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Conjugate of pyrimidine derivative, the drug xymedon with succinic acid protects liver cells
Journal of Biochemical and Molecular Toxicology ( IF 3.2 ) Pub Date : 2020-11-06 , DOI: 10.1002/jbt.22660
Alexandra B Vyshtakalyuk 1 , Andrey A Parfenov 1 , Lilya F Gumarova 1 , Leyla R Khasanshina 1 , Grigory P Belyaev 1 , Nail G Nazarov 1 , Darya A Kondrashina 1 , Irina V Galyametdinova 1 , Vyacheslav E Semenov 1 , Vladimir V Zobov 1
Affiliation  

The aim of the study was to investigate the hepatoprotective properties of the conjugate of the xymedon drug substance with succinic acid (1a). The study presents an in vitro comparative evaluation of the cytotoxicity and cytoprotective properties of 1a and succinic acid on a cell line of normal human hepatocytes Chang Liver, and in vivo investigation of the ability of 1a to restore liver from the toxic damage caused by CCl4 in Wistar rats. It was shown that the cytotoxicity of 1a was 19.9 ± 0.8 mmol/L, and that of succinic acid was 14.1 ± 0.2 mmol/L. Against the background of d‐galactosamine exposure, the cytoprotective effect of 1a was found to be superior to that of succinic acid. It was shown that 1a caused a significant reduction in necrotic and steatosis changes in the liver and restoration of biochemical markers of cytolysis, as well as bilirubin metabolism and synthetic liver function.

中文翻译:

与嘧啶衍生物共轭,药物木丁酮与琥珀酸共同保护肝细胞

该研究的目的是研究木酮类药物与琥珀酸(1a)的结合物的肝保护特性。这项研究提出了对1a和琥珀酸对正常人肝细胞Chang Liver的细胞系的细胞毒性和细胞保护特性的体外比较评估,以及对1a从CCl 4引起的毒性损伤中恢复肝脏能力的体内研究。在Wistar大鼠中。结果表明,1a的细胞毒性为19.9±0.8 mmol / L,琥珀酸的细胞毒性为14.1±0.2 mmol / L。在d-半乳糖胺暴露的背景下,1a的细胞保护作用被发现优于琥珀酸。结果表明1a引起肝脏坏死和脂肪变性的明显减少,细胞溶解,胆红素代谢和合成肝功能的生化标志物的恢复。
更新日期:2020-11-06
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