The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental Study

Objective: to investigate the activity of sevoflurane, dalargin, and lithium chloride in protecting the rat brain from total ischemia/reperfusion and to define whether the GSK=3^ deposphorylation contributes to the mechanism of pharmacological preconditioning. Materials and methods. Experiments were...

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Main Authors: V. V. Likhvantsev, O. A. Grebenchikov, K. Yu. Borisov, V. L., Shaibakova, A. A. Shaposhnikov, R. A. Cherpakov, E. V. Shmeleva
Format: Article
Language:English
Published: Federal Research and Clinical Center of Intensive Care Medicine and Rehabilitology, Moscow, Russia 2012-12-01
Series:Общая реаниматология
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Online Access:https://www.reanimatology.com/rmt/article/view/175
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author V. V. Likhvantsev
O. A. Grebenchikov
K. Yu. Borisov
V. L., Shaibakova
A. A. Shaposhnikov
R. A. Cherpakov
E. V. Shmeleva
author_facet V. V. Likhvantsev
O. A. Grebenchikov
K. Yu. Borisov
V. L., Shaibakova
A. A. Shaposhnikov
R. A. Cherpakov
E. V. Shmeleva
author_sort V. V. Likhvantsev
collection DOAJ
description Objective: to investigate the activity of sevoflurane, dalargin, and lithium chloride in protecting the rat brain from total ischemia/reperfusion and to define whether the GSK=3^ deposphorylation contributes to the mechanism of pharmacological preconditioning. Materials and methods. Experiments were carried out on 80 male albino rats in which temporary circulatory arrest (CA) was simulated by ligating the cardiovascular fascicle for 10 and 20 minutes. The animals were revived by mechanical ventilation external cardiac massage, and the intratracheal injection of adrenaline (epinephrine, Moscow Endocrinology Plant) at a dose of 0.1 mg/kg. Animals were divided into 9 groups and sevorane (sevoflurane, Abbott Laboratories), dalargin (Microgen Research-and-Production Association), or lithium chloride (Sigma Chemical Co.) were separately given with and without CA. Brain tissue homogenate specimens were obtained from euthanized animals. The concentration of total glycogen synthase kinase-3^ (GSK-3^) was colorimetrically determined using a Hitachi-557 spectrophotometer (Hitachi Ltd., Japan). The content of phosphorylated GSK-3/3 (pGSK-3^) in brain homogenate was estimated by Western blotting. Results. The total level of GSK-3^ in each group was similar (80—90 relative units) and remained unchanged throughout each experiment. Twenty-minute ischemia maximally activated GSK-30 through dephosphorylation. Ten-minute ischemia elevated pGSK-3^ levels by more than 5 times as compared to the baseline value revealing the «training» effect. The quantity of pGSK-3^ was unchanged in the ischemia/perfusion group during sevoflurane insufflation and was decreased by 27% during dalargin administration. Conclusion. The experimental model of total ischemia provided evidence that the test drugs had a pharmacological preconditioning effect on brain neurons. According to their increasing effect, the drugs were arranged in the following order: dalargin < sevoflurane < lithium chloride. The data warranties further studies to reveal the clinical significance of dalargin, sevofluran and lithium for preconditioning to protect the brain. Key words: lithium, dalargin, sevofluran, preconditioning, brain.
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publisher Federal Research and Clinical Center of Intensive Care Medicine and Rehabilitology, Moscow, Russia
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spelling doaj-art-08f1966f26ce4e93bbded6639f2b1fed2025-08-20T03:59:40ZengFederal Research and Clinical Center of Intensive Care Medicine and Rehabilitology, Moscow, RussiaОбщая реаниматология1813-97792411-71102012-12-018610.15360/1813-9779-2012-6-37175The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental StudyV. V. LikhvantsevO. A. GrebenchikovK. Yu. BorisovV. L., ShaibakovaA. A. ShaposhnikovR. A. CherpakovE. V. ShmelevaObjective: to investigate the activity of sevoflurane, dalargin, and lithium chloride in protecting the rat brain from total ischemia/reperfusion and to define whether the GSK=3^ deposphorylation contributes to the mechanism of pharmacological preconditioning. Materials and methods. Experiments were carried out on 80 male albino rats in which temporary circulatory arrest (CA) was simulated by ligating the cardiovascular fascicle for 10 and 20 minutes. The animals were revived by mechanical ventilation external cardiac massage, and the intratracheal injection of adrenaline (epinephrine, Moscow Endocrinology Plant) at a dose of 0.1 mg/kg. Animals were divided into 9 groups and sevorane (sevoflurane, Abbott Laboratories), dalargin (Microgen Research-and-Production Association), or lithium chloride (Sigma Chemical Co.) were separately given with and without CA. Brain tissue homogenate specimens were obtained from euthanized animals. The concentration of total glycogen synthase kinase-3^ (GSK-3^) was colorimetrically determined using a Hitachi-557 spectrophotometer (Hitachi Ltd., Japan). The content of phosphorylated GSK-3/3 (pGSK-3^) in brain homogenate was estimated by Western blotting. Results. The total level of GSK-3^ in each group was similar (80—90 relative units) and remained unchanged throughout each experiment. Twenty-minute ischemia maximally activated GSK-30 through dephosphorylation. Ten-minute ischemia elevated pGSK-3^ levels by more than 5 times as compared to the baseline value revealing the «training» effect. The quantity of pGSK-3^ was unchanged in the ischemia/perfusion group during sevoflurane insufflation and was decreased by 27% during dalargin administration. Conclusion. The experimental model of total ischemia provided evidence that the test drugs had a pharmacological preconditioning effect on brain neurons. According to their increasing effect, the drugs were arranged in the following order: dalargin < sevoflurane < lithium chloride. The data warranties further studies to reveal the clinical significance of dalargin, sevofluran and lithium for preconditioning to protect the brain. Key words: lithium, dalargin, sevofluran, preconditioning, brain.https://www.reanimatology.com/rmt/article/view/175литийдаларгинсевофлуранпрекондиционированиеголовной мозг.
spellingShingle V. V. Likhvantsev
O. A. Grebenchikov
K. Yu. Borisov
V. L., Shaibakova
A. A. Shaposhnikov
R. A. Cherpakov
E. V. Shmeleva
The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental Study
Общая реаниматология
литий
даларгин
севофлуран
прекондиционирование
головной мозг.
title The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental Study
title_full The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental Study
title_fullStr The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental Study
title_full_unstemmed The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental Study
title_short The Mechanisms of Pharmacological Preconditioning of the Brain and the Comparative Efficacy of the Drugs — Direct- and Indirect-Acting Glycogen Synthase Kinase-3β Inhibitors: Experimental Study
title_sort mechanisms of pharmacological preconditioning of the brain and the comparative efficacy of the drugs direct and indirect acting glycogen synthase kinase 3β inhibitors experimental study
topic литий
даларгин
севофлуран
прекондиционирование
головной мозг.
url https://www.reanimatology.com/rmt/article/view/175
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