Zhang Li, Chow Moses S S, Zuo Zhong
School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, New Territories.
J Pharm Pharmacol. 2006 Jan;58(1):37-44. doi: 10.1211/jpp.58.1.0005.
This study aimed to investigate the effect of co-occurring components from green tea on the intestinal absorption and disposition of green tea polyphenols (GTPs) using the Caco-2 cell monolayer model. The absorption and secretion transport of the four GTPs, in the form of individual pure compounds, pure compound mixtures and green tea extract, were studied in the Caco-2 cell model. Four GTPs and their metabolites were analysed by HPLC/MS and HPLC coupled with electrochemical detector. The apparent permeability coefficients (P(app)) of each compound, as well as the metabolites (mainly sulfation and methylation conjugates) generated, were compared for the different dosing formulations utilized. The results showed that the absorption transport of the four GTPs in different dosing formulations was similar. However, the secretion transport profiles of (-)-epicatechin (EC), (-)-epigallocatechin (EGC) and (-)-epigallocatechin gallate (EGCG) were altered when the GTP mixture was administered. It was suggested that transporter competition resulting in reduced efflux of EC, as well as metabolic competition resulting in reduced formation of EGC sulfate and methylated EGC sulfate, might be involved during the secretion transport of GTP mixture.
本研究旨在利用Caco-2细胞单层模型,研究绿茶中共存成分对绿茶多酚(GTPs)肠道吸收和处置的影响。在Caco-2细胞模型中,研究了四种GTPs以单一纯化合物、纯化合物混合物和绿茶提取物形式的吸收和分泌转运。通过HPLC/MS和HPLC与电化学检测器联用,分析了四种GTPs及其代谢产物。比较了不同给药制剂中各化合物以及生成的代谢产物(主要是硫酸化和甲基化共轭物)的表观渗透系数(P(app))。结果表明,四种GTPs在不同给药制剂中的吸收转运相似。然而,当给予GTP混合物时,(-)-表儿茶素(EC)、(-)-表没食子儿茶素(EGC)和(-)-表没食子儿茶素没食子酸酯(EGCG)的分泌转运曲线发生了改变。提示在GTP混合物的分泌转运过程中,可能涉及转运体竞争导致EC外排减少,以及代谢竞争导致EGC硫酸盐和甲基化EGC硫酸盐生成减少。
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