首页> 外文期刊>Life sciences >Short term treatment with St. John's wort, hypericin or hyperforin fails to induce CYP450 isoforms in the Swiss Webster mouse.
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Short term treatment with St. John's wort, hypericin or hyperforin fails to induce CYP450 isoforms in the Swiss Webster mouse.

机译:用圣约翰草,金丝桃素或金丝桃素的短期治疗未能在Swiss Webster小鼠中诱导CYP450亚型。

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This investigation was designed to determine whether St. John's wort (SJW)(435 mg/kg/d), a readily available antidepressant, or its purported active constituents hypericin (1 mg/kg/d) and hyperforin (10 mg/kg/d) were able to induce various hepatic cytochrome P450 (CYP450) isoforms. SJW, hypericin and hyperforin were administered to male Swiss Webster mice for four consecutive days and hepatic microsomes were prepared on day 5. None of the three treatments resulted in a statistical change in total hepatic CYP450 (SJW treated 0.95 +/- 0.09 nmol/mg vs control 1.09 +/- 0.14 nmol/mg). Furthermore, the catalytic activities of CYP1A2. CYP2E1 and CYP3A were unchanged from control following all three treatments as determined by ethoxyresorufin O-deethylation, p-nitrophenol hydroxylation and erythromycin N-demethylation respectively. Additionally, western immunoblotting demonstrated that there was no significant change in the polypeptide levels of any of the three isoforms. These results indicate that four days of treatment with moderate to high doses of SJW, hyperforin or hypericin fails to induce these CYP450 isoforms in the male Swiss Webster mouse.
机译:这项研究旨在确定是否容易获得抗抑郁药圣约翰草(SJW)(435 mg / kg / d)或其声称的活性成分金丝桃素(1 mg / kg / d)和金丝桃素(10 mg / kg / d) d)能够诱导各种肝细胞色素P450(CYP450)亚型。将SJW,金丝桃素和金丝桃素连续四天施用于雄性Swiss Webster小鼠,并在第5天制备肝微粒体。这三种治疗均未导致总肝CYP450的统计变化(SJW治疗为0.95 +/- 0.09 nmol / mg与对照相比1.09 +/- 0.14 nmol / mg)。此外,CYP1A2的催化活性。分别通过乙氧基间苯二酚的O-脱乙基,对硝基苯酚羟基化和红霉素N-脱甲基测定,在所有三种处理之后,CYP2E1和CYP3A均与对照相比没有变化。另外,蛋白质免疫印迹证明三种同工型中任何一种的多肽水平都没有显着变化。这些结果表明用中至高剂量的SJW,hyperforin或hypericin治疗四天未能在雄性Swiss Webster小鼠中诱导这些CYP450亚型。

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