Laboratory of Drug Metabolism and Drug Toxicity, Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav st., 1000 Sofia, Bulgaria.
Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav st., 1000 Sofia, Bulgaria.
Int J Mol Sci. 2023 Jun 25;24(13):10631. doi: 10.3390/ijms241310631.
An in vitro/in vivo hepatotoxicity and hepatoprotection evaluation of a defatted extract and a phenolic fraction from , administered alone and in a carbon tetrachloride (CCl)-induced metabolic bioactivation model, was performed. The extract and the phenolic fraction were analysed by high performance liquid chromatography (HPLC) to determine the total flavonoid content, to identify flavonoids and to quantify verbascoside. In addition, total polyphenolics in the samples were expressed as gallic acid equivalents. Applied alone, the extract and the fraction (5, 10 and 50 µg/mL) did not show a statistically significant hepatotoxic effect on isolated rat hepatocytes in vitro. In a CCl-induced hepatotoxicity model, the samples exhibited a concentration-dependent, statistically significant hepatoprotective effect, which was most pronounced at 50 µg/mL for both. The phenolic fraction exhibited a more pronounced hepatoprotective effect compared to the extract. Data from the in vitro study on the effects of the extract were also confirmed in the in vivo experiment conducted in a CCl-induced hepatotoxicity model in rats. A histopathological study showed that the animals treated with CCl and the extract had an unaltered histoarchitecture of the liver. The effects of the extract were the same as those of silymarin.
采用体外/体内方法,对 进行了去脂提取物和酚类部位的肝毒性和肝保护作用评价,分别单独给药和在四氯化碳(CCl)诱导的代谢生物活化模型中给药。采用高效液相色谱法(HPLC)对提取物和酚类部位进行分析,以测定总黄酮含量、鉴定类黄酮并定量测定毛蕊花糖苷。此外,样品中的总多酚以没食子酸当量表示。单独应用时,提取物和酚类部位(5、10 和 50μg/mL)在体外对分离的大鼠肝细胞没有表现出统计学显著的肝毒性作用。在 CCl 诱导的肝毒性模型中,样品表现出浓度依赖性的、统计学显著的肝保护作用,在 50μg/mL 时最为明显,对两者均如此。与提取物相比,酚类部位表现出更明显的肝保护作用。在 CCl 诱导的肝毒性模型中进行的体内实验也证实了体外研究中关于提取物作用的数据。组织病理学研究表明,用 CCl 和提取物处理的动物的肝脏组织形态结构没有改变。提取物的作用与水飞蓟素相同。