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• MakaleAçık Erişim2024Scopus SJRQ2/r/bayburt/12901
  Antioxidant 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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  AtıfScopus4·WoS4·OpenAlex4

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• MakaleYalnız künye2024Scopus SJRQ3/r/bayburt/11620
  Exploring 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.

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  İncele
• MakaleAçık Erişim2023/r/bayburt/16564
  Benzaldehit türevlerinin sığır böbrek aldoz redüktaz inhibitörleri olarak değerlendirilmesi

  Sengül, Bülent

  Aldoz redüktaz (AR), poliol yolunda glikozdan sorbitol üretimini katalize eder ve insülinden bağımsız dokularda anormal sorbitol agregasyonuna neden olan, retinopati, nöropati ve nefropati gibi bazı problemler yaratan kritik bir enzimdir. AR inhibisyonunun bu yan etkileri azaltmak için uygun bir yaklaşım olduğu gösterilmiştir. Mevcut çalışma, literatüre yeni AR inhibitörlerini tanıtmayı amaçlamıştır. Bu amaçla AR inhibitörleri olarak benzaldehitler incelenmiştir. İlk olarak sığır böbreğinden homojenat hazırlanmış, ardından inhibisyon çalışmaları yapılmıştır. Çalışılan bütün benzaldehit türevlerinin AR'yi inhibe ettiği bulundu. 0,23 ve 1,37 μM IC50 değerlerine sahip olan 4- Phenyl benzaldehyde (3) ve 2- Bromobenzaldehyde (6)'in inhibitör aktivitesi, standart inhibitör sorbinilden daha yüksek olduğu tespit edildi. In vitro inhibisyon çalışmalarından sonra, tahmini bağlanma enerjileri ve türevlerin enzime bağlanma modları moleküler docking ile tahmin edildi. Bileşik 3, -8,61 kcal/mol'lük bir maksimum yerleştirme puanı sergiledi. Sonuç olarak, bu bileşikler, özellikle bileşik 3, diyabetik komplikasyonların tedavisinde veya önlenmesinde yeni ilaç aday moleküllerinin sentezi için yol gösterici moleküller olabilir.

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  AtıfOpenAlex3·TR Dizin1

  İncele
• DüzeltmeYalnız künye2023/r/bayburt/16503
  Düzeltilmiş: Benzaldehit türevlerinin sığır böbrek aldoz redüktaz inhibitörleri olarak değerlendirilmesi

  Sengül, Bülent

  Aldoz redüktaz (AR), poliol yolunda glikozdan sorbitol üretimini katalize eder ve insülinden bağımsız dokularda anormal sorbitol agregasyonuna neden olan, retinopati, nöropati ve nefropati gibi bazı problemler yaratan kritik bir enzimdir. AR inhibisyonunun bu yan etkileri azaltmak için uygun bir yaklaşım olduğu gösterilmiştir. Mevcut çalışma, literatüre yeni AR inhibitörlerini tanıtmayı amaçlamıştır. Bu amaçla AR inhibitörleri olarak benzaldehitler incelenmiştir. İlk olarak sığır böbreğinden homojenat hazırlanmış, ardından inhibisyon çalışmaları yapılmıştır. Çalışılan bütün benzaldehit türevlerinin AR'yi inhibe ettiği bulundu. 0,23 ve 1,37 μM IC50 değerlerine sahip olan 4- Phenyl benzaldehyde (3) ve 2- Bromobenzaldehyde (6)'in inhibitör aktivitesi, standart inhibitör sorbinilden daha yüksek olduğu tespit edildi. In vitro inhibisyon çalışmalarından sonra, tahmini bağlanma enerjileri ve türevlerin enzime bağlanma modları moleküler docking ile tahmin edildi. Bileşik 3, -8,61 kcal/mol'lük bir maksimum yerleştirme puanı sergiledi. Sonuç olarak, bu bileşikler, özellikle bileşik 3, diyabetik komplikasyonların tedavisinde veya önlenmesinde yeni ilaç aday moleküllerinin sentezi için yol gösterici moleküller olabilir.

  İncele
• MakaleAçık Erişim2020Scopus SJRQ4/r/bayburt/13314
  Effects 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.

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  AtıfScopus6·WoS6·OpenAlex4·TR Dizin2

  İncele
• MakaleYalnız künye2018/r/bayburt/15288
  Evaluation of Inhibition Effects of Some Cardiovascular Therapeutics on Human Erythrocyte Carbonic Anhydrase Isoenzymes

  Isgor, Mehmet Mustafa; Kılınç, Namık; Alim, Zuhal; Beydemir, Şükrü; Sengül, Bülent

  Carbonic anhydrase enzyme plays a vital role in metabolic events such as acid-base regulation and respiration. Inour research, it is tried to determine the inhibitory influences of the cardiovascular therapeutics esmololhydrochloride, amiodarone hydrochloride and lidocaine hydrochloride on human erythrocytes carbonic anhydrases(hCA I and II). In accordance with this purpose, carbonic anhydrase isoenzymes were purified from humanerythrocytes by using affinity chromatography method. Enzyme purity was checked by SDS-PAGEelectrophoresis method. After the carbonic anhydrase enzymes were purified, the inhibitory affects ofcardiovascular therapeutics on these enzymes, using esterase activity, which is the method of measuring in vitroactivity, were examined. The three cardiovascular therapeutics dose-dependently decreased activity of hCAs. IC50values of amiodarone hydrochloride, esmolol hydrochloride and lidocaine hydrochloride were found to be,respectively, 0.91 mM, 5 mM, 5.8 mM for hCA-I and 0.41 mM, 3.5 mM, and 6.36 mM for hCA-II. Our resultsproved that, under in vitro conditions, cardiovascular therapeutics significantly inhibit human CA-I and IIactivities. So, irregular use of these medicines may cause serious adverse effects in terms of human health.

  AtıfTR Dizin2

  İncele
• MakaleYalnız künye2018Scopus SJRQ4/r/bayburt/15223
  Gökkuşağı Alabalığı (Oncorhynchus mykiss) İşletmelerinde Bazı Antioksidan Enzim Aktivitelerinin Ağır Metal İnhibisyonlarının Araştırılması

  Önalan, Şükrü; Demir, Yeliz; Sengül, Bülent

  Endüstriyel, tarımsal ve ticari kimyasalların, sucul ekosistemlerde meydana getirdiği kirlilik, giderek artanciddi bir problemdir. Çevresel kirleticiler, sucul organizmalarda çeşitli zararlı etkilere neden olur. Balıklar, suculorganizmalar arasında ağır metallere en çok maruz kalan türlerdir. Ağır metallerin balıklarda birikmesi balıkhastalıkları konusunda önemli bir sorun olmanın yanında, oksidatif stres sebebi olan reaktif oksijen türlerinin(ROT) artmasına da neden olmaktadır. Biyolojik sistemlerde oksidatif strese bağlı reaktif oksijen türlerindekiartış antioksidan savunma sistemlerinde hasara yol açar. Bu çalışmanın amacı gökkuşağı alabalık çiftliklerindeüretimi yapılan balıkların karaciğer, böbrek ve solungaç dokularındaki bazı antioksidan enzim aktiviteleri ileağır metal iyonlarından kaynaklanan su kirliliği arasındaki ilişkiyi ortaya koymaktır. Bu amaçla; Suörneklerindeki ağır metal iyonlarının (Zn, Fe, Cu, Ni, Co, Hg, As, Mn) seviyeleri belirlenerek, bu iyonlarınbalıklardan alınan kalp, karaciğer ve solungaç dokularındaki antioksidan enzimlerin (Süperoksid dismutaz(SOD), Katalaz (CAT), Glutatyon redüktaz (GR), Glutatyon S-transferaz (GST), Glutatyon peroksidaz (GPx))aktiviteleri üzerine etkileri incelenmiştir.

  İncele
• MakaleYalnız künye2018Scopus SJRQ2/r/bayburt/12249
  The 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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  AtıfScopus12·WoS12·OpenAlex13

  İncele
• BildiriAçık Erişim2017Scopus SJRQ1/r/bayburt/14215
  Determination of the Antigenotoxic effects of Evernic acid against genotoxic effects of CCL4 on HUVEC lines

  Agar, Guleray; Kizil, Hamit Emre; Ceker, Selcuk; Capik, Ozel; Sengul, Bulent

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  İncele
• MakaleYalnız künye2017/r/bayburt/15321
  Alcohol Dehydrogenase from Sheep Liver: Purification, Characterization and Impacts of Some Antibiotics

  Demir, Yeliz; Ergun, Bülent; Beydemir, Şükrü; Sengül, Bülent

  Alcohol dehydrogenase (ADH) is a dimeric enzyme in which each subunit of the enzyme has a Zn2+metal-containing catalytic domain and a cofactor-binding domain. This enzyme converts the alcohol to aldehyde. The present article focuses on the purification, characterization and in vitro effects of some antibiotics on alcohol dehydrogenase from sheep liver. ADH was purified with specific activity of 0.5 U/mg proteins and approximately 52.03-fold from sheep liver by DEAE-Sephadex A-50 ion exchange chromatography and gel filtration on Sephadex G-100. The subunit and the natural molecular weights of the enzyme were determined by gel filtration and SDSPAGE 38.16 kDa and 80.49 kDa, respectively. The optimum ionic strenght, temperature and pH of ADH were found 400 mM, 40 °C and 10.5, respectively. The inhibitory effects of the antibiotics were tested at various concentrations. IC values for kanamycin sulfate, amikacin sulfate, gentamicin, lincomycin, and clindamycin were found to be 43.31, 36.47, 20.38, 18.73 and 1.31 mM, respectively

  AtıfTR Dizin2

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