Sürdürülebilir Kalkınma Amaçları
Yayınlar
- MakaleYalnız künye2019Investigation of Inhibition Effect of Nitro Group Containing Substances on Glutathione Reductase Enzyme
Şentürk, Murat; Kaya, Elif Çelenk; Kaya, Afşin Ahmet
Glutathione reductase (Glutathione: NADP+ oxidoreductase, EC 1.8.1.7; GR) catalyzes electron transfer between reduced (GSH) or high molecular weight (GSSG) disulfide substrates and reduced pyridine nucleotides (NADPH). Discovery of glutathione reductase (GR) inhibitors has become very popular recently due to antimalarial and anticancer activities. Enzymatic activity was measured by Beutler’s method with a Spectrophotometer, at 25°C. The assay system contained 100 mM Tris-HCl buffer pH 8.0, including 0.5 mM EDTA, 3.3 mM GSSG and 0.1 mM NADPH. Inhibition effects of Nitrobenzene (1), 3,5- Dinitrosalicylic acid (2), (2,4-Dinitrophenyl)((4-(prop1-en-2-yl)cyclohex-1-enyl)-methyl)sulfane (3), ((7,7- dimethylbicyclo[2.2.1]heptan-1-yl)methyl)-(2,4- dinitrophenyl)sulfane (4), and ((2-Chloro-7,7- dimethylbicyclo[2.2.1]heptan-1-yl)methyl)-(2,4- dinitrophenyl)sulfane (5) compounds on GR have been investigated in vitro. IC50 values were determined by drawing % activity- [I] graphs for compounds showing inhibition effects. IC50 values of GR for these substances were observed to be at micromolar level.
- MakaleAçık Erişim2015Synthesis and determination of some biological activities of novel 2,4-dinitrophenyl derivatives
Öztürk Sarikaya, Sevim B.; Kaya, Afşin A.; Kaya, Elif C¸elenk; Şentürk, Murat
The antioxidant and radical scavenging activities of the synthesized compounds 3, 5, and 6 were determined by various in vitro assays such as 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid radical (ABTS.+) scavenging, ferric ion (Fe3+) reducing power and ferrous ion (Fe2+) chelating activities. Moreover, these activities were compared to those of standard antioxidants such as butylated hydroxyanisole, butylated hydroxytoluene, and trolox. The results showed that the new compounds (3, 5, and 6) had potential antioxidant activity. Besides, inhibition of the two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II with some nitrobenzene compounds was investigated. Compounds 1-6 showed Ki values in the range of 4.88-193.4 μM and 5.295-54.75 μM for hCA I and hCA II, respectively.
- MakaleAçık Erişim2011In vitro inhibition of α-carbonic anhydrase isozymes by some phenolic compounds
Öztürk Sarikaya, Sevim Beyza; Topal, Fevzi; Şentürk, Murat; Gülin, Ihami; Supuran, Claudiu T.
Carbonic anhydrase inhibitors (CAIs) are a class of pharmaceuticals used as antiglaucoma agents, diuretics, antiepileptics, in the management of mountain sickness, gastric and duodenal ulcers, neurological disorders or osteoporosis. We report here the inhibitory capacities of some phenolic compounds against three human CA isozymes (hCA I, hCA II, and hCA VI) and the gill carbonic anhydrase of the teleost fish Dicentrarchus labrax (European seabass) (dCA). The isozymes showed quite diverse inhibition profiles with these compounds. These data may lead to design novel CAIs with a diverse inhibition mechanism compared to sulfonamide/sulfamate inhibitors.