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Effects of Mollugin on Hepatic Cytochrome P450 in Male ICR Mice as Determined by Liquid Chromatography/Tandem Mass Spectrometry

机译:液相色谱/串联质谱法测定莫洛金对雄性ICR小鼠肝细胞色素P450的影响

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摘要

Mollugin isolated from Rubia cordifolia is known to have anti-inflammatory, anti-cancer, and anti-viral activities. In the present study, a cocktail probe assay and LC-MS/MS were used to investigate the modulating effect of mollugin on cytochrome P450 (CYP) enzymes in male ICR mice. After mollugin was orally administrated to mice at the 20, 40, or 80 mg/kg for 3 days, the activities of CYP in hepatic S-9 fractions were investigated. Unlike the selective inhibitory effect of mollugin on CYP1A2-catalyzed phenacetin O-deethylation in vitro, mollugin only significantly inhibited the activity of CYP2E1-catalyzed chlorzoxazone 6-hydroxylase in vivo. The activities of other CYPs were only slightly altered by mollugin. The results of this study suggest that mollugin might cause herb-drug interactions via the selective inhibition of CYP2E1 in vivo.
机译:已知从茜草中分离出的软体动物具有抗炎,抗癌和抗病毒活性。在本研究中,使用鸡尾酒探针测定法和LC-MS / MS研究了软体动物对雄性ICR小鼠中细胞色素P450(CYP)酶的调节作用。在以20、40或80 mg / kg的剂量向小鼠口服mollugin 3天后,研究了肝S-9组分中CYP的活性。不同于软体动物在体外对CYP1A2催化的非那西丁O-脱乙基的选择性抑制作用,软体动物仅在体内显着抑制CYP2E1催化的氯唑沙宗6-羟化酶的活性。其他CYP的活性仅被软体动物略微改变。这项研究的结果表明,软体动物可能通过选择性抑制CYP2E1在体内引起药草相互作用。

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