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莪术油对硫代乙酰胺诱导的肝硬化大鼠P450活性的影响。

Effects of zedoary turmeric oil on P450 activities in rats with liver cirrhosis induced by thioacetamide.

作者信息

Cheng Jing-Jing, Yang Nai-Bin, Wu Liang, Lin Jia-Le, Dai Ge-Xin, Zhu Jia-Yin

机构信息

Affiliated Stomatology Hospital, Wenzhou Medical University Wenzhou, China.

The First Affiliated Hospital, Wenzhou Medical University Wenzhou, China.

出版信息

Int J Clin Exp Pathol. 2014 Oct 15;7(11):7854-62. eCollection 2014.

Abstract

The aim of this study was to elucidate the effects of zedoary turmeric oil (ZTO) on P450 activities (CYP1A2, CYP2C9, CYP2C19, CYP2B6, CYP2D6 and CYP3A4) in rats with liver cirrhosis induced by thioacetamide (TAA). For the induction of liver cirrhosis, rats were given TAA in their drinking water at a concentration of 0.03% for consecutive 5 weeks and then 0.04% for the next consecutive 5 weeks throughout the establishment of cirrhosis. Then the cirrhotic rats were ip given saline, ZTO 100, 200 and 400 mg/kg, respectively, once daily for 2 weeks. When cirrhosis model was established at week 10, all rats of five groups were administered intragastrically with 15 mg/kg phenacetin, 0.6 mg/kg tolbutamide, 15 mg/kg omeprazole, 15 mg/kg bupropion, 15 mg/kg metoprolol, and 10 mg/kg midazolam. Blood samples were collected at a series of time-points and the concentrations of probe drugs in plasma were determined by HPLC-MS/MS. The degree of liver cirrhosis was assessed by HE staining. The serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) from the model group increased by approximately 4-fold, and a decreased level of albumin (Alb) was also observed, as compared to the control group (P < 0.05). However, ZTO was found to reverse those changes of serum levels observed in the model group, and the 200 mg/kg ZTO treatment group showed the most obvious reverse tendency with significantly decreased ALT, AST and increased Alb levels (P < 0.05). The results indicated that ZTO with the dose of 100 mg/kg could inhibit the activities of CYP450 isoforms CYP2C9 and CYP2D6 in vivo in cirrhotic rats induced by TAA, while ZTO with the dose of 400 mg/kg could induce the activity of CYP2C19 in vivo in cirrhotic rats induced by TAA. However, ZTO showed no influence on cirrhotic rat hepatic CYP1A2, CYP2B6 and CYP3A4 activity in vivo. This has certain guiding significance to clinical treatment.

摘要

本研究旨在阐明莪术油(ZTO)对硫代乙酰胺(TAA)诱导的肝硬化大鼠体内P450酶活性(CYP1A2、CYP2C9、CYP2C19、CYP2B6、CYP2D6和CYP3A4)的影响。为诱导肝硬化,在整个肝硬化建立过程中,大鼠连续5周饮用含0.03% TAA的饮用水,随后连续5周饮用含0.04% TAA的饮用水。然后,对肝硬化大鼠分别腹腔注射生理盐水、100、200和400 mg/kg的ZTO,每日1次,持续2周。在第10周建立肝硬化模型时,五组所有大鼠均灌胃给予15 mg/kg非那西丁、0.6 mg/kg甲苯磺丁脲、15 mg/kg奥美拉唑、15 mg/kg安非他酮、15 mg/kg美托洛尔和10 mg/kg咪达唑仑。在一系列时间点采集血样,采用HPLC-MS/MS测定血浆中探针药物的浓度。通过HE染色评估肝硬化程度。与对照组相比,模型组血清丙氨酸氨基转移酶(ALT)和天冬氨酸氨基转移酶(AST)水平升高约4倍,同时白蛋白(Alb)水平降低(P < 0.05)。然而,发现ZTO可逆转模型组观察到的血清水平变化,200 mg/kg ZTO治疗组显示出最明显的逆转趋势,ALT、AST显著降低,Alb水平升高(P < 0.05)。结果表明,100 mg/kg剂量的ZTO可抑制TAA诱导的肝硬化大鼠体内CYP450同工酶CYP2C9和CYP2D6的活性,而400 mg/kg剂量的ZTO可诱导TAA诱导的肝硬化大鼠体内CYP2C19的活性。然而,ZTO对肝硬化大鼠肝脏CYP1A2、CYP2B6和CYP3A4活性无体内影响。这对临床治疗具有一定的指导意义。

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