Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies

This study investigates the effect of pyrimidine derivatives (Xymedon and its conjugate with L-ascorbic acid, both exhibiting hepatoprotective activity) on the apoptosis of rat liver cells against the background of exposure to carbon tetrachloride as a hepatotoxic agent. The characteristic markers o...

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Main Authors: A.A. Parfenov, A.B. Vyshtakalyuk, I.V. Galyametdinova, V.E. Semenov, V.V. Zobov
Format: Article
Language:English
Published: Kazan Federal University 2022-06-01
Series:Учёные записки Казанского университета: Серия Естественные науки
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Online Access:https://kpfu.ru/uz-eng-ns-2022-2-4.html
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author A.A. Parfenov
A.B. Vyshtakalyuk
I.V. Galyametdinova
V.E. Semenov
V.V. Zobov
author_facet A.A. Parfenov
A.B. Vyshtakalyuk
I.V. Galyametdinova
V.E. Semenov
V.V. Zobov
author_sort A.A. Parfenov
collection DOAJ
description This study investigates the effect of pyrimidine derivatives (Xymedon and its conjugate with L-ascorbic acid, both exhibiting hepatoprotective activity) on the apoptosis of rat liver cells against the background of exposure to carbon tetrachloride as a hepatotoxic agent. The characteristic markers of apoptosis affected by the considered compounds were identified. Modern multiplex analysis of the early apoptosis markers Akt, BAD, BCL-2, p53, Active Caspase-8, and Active Caspase-9 in rat liver homogenates using the MagPix system (MerkMillipore, USA) was selected as the main research method. The results obtained show that Xymedon and its derivative with L-ascorbic acid exert an anti-apoptotic effect by causing a significant decrease in the number of the early apoptosis markers BAD and Active Caspase-9. The derivative with L-ascorbic acid was also found to reduce p53 expression. Moreover, it was revealed that the studied pyrimidine derivatives normalize the biochemical markers of liver damage (transaminases, alkaline phosphatase, bilirubin, total protein, and albumin) and increase the level of glucose in the blood serum of rats against the background of acute toxic damage to the liver by carbon tetrachloride. Our findings are of the utmost theoretical and practical relevance for better understanding the mechanisms of the action of pyrimidine derivatives and for developing a highly effective hepatoprotective drug.
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institution Kabale University
issn 2542-064X
2500-218X
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publishDate 2022-06-01
publisher Kazan Federal University
record_format Article
series Учёные записки Казанского университета: Серия Естественные науки
spelling doaj-art-395171a9f416480ba5097934400d232e2025-01-02T05:48:09ZengKazan Federal UniversityУчёные записки Казанского университета: Серия Естественные науки2542-064X2500-218X2022-06-01164223124810.26907/2542-064X.2022.2.231-248Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studiesA.A. Parfenov0A.B. Vyshtakalyuk1I.V. Galyametdinova2V.E. Semenov3V.V. Zobov4Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, 420088 RussiaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, 420088 Russia; Kazan Federal University, Kazan, 420008 RussiaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, 420088 RussiaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, 420088 Russia; Kazan National Research Technological University, Kazan, 420015 RussiaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, 420088 Russia; Kazan Federal University, Kazan, 420008 RussiaThis study investigates the effect of pyrimidine derivatives (Xymedon and its conjugate with L-ascorbic acid, both exhibiting hepatoprotective activity) on the apoptosis of rat liver cells against the background of exposure to carbon tetrachloride as a hepatotoxic agent. The characteristic markers of apoptosis affected by the considered compounds were identified. Modern multiplex analysis of the early apoptosis markers Akt, BAD, BCL-2, p53, Active Caspase-8, and Active Caspase-9 in rat liver homogenates using the MagPix system (MerkMillipore, USA) was selected as the main research method. The results obtained show that Xymedon and its derivative with L-ascorbic acid exert an anti-apoptotic effect by causing a significant decrease in the number of the early apoptosis markers BAD and Active Caspase-9. The derivative with L-ascorbic acid was also found to reduce p53 expression. Moreover, it was revealed that the studied pyrimidine derivatives normalize the biochemical markers of liver damage (transaminases, alkaline phosphatase, bilirubin, total protein, and albumin) and increase the level of glucose in the blood serum of rats against the background of acute toxic damage to the liver by carbon tetrachloride. Our findings are of the utmost theoretical and practical relevance for better understanding the mechanisms of the action of pyrimidine derivatives and for developing a highly effective hepatoprotective drug.https://kpfu.ru/uz-eng-ns-2022-2-4.htmlpyrimidine derivativesxymedonapoptosiscarbon tetrachloridetoxic liver damage
spellingShingle A.A. Parfenov
A.B. Vyshtakalyuk
I.V. Galyametdinova
V.E. Semenov
V.V. Zobov
Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies
Учёные записки Казанского университета: Серия Естественные науки
pyrimidine derivatives
xymedon
apoptosis
carbon tetrachloride
toxic liver damage
title Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies
title_full Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies
title_fullStr Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies
title_full_unstemmed Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies
title_short Anti-apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies
title_sort anti apoptosis mechanism of the hepatoprotective effect of pyrimidine derivatives in in vivo studies
topic pyrimidine derivatives
xymedon
apoptosis
carbon tetrachloride
toxic liver damage
url https://kpfu.ru/uz-eng-ns-2022-2-4.html
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AT ivgalyametdinova antiapoptosismechanismofthehepatoprotectiveeffectofpyrimidinederivativesininvivostudies
AT vesemenov antiapoptosismechanismofthehepatoprotectiveeffectofpyrimidinederivativesininvivostudies
AT vvzobov antiapoptosismechanismofthehepatoprotectiveeffectofpyrimidinederivativesininvivostudies