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首页> 外文期刊>Brazilian Journal of Pharmaceutical Sciences >In vitro investigations of Cynara scolymus L. extract on cell physiology of HepG2 liver cells
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In vitro investigations of Cynara scolymus L. extract on cell physiology of HepG2 liver cells

机译：Cynara scolymus L.提取物对HepG2肝细胞细胞生理学的体外研究。

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The objective of this study was the investigation of a potential influence of artichoke leaf extract (ALE) on the cell physiology and gene expression of phase I/II enzymes of human liver cells HepG2 and investigation on potential cell protective effects against ethanol-induced cell toxicity against HepG2 cells. Cell biological assays under in vitro conditions using HepG2 liver cells and investigation of mitochondrial activity (MTT test), proliferation assay (BrdU incorporation ELISA), LDH as toxicity marker, gene expression analysis by RT-PCR and enzyme activity of glutationtransferase. Artichocke extract, containing 27% caffeoylquinic acids and 7% flavonoids induced mitochondrial activity, proliferation and total protein content under in vitro conditions in human liver cells HepG2. These effects could not be correlated to the well-known artichoke secondary compounds cynarin, caffeic acid, chlorogenic acid, luteolin and luteolin-7-O-glucoside. The flavones luteolin and luteolin-7-O-glucoside had inhibitory effects at 100 μg/mL level on HepG2 cells, with luteolin being a significant stronger inhibitor compared to the respective glucoside. Artichoke leaf extract had minor stimulating effect on gene expression of CYP1A2, while CYP3A4, GGT, GPX2, GSR and GST were slightly inhibited. GST inhibition under in vitro conditions was also shown by quantification of GST enzyme activity. Induction of gene expression of CYP1A2 was shown to be supraadditive after simultaneous application of ethanol plus artichoke extract. Artichoke leaf extract exhibited cell protective effects against ethanol-induced toxicity within cotreatment under in vitro conditions. Also H2O2 damage was significantly inhibited by simultaneous artichoke incubation. Pre- and posttreatments did not exert protective effects. DMSO-induced toxicity was significantly reduced by pre-, post- and cotreatment with artichoke extract and especially with luteolin-7-O-glucoside, indicating a direct interaction with the toxifying agent and an induction of repair mechanisms.
机译：这项研究的目的是研究朝鲜蓟叶提取物（ALE）对人肝细胞HepG2的细胞生理学和I / II期酶基因表达的潜在影响，并研究对乙醇诱导的细胞毒性的潜在细胞保护作用对抗HepG2细胞。在体外条件下使用HepG2肝细胞进行细胞生物学测定，并研究线粒体活性（MTT试验），增殖测定（BrdU掺入ELISA），LDH作为毒性标志物，通过RT-PCR进行基因表达分析和谷氨酸转移酶的酶活性。在体外条件下，人肝细胞HepG2中含有27％的咖啡酰奎尼酸和7％的类黄酮的洋蓟提取物可诱导线粒体活性，增殖和总蛋白含量。这些作用与众所周知的洋蓟仲化合物cynarin，咖啡酸，绿原酸，木犀草素和木犀草素-7-O-葡萄糖苷无关。黄酮木犀草素和木犀草素-7-O-葡糖苷以100μg/ mL的水平对HepG2细胞具有抑制作用，与​​各自的葡糖苷相比，木犀草素是明显更强的抑制剂。朝鲜蓟叶提取物对CYP1A2的基因表达有较小的刺激作用，而对CYP3A4，GGT，GPX2，GSR和GST的抑制作用稍有抑制。还通过定量GST酶活性显示了在体外条件下的GST抑制。同时应用乙醇和朝鲜蓟提取物后，CYP1A2基因表达的诱导显示是超加性的。朝鲜蓟叶提取物在体外条件下的共处理内对乙醇诱导的毒性表现出细胞保护作用。同时朝鲜蓟孵育还显着抑制了H2O2损害。预处理和后处理均未发挥保护作用。 DMSO诱导的毒性通过用朝鲜蓟提取物，尤其是木犀草素7-O-葡萄糖苷的预处理，后处理和共处理而显着降低，表明与毒素的直接相互作用和诱导的修复机制。

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