一种基于白桦脂酸的化合物的促肝活性。

Q3 Biochemistry, Genetics and Molecular Biology
K I Mosalev, I D Ivanov, M V Tenditnik, E E Shults, V A Vavilin
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引用次数: 0

摘要

利用环磷酰胺(CP)诱导的 C57BL/6 小鼠免疫抑制模型,研究了白桦脂酸与 9-(4-甲基哌嗪-1-基甲基)-2-(1,2,3-三唑基)奥曲泽兰酮(BABC)共轭物的促肝作用。研究人员测定了受试动物肝脏中细胞色素(CYP 1A1、CYP 1A2、CYP 3A44、CYP 2B10、CYP 2C29、CYP 17A1)、PPARA、细胞因子(TNF-α、IL-1β、IL-12α、IL-10)基因的表达情况,以及 NF-κB p65、GST-π 和 NAT-1 蛋白质的相对水平。在对动物施用化合物和氯化石蜡后的第六天,与对照组相比,观察到 CYP 2B10 的表达显著增加(3.2 倍)。与接受氯化石蜡的动物组相比,用该化合物和氯化石蜡处理小鼠还导致促炎 TNF-α 基因的 mRNA 水平增加了 2.4 倍。与对照组相比,给完整的动物施用所研究的化合物会导致 IL-1β 表达量增加 2.5 倍,IL-10 表达量减少 1.8 倍。与对照组相比,用该化合物治疗的动物肝脏中促炎细胞因子基因的表达增加,同时 NF-κB p65 的含量增加(1.6 倍),NAT-1 蛋白质的相对含量增加(2.7 倍)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Hepatotropic activity of a betulonic acid based compound.

Using the model of cyclophosphamide (CP)-induced immunosuppression in C57BL/6 mice, the hepatotropic effects of a conjugate of betulonic acid with 9-(4-methylpiperazin-1-ylmethyl)-2-(1,2,3-triazolyl) oreozelone (BABC) have been studied. In the liver of treated animals the expression of genes for cytochromes (CYP 1A1, CYP 1A2, CYP 3A44, CYP 2B10, CYP 2C29, CYP 17A1), PPARA, and cytokines (TNF-α, IL-1β, IL-12α, IL-10) and the relative levels of NF-κB p65, GST-π, and NAT-1 proteins were determined. On day six after administration of the compound and CP to animals a significant (3.2-fold) increase in the expression of the CYP 2B10 as compared to the control group was observed. Treatment of mice with the compound and CP also caused a 2.4-fold increase in the mRNA level of the pro-inflammatory TNF-α gene as compared to the group of animals receiving CP. Administration of the studied compound to intact animals was accompanied by a 2.5-fold increase in the IL-1β expression and a 1.8-fold decrease in the IL-10 expression as compared to the control group. An increase in the expression of pro-inflammatory cytokine genes in the liver of animals treated with the compound was accompanied by an increase in the content of NF-κB p65 (by 1.6 times), as well as an increase in the relative amount of NAT-1 protein (by 2.7 times) as compared to control animals.

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来源期刊
Biomeditsinskaya khimiya
Biomeditsinskaya khimiya Biochemistry, Genetics and Molecular Biology-Biochemistry, Genetics and Molecular Biology (all)
CiteScore
1.30
自引率
0.00%
发文量
49
期刊介绍: The aim of the Russian-language journal "Biomeditsinskaya Khimiya" (Biomedical Chemistry) is to introduce the latest results obtained by scientists from Russia and other Republics of the Former Soviet Union. The Journal will cover all major areas of Biomedical chemistry, including neurochemistry, clinical chemistry, molecular biology of pathological processes, gene therapy, development of new drugs and their biochemical pharmacology, introduction and advertisement of new (biochemical) methods into experimental and clinical medicine etc. The Journal also publish review articles. All issues of journal usually contain invited reviews. Papers written in Russian contain abstract (in English).
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