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菊花提取物增加大鼠体内维生素 A 的暴露量并非通过诱导 CYP1A1、CYP1A2 和 CYP2B1。

Increased exposure of vitamin A by Chrysanthemum morifolium Ramat extract in rat was not via induction of CYP1A1, CYP1A2, and CYP2B1.

机构信息

Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical Univ, Nanjing, PR China.

出版信息

J Food Sci. 2012 Jun;77(6):H121-7. doi: 10.1111/j.1750-3841.2012.02732.x.

Abstract

The aim of this study was to investigate the effect of Chrysanthemum morifolium Ramat (CM) extract on the pharmacokinetics of retinol and activities of cytochrome P450s (CYP450s) related to retinoid metabolism. Rats were treated with CM extract for 15 d. Plasma concentrations of retinol were measured following oral administration of retinol (45 mg/kg). Basal levels of retinol and retinoic acid in serum and liver were also measured. 7-Ethoxyresorufin-O-deethylase activity, phenacetin-O-deethylase activity, and 7-pentoxyresorufin-O-deethylase activities were used to assay the activities of CYP1A1, CYP1A2, and CYP2B1 in hepatic microsomes of rats, respectively. Protein expressions of the 3 CYP450s were measured by western blot. Our studies demonstrated that CM extract dose-dependently increased basal level of retinol in serum. In pharmacokinetic experiment, CM extract dose-dependently increased plasma concentrations of retinol after oral administration of retinol to rats treated with CM extract. But activities and expressions of CYP1A1, CYP1A2, and CYP2B1 in hepatic microsomes of rats were also induced by CM extract.

摘要

本研究旨在探讨菊花(CM)提取物对视黄醇药代动力学和与类视黄醇代谢相关的细胞色素 P450s(CYP450s)活性的影响。大鼠用 CM 提取物处理 15 天。在给予大鼠视黄醇(45mg/kg)后,测量视黄醇的血浆浓度。还测量了血清和肝脏中视黄醇和视黄酸的基础水平。使用 7-乙氧基香豆素-O-脱乙基酶活性、苯乙酮-O-脱乙基酶活性和 7-戊氧基香豆素-O-脱乙基酶活性分别测定大鼠肝微粒体中 CYP1A1、CYP1A2 和 CYP2B1 的活性。通过 Western blot 测量 3 种 CYP450s 的蛋白表达。我们的研究表明,CM 提取物剂量依赖性地增加血清中视黄醇的基础水平。在药代动力学实验中,CM 提取物剂量依赖性地增加了给予 CM 提取物处理的大鼠口服视黄醇后的血浆视黄醇浓度。但 CM 提取物也诱导了大鼠肝微粒体中 CYP1A1、CYP1A2 和 CYP2B1 的活性和表达。

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