınma Amaçları
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.
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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 Erişim2020Scopus SJRQ4Effects of race, gender, body condition score and pregnancy on serum apelin levels in ewe
Bayraktar, Bülent; Tekce, Emre; Aksakal, Vecihi; Takma, Çiğdem; Bayraktar, Fatma Gülten; Şengül, Bülent
Apelin is an important adipokine hormone that is released from adipose tissue, which is considered as the energy store of the body, which plays a role in many physiological processes in the body, as well as cardiovascular, immune functions and energy, nutrients and fluid metabolism. In this study, it was aimed to determine the effect of lactation, pregnancy and gender on apelin hormone levels in blood serums belonging to different races of ewe. In the present study, the hormone levels of the pregnant, non-pregnant ewe and rams of the Akkaraman Kangal and Morkaraman races were thin, with different body condition scores (<2, 3 to 3.5 and ≥4). Apelin hormone level was determined by ELISA technique in blood serum samples of ewe's Jugular vein. It was determined that there was a difference in body scores between races and the interaction between race and body score was important (P<0.05). Apelin level in ewe in lactation and pregnant ewe did not change according to body condition scores (P>0.05). In terms of apelin, gender and body condition score, race and gender, and body condition score interactions were found to be significant.
AtıfScopus6WoS6OpenAlex4TR Dizin2İncele - MakaleYalnız künye2018Scopus SJRQ2The interactions of cephalosporins on polyol pathway enzymes from sheep kidney
Şengül, Bülent; Beydemir, Şükrü
Context: Cephalosporins are derived from the fungus Acremonium. Due to their strong bactericidal ability, these drugs have to a wide usage in medicine. Objective: An investigation of the effects on sheep renal aldose reductase (AR) and sorbitol dehydrogenase (SDH) of cefoperazone, cefazolin, cefuroxime, ceftazidime and ceftriaxone as cephalosporin drugs was carried out in the present study. Methods: AR and SDH were purified from sheep kidney by ion exchange, gel filtration and affinity methods with approximately 219- and 484-fold, respectively. Some kinetic properties of the enzymes were determined such as optimal pH, optimal ionic strength, optimal temperature, stable pH, Km and Vmax. IC50 values of the drugs were found for each enzyme. Results: While the AR was inhibited by all drugs, SDH enzyme was inhibited by only CXM (IC50 8.10 mM). Interestingly, CZO activated SDH enzyme. This result was evaluated as important for the flow of the polyol reactions. Ki values and inhibition types were determined for AR. However, these values could not have determined for SDH, due to insufficient inhibition. Conclusions: From these results, it was concluded that cephalosporins may have an important effect on flow of the polyol metabolism.
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İncele - 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.
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