Open Access
Open access
Molecules, volume 27, issue 17, pages 5488

The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke

Borozdenko D A 1
, 
Shmigol Tatiana A 1
, 
Ezdoglian Aiarpi A 1
, 
Gonchar Darya I 1
, 
Karpechenko Natalia Yu 1
, 
Lyakhmun Dmitri N 1
, 
Shagina Anastasia D 1
, 
Cherkashova Elvira A 2
, 
Namestnikova Daria D 2, 3
, 
Gubskiy Ilya L 2
, 
Chernysheva A A 4
, 
Kiseleva Nina K. 1
, 
Negrebetsky Vadim V 1
, 
Baukov Yuri I 1
1
 
2
 
3
 
4
 
Publication type: Journal Article
Publication date: 2022-08-26
Journal: Molecules
Quartile SCImago
Q1
Quartile WOS
Q2
Impact factor: 4.6
ISSN: 14203049
Organic Chemistry
Drug Discovery
Physical and Theoretical Chemistry
Pharmaceutical Science
Molecular Medicine
Analytical Chemistry
Chemistry (miscellaneous)
Abstract

Ischemic stroke triggers a whole cascade of pathological changes in the brain, one of which is postischemic inflammation. Since in such cases thrombolytic therapy is often not possible, methods that modulate inflammation and affect microglia become particularly interesting. We synthesized 3-(2-oxo-4-phenylpyrrolidin-1-yl)propane-1-sulfonate calcium(II) (Compound 4) and studied its anti-inflammatory activity in in vitro and in vivo models of inflammation and ischemia. Macrophage cell line RAW 264.7 was treated with lipopolysaccharides (LPS) and Compound 4 at various dosages to study the cytokine profile using real-time PCR and cytometric bead array (CBA). Stroke in rats was simulated by the middle cerebral artery occlusion method (MCAO). Several tests were performed to characterize the neurological deficit and locomotor activity of the rats, and afterwards, postmortem, the number of astrocytes was counted using immunohistochemistry. Compound 4 in in vitro tests dose-dependently reduced the expression of interleukin-1β (IL1β), and inducible nitric oxide synthase (iNOS) genes in cell culture and increased the concentration of cytokines: interleukin-2, 4, 6 (IL-2, IL-4, and IL-6). In vivo Compound 4 increased the orienting-exploratory behavior, and reduced neurological and motor deficit. The number of astrocytes that promote and support inflammation was lower in the group treated with Compound 4. The stroke volume measured by magnetic resonance imaging (MRI) showed no difference. We have shown that Compound 4 demonstrates anti-inflammatory activity by increasing the synthesis of anti-inflammatory and reducing pro-inflammatory cytokines, and positively affects the neurological deficit in rats. Thus, Compound 4 has a high therapeutic potential in the management of patients after a stroke and requires further study of its neuroprotective properties.

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Molecules
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1 publication, 33.33%
Journal of Inflammation Research
Journal of Inflammation Research, 1, 33.33%
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1 publication, 33.33%
Mendeleev Communications
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Citations by publishers

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Multidisciplinary Digital Publishing Institute (MDPI)
Multidisciplinary Digital Publishing Institute (MDPI), 1, 33.33%
Multidisciplinary Digital Publishing Institute (MDPI)
1 publication, 33.33%
Dove Medical Press
Dove Medical Press, 1, 33.33%
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1 publication, 33.33%
Elsevier
Elsevier, 1, 33.33%
Elsevier
1 publication, 33.33%
1
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GOST Copy
Borozdenko D. A. et al. The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke // Molecules. 2022. Vol. 27. No. 17. p. 5488.
GOST all authors (up to 50) Copy
Borozdenko D. A., Shmigol T. A., Ezdoglian A. A., Gonchar D. I., Karpechenko N. Yu., Lyakhmun D. N., Shagina A. D., Cherkashova E. A., Namestnikova D. D., Gubskiy I. L., Chernysheva A. A., Kiseleva N. K., Negrebetsky V. V., Baukov Y. I. The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke // Molecules. 2022. Vol. 27. No. 17. p. 5488.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.3390/molecules27175488
UR - https://doi.org/10.3390%2Fmolecules27175488
TI - The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke
T2 - Molecules
AU - Shagina, Anastasia D
AU - Baukov, Yuri I
AU - Borozdenko, D A
AU - Shmigol, Tatiana A
AU - Ezdoglian, Aiarpi A
AU - Gonchar, Darya I
AU - Karpechenko, Natalia Yu
AU - Lyakhmun, Dmitri N
AU - Cherkashova, Elvira A
AU - Namestnikova, Daria D
AU - Gubskiy, Ilya L
AU - Chernysheva, A A
AU - Kiseleva, Nina K.
AU - Negrebetsky, Vadim V
PY - 2022
DA - 2022/08/26 00:00:00
PB - Multidisciplinary Digital Publishing Institute (MDPI)
SP - 5488
IS - 17
VL - 27
PMID - 36080256
SN - 1420-3049
ER -
BibTex |
Cite this
BibTex Copy
@article{2022_Borozdenko,
author = {Anastasia D Shagina and Yuri I Baukov and D A Borozdenko and Tatiana A Shmigol and Aiarpi A Ezdoglian and Darya I Gonchar and Natalia Yu Karpechenko and Dmitri N Lyakhmun and Elvira A Cherkashova and Daria D Namestnikova and Ilya L Gubskiy and A A Chernysheva and Nina K. Kiseleva and Vadim V Negrebetsky},
title = {The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke},
journal = {Molecules},
year = {2022},
volume = {27},
publisher = {Multidisciplinary Digital Publishing Institute (MDPI)},
month = {aug},
url = {https://doi.org/10.3390%2Fmolecules27175488},
number = {17},
pages = {5488},
doi = {10.3390/molecules27175488}
}
MLA
Cite this
MLA Copy
Borozdenko, D. A., et al. “The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke.” Molecules, vol. 27, no. 17, Aug. 2022, p. 5488. https://doi.org/10.3390%2Fmolecules27175488.
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