Alcohol Dehydrogenase from Sheep Liver: Purification, Characterization and Impacts of Some Antibiotics

During this investigation, N,N'-bis-azidomethylamines, N,N'-bis-cyanomethylamine, new alkoxymethylamine and chiral derivatives, which are considered to be a new generation of multifunctional compounds, were synthesized, functional properties were investigated, and anticholinergic and antidiabetic properties of those compounds were studied through the laboratory tests, and it was approved that they contain physiologically active compounds rather than analogues. Novel N-bis-cyanomethylamine and alkoxymethylamine derivatives were effective inhibitors of the α-glycosidase, cytosolic carbonic anhydrase I and II isoforms, butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with K values in the range of 0.15-13.31 nM for α-glycosidase, 2.77-15.30 nM for human carbonic anhydrase isoenzymes I (hCA I), 3.12-21.90 nM for human carbonic anhydrase isoenzymes II (hCA II), 23.33-73.23 nM for AChE, and 3.84-48.41 nM for BChE, respectively. Indeed, the inhibition of these metabolic enzymes has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances.

Section: Methodsmentioning

confidence: 99%

Synthesis and discovery of potent carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase, and α‐glycosidase enzymes inhibitors: The novel N,N′‐bis‐cyanomethylamine and alkoxymethylamine derivatives

Taslimi

Çağlayan

Farzaliyev

et al. 2018

“…CDNB was used as a substrate for the analysis of the enzyme activities. The K i values and inhibition types were determined by Lineweaver–Burk curves according to our previous studies …”

Section: Methodsmentioning

confidence: 99%

Evaluation of chalcones as inhibitors of glutathione S‐transferase

Özaslan

Demir

Aslan

et al. 2018

Glutathione S-transferases (GSTs) are the superfamily of multifunctional detoxification isoenzymes and play an important role in cellular signaling. In the present study, potential inhibition effects of chalcones were tested against human GST. For this purpose, GST was purified from human erythrocytes with 5.381 EU⋅mg specific activity and 51.95% yield using a GSH-agarose affinity chromatographic method. The effects of chalcones on in vitro GST activity were tested at various concentrations. K constants of chalcones were found in the range of 7.76-41.93 μM. According to the results, 4-fluorochalcone showed a better inhibitory effect compared with the other compounds. The inhibition mechanisms of 2'-hydroxy-4-methoxychalcone and 4-methoxychalcone were noncompetitive, whereas the inhibition mechanisms of 4'- hydroxychalcone, 4- fluorochalcone, and 4,4'- diflurochalcone were competitive.

“…[24] The column was balanced using was applied to the column and was eluted from the column with the same buffer.…”

Section: Molecular Weight Determination By Gel Filtrationmentioning

confidence: 99%

Inhibition effects of pesticides on glutathione‐S‐transferase enzyme activity of Van Lake fish liver

Özaslan

Demir

Aksoy

et al. 2018

Glutathione-S-transferases (GSTs) have a function in xenobiotic metabolism. They are a significant multifunctional family with a wide variety of catalytic activities. In the current study, we determined in vitro inhibition effects of 2,4-dichlorophenoxyacetic acid dimethylamine salt (2,4-D DMA), haloxyfop-P-methyl, glyphosate isopropylamine, dichlorvos, and λ-cyhalothrin on purified GST. For this purpose, GST were purified from Van Lake fish (Chalcalburnus tarichii Pallas) liver with 29.25 EU mg specific activity and 10.76% yield using GSH-agarose affinity chromatographic method. The pesticides were tested at various concentrations on in vitro GST activity. K constants were calculated as 0.17 ± 0.01, 0.25 ± 0.05, 3.72 ± 0.32, 0.42 ± 0.06, and 0.025 ± 0.004 mM, for 2,4-D DMA, haloxyfop-P-methyl, glyphosate isopropylamine, dichlorvos, and λ-cyhalothrin, respectively. λ-Cyhalothrin showed a better inhibitory effect compared to the other pesticides. The inhibition mechanisms of λ-cyhalothrin were competitive, while the other pesticides were noncompetitive.