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Your search keyword '"Schepetkin, Igor A."' showing total 20 results
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20 results on '"Schepetkin, Igor A."'

2. Evaluation of Nitric Oxide-Donating Properties of 11 H -indeno[1,2- b ]quinoxalin-11-one Oxime (IQ-1) by Electron Paramagnetic Resonance Spectroscopy.

Author

Andrianov, Viacheslav V., Schepetkin, Igor A., Bazan, Leah V., Gainutdinov, Khalil L., Kovrizhina, Anastasia R., Atochin, Dmitriy N., and Khlebnikov, Andrei I.

Subjects
*ELECTRON paramagnetic resonance spectroscopy, *ELECTRON paramagnetic resonance, *LIVER microsomes, *DENSITY functional theory, *RADICAL anions
Abstract

IQ-1 (11H-indeno[1,2-b]quinoxalin-11-one oxime) is a specific c-Jun N-terminal kinase (JNK) inhibitor with anticancer and neuro- and cardioprotective properties. Because aryloxime derivatives undergo cytochrome P450-catalyzed oxidation to nitric oxide (NO) and ketones in liver microsomes, NO formation may be an additional mechanism of IQ-1 pharmacological action. In the present study, electron paramagnetic resonance (EPR) of the Fe2+ complex with diethyldithiocarbamate (DETC) as a spin trap and hemoglobin (Hb) was used to detect NO formation from IQ-1 in the liver and blood of rats, respectively, after IQ-1 intraperitoneal administration (50 mg/kg). Introducing the spin trap and IQ-1 led to signal characteristics of the complex (DETC)2-Fe2+-NO in rat liver. Similarly, the introduction of the spin trap components and IQ-1 resulted in an increase in the Hb-NO signal for both the R- and the T-conformers in blood samples. The density functional theory (DFT) calculations were in accordance with the experimental data and indicated that the NO formation of IQ-1 through the action of superoxide anion radical is thermodynamically favorable. We conclude that the administration of IQ-1 releases NO during its oxidoreductive bioconversion in vivo. [ABSTRACT FROM AUTHOR]

Published
2024
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3. Volatile Composition, Antimicrobial Activity, and In Vitro Innate Immunomodulatory Activity of Echinacea purpurea (L.) Moench Essential Oils

Author

Dosoky, Noura S., primary, Kirpotina, Liliya N., additional, Schepetkin, Igor A., additional, Khlebnikov, Andrei I., additional, Lisonbee, Brent L., additional, Black, Jeffrey L., additional, Woolf, Hillary, additional, Thurgood, Trever L., additional, Graf, Brittany L., additional, Satyal, Prabodh, additional, and Quinn, Mark T., additional

Published
2023
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4. Immunomodulatory Activity of Polysaccharides Isolated from Saussurea salicifolia L. and Saussurea frolovii Ledeb

Author

Schepetkin, Igor A., primary, Danilets, Marina G., additional, Ligacheva, Anastasia A., additional, Trofimova, Evgenia S., additional, Selivanova, Natalia S., additional, Sherstoboev, Evgenii Yu., additional, Krivoshchekov, Sergei V., additional, Gulina, Ekaterina I., additional, Brazovskii, Konstantin S., additional, Kirpotina, Liliya N., additional, Quinn, Mark T., additional, and Belousov, Mikhail V., additional

Published
2023
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6. Inhibition of Acetylcholinesterase by Novel Lupinine Derivatives

Author

Schepetkin, Igor A., primary, Nurmaganbetov, Zhangeldy S., additional, Fazylov, Serik D., additional, Nurkenov, Oralgazy A., additional, Khlebnikov, Andrei I., additional, Seilkhanov, Tulegen M., additional, Kishkentaeva, Anarkul S., additional, Shults, Elvira E., additional, and Quinn, Mark T., additional

Published
2023
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10. Pyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis

Author

Crocetti, Letizia, primary, Vergelli, Claudia, additional, Guerrini, Gabriella, additional, Giovannoni, Maria Paola, additional, Kirpotina, Liliya N., additional, Khlebnikov, Andrei I., additional, Ghelardini, Carla, additional, Di Cesare Mannelli, Lorenzo, additional, Lucarini, Elena, additional, Schepetkin, Igor A., additional, and Quinn, Mark T., additional

Published
2021
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16. Protective Effects of a New C-Jun N-terminal Kinase Inhibitor in the Model of Global Cerebral Ischemia in Rats

Author

Plotnikov, Mark B., primary, Chernysheva, Galina A., additional, Aliev, Oleg I., additional, Smol’iakova, Vera I., additional, Fomina, Tatiana I., additional, Osipenko, Anton N., additional, Rydchenko, Victoria S., additional, Anfinogenova, Yana J., additional, Khlebnikov, Andrei I., additional, Schepetkin, Igor A., additional, and Atochin, Dmitriy N., additional

Published
2019
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20. Novel c-Jun N-Terminal Kinase (JNK) Inhibitors with an 11 H -Indeno[1,2- b ]quinoxalin-11-one Scaffold.

Author

Liakhov, Serhii A., Schepetkin, Igor A., Karpenko, Olexander S., Duma, Hanna I., Haidarzhy, Nadiia M., Kirpotina, Liliya N., Kovrizhina, Anastasia R., Khlebnikov, Andrei I., Bagryanskaya, Irina Y., and Quinn, Mark T.

Subjects
*CELLULAR signal transduction, *NUCLEAR proteins, *REPERFUSION injury, *LIPOPOLYSACCHARIDES, *RHEUMATOID arthritis, *CHOLINESTERASE reactivators
Abstract

c-Jun N-terminal kinase (JNK) plays a central role in stress signaling pathways implicated in important pathological processes, including rheumatoid arthritis and ischemia-reperfusion injury. Therefore, inhibition of JNK is of interest for molecular targeted therapy to treat various diseases. We synthesized 13 derivatives of our reported JNK inhibitor 11H-indeno[1,2-b]quinoxalin-11-one oxime and evaluated their binding to the three JNK isoforms and their biological effects. Eight compounds exhibited submicromolar binding affinity for at least one JNK isoform. Most of these compounds also inhibited lipopolysaccharide (LPS)-induced nuclear factor-κB/activating protein 1 (NF-κB/AP-1) activation and interleukin-6 (IL-6) production in human monocytic THP1-Blue cells and human MonoMac-6 cells, respectively. Selected compounds (4f and 4m) also inhibited LPS-induced c-Jun phosphorylation in MonoMac-6 cells, directly confirming JNK inhibition. We conclude that indenoquinoxaline-based oximes can serve as specific small-molecule modulators for mechanistic studies of JNKs, as well as potential leads for the development of anti-inflammatory drugs. [ABSTRACT FROM AUTHOR]

Published
2021
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