Characteristics of uptake, transport and efflux of Z- and E-ajoenes in Caco-2 cell monolayers in vitro.
- Author:
Li TIAN
1
;
Xiu-Wei YANG
;
Ying WANG
;
Wei XU
Author Information
1. The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
- Publication Type:Journal Article
- MeSH:
Antioxidants;
pharmacology;
Ascorbic Acid;
pharmacology;
Biological Transport;
drug effects;
Caco-2 Cells;
Cell Membrane;
drug effects;
metabolism;
Cytochrome P-450 CYP3A;
metabolism;
Cytochrome P-450 CYP3A Inhibitors;
Disulfides;
chemistry;
isolation & purification;
pharmacokinetics;
Enzyme Inhibitors;
pharmacology;
Garlic;
chemistry;
Humans;
Metyrapone;
pharmacology;
Plants, Medicinal;
chemistry;
Sodium Azide;
pharmacology;
Stereoisomerism
- From:
Acta Pharmaceutica Sinica
2007;42(1):87-92
- CountryChina
- Language:Chinese
-
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.
