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首页> 外文期刊>Pharmacognosy Research >Protective effects of goldenseal (Hydrastis canadensis L.) on acetaminophen-induced hepatotoxicity through inhibition of CYP2E1 in rats
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Protective effects of goldenseal (Hydrastis canadensis L.) on acetaminophen-induced hepatotoxicity through inhibition of CYP2E1 in rats

机译：毛eal（Hydrastis canadensis L.）通过抑制CYP2E1对大鼠对乙酰氨基酚诱导的肝毒性的保护作用

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Background:Goldenseal (Hydrastis canadensis L.) inhibits various cytochrome P450 (CYP) isoforms such as CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A in vitro. High doses of acetaminophen (APAP) generate the highly reactive intermediate, N-acetyl-p-benzoquinone imine (NAPQI), catalyzed mainly by CYP2E1. The aim of this study was to investigate the hepatoprotective effects of orally administrated goldenseal against APAP-induced acute liver failure (ALF) via inhibition of CYP2E1.Materials and Methods:Male Wistar rats were treated orally with goldenseal (300 and 1000 mg/kg) 2, 18, and 26 h before and 6 h after oral APAP (400 mg/kg) administration. Serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) activities as well as serum APAP concentration were evaluated.Results:Goldenseal extract inhibited CYP1A2, CYP2D6, CYP2E1, and CYP3A activity, and the inhibitory effect on CYP2E1 was the strongest (IC50 4.32 μg/mL). Treatment with goldenseal (300 mg/kg) significantly attenuated the APAP-induced increase in serum AST and ALT, and the hepatoprotective effect of goldenseal was stronger than that of silymarin (200 mg/kg). Moreover, serum APAP concentration was increased by goldenseal treatment, presumably as a result of the inhibitory effect of goldenseal on the metabolism of APAP to NAPQI.Conclusion:These results suggest that goldenseal ameliorates APAP-induced ALF and that this protection can likely be attributed to the inhibition of CYP2E1 activity, which generates the highly reactive intermediate of APAP.
机译：背景：Goldenseal（Hydrastis canadensis L.）在体外抑制多种细胞色素P450（CYP）亚型，例如CYP2C9，CYP2C19，CYP2D6，CYP2E1和CYP3A。高剂量的对乙酰氨基酚（APAP）产生高反应性的中间体N-乙酰基-对-苯醌亚胺（NAPQI），主要由CYP2E1催化。这项研究的目的是研究口服金枪鱼通过抑制CYP2E1对APAP诱导的急性肝衰竭（ALF）的保肝作用。材料和方法：雄性Wistar大鼠口服金枪鱼（300和1000 mg / kg）口服APAP（400 mg / kg）之前，之后2小时，18小时和26小时。测定血清天冬氨酸转氨酶（AST）和丙氨酸转氨酶（ALT）的活性以及血清APAP的浓度。 / mL）。用金毛（300 mg / kg）处理可显着减弱APAP诱导的血清AST和ALT升高，并且金毛的肝保护作用比水飞蓟素（200 mg / kg）强。此外，白毛treatment处理可能会导致血清APAP浓度升高，这可能是由于白毛on对APAP代谢成NAPQI的抑制作用。结论：这些结果表明，白毛eal改善了APAP诱导的ALF，这种保护作用可能归因于抑制CYP2E1活性，从而产生APAP的高反应性中间体。

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