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[体外Caco-2细胞单层中Z-和E-大蒜烯的摄取、转运和外排特性]

[Characteristics of uptake, transport and efflux of Z- and E-ajoenes in Caco-2 cell monolayers in vitro].

作者信息

Tian Li, Yang Xiu-Wei, Wang Ying, Xu Wei

机构信息

The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.

出版信息

Yao Xue Xue Bao. 2007 Jan;42(1):87-92.

Abstract

The characteristics of uptake, transepithelial transport and efflux of Z- and E-ajoenes isolated from the bulbs of Allium sativum were studied. A human colon cell model Caco-2 cell monolayers in vitro cultured had been applied to study the characteristics of uptake, transepithelial transport and efflux of Z- and E-ajoenes. The quantitative determination of Z- and E-ajoenes was performed by high-performance liquid chromatography. Z- and E-Ajoenes can be detected only in the apical side and can be metabolized, but both compounds can not be transported from apical-to-basolateral and basolateral-to-apical directions in cultured Caco-2 cell monolayers. The metabolism of Z- and E-ajoenes in Caco-2 cell monolayers can be partially inhibited by vitamin C as an anti-oxidant, metyrapone as an inhibitor to subtype CYP3A of cytochrome P450 drug metabolism enzymes, and sodium azide as an inhibitor to ATP production. It is shown that neither Z-ajoene nor E-ajoene can pass through Caco-2 cell monolayers, and that they can be metabolized by the cells. The metabolism might be in correlation with cytochrome P450 drugs metabolism enzymes in Caco-2 cell monolayers.

摘要

研究了从大蒜鳞茎中分离出的Z-和E-ajoene的摄取、跨上皮转运和外排特性。应用体外培养的人结肠细胞模型Caco-2细胞单层来研究Z-和E-ajoene的摄取、跨上皮转运和外排特性。采用高效液相色谱法对Z-和E-ajoene进行定量测定。Z-和E-ajoene仅能在顶侧检测到且可被代谢,但在培养的Caco-2细胞单层中,这两种化合物均不能从顶侧向基底侧以及从基底侧向顶侧转运。Caco-2细胞单层中Z-和E-ajoene的代谢可被作为抗氧化剂的维生素C、作为细胞色素P450药物代谢酶CYP3A亚型抑制剂的甲吡酮以及作为ATP生成抑制剂的叠氮化钠部分抑制。结果表明,Z-ajoene和E-ajoene均不能穿过Caco-2细胞单层,且它们可被细胞代谢。这种代谢可能与Caco-2细胞单层中的细胞色素P450药物代谢酶相关。

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