Sürdürülebilir Kalkınma Amaçları

• 3

• MakaleAçık Erişim2017Scopus SJRQ1/r/bayburt/13817
  Inhibition 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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  AtıfScopus61·WoS60·OpenAlex64

  İncele
• MakaleYayıncıda açık erişim2015Scopus SJRQ1/r/bayburt/13858
  Human serum paraoxonase-1 (hPON1): In vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium

  Türkeş, Cüneyt; Söyüt, Hakan; Beydemir, Şükrü

  In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. Ki constants were calculated to be 2.641 ± 0.040 mM, 5.525 ± 0.817 mM, 35.092 ± 1.093 mM, 252.762 ± 5.749 mM and 499.244 ± 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium were noncompetitive inhibitors.

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  AtıfScopus53·WoS53·OpenAlex57

  İncele
• MakaleAçık Erişim2012Scopus SJRQ2/r/bayburt/13975
  Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products

  Balaydiin, Halis Türker; Soyut, Hakan; Ekinci, Deniz; Göksu, Sleyman; Beydemir, Şkrü; Menzek, Abdullah; Şahin, Ertan

  (2-Bromo-3,4-dimethoxyphenyl) (3,4-dimethoxyphenyl)methanone (10) and its derivatives with Br, one dibromide and isomeric three tribromides, were synthesized. Demethylation of these compounds afforded a series of new bromophenols. Inhibition of human cytosolic carbonic anhydrase II (hCA II) isozyme by these new bromophenols and naturally occurring 3,4,6-tribromo-5-(2,5- dibromo-3,4-dihydroxybenzyl)benzene-1,2-diol (3), and 5,5′-methylenebis(3, 4,6-tribromo-benzene-1,2-diol) (4) was investigated. The synthesized compounds showed carbonic anhydrase inhibitory capacities with IC 50 values in the range of 0.7372 μM against hCA II. Some bromophenols investigated here showed effective hCA II inhibitory activity and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, or osteoporosis.

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  AtıfScopus42·WoS43·OpenAlex41

  İncele