title: [Characteristics of uptake, transport and efflux of Z- and E-ajoenes in Caco-2 cell monolayers in vitro].
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.
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
authors.forename: Li
authors.initials: L
authors.lastname: Tian
authors.forename: Xiu-Wei
authors.initials: XW
authors.lastname: Yang
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.forename: Wei
authors.initials: W
authors.lastname: Xu
mesh_terms: D000975:Antioxidants / Q000494:pharmacology; D001205:Ascorbic Acid / Q000494:pharmacology; D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism*; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D065692:Cytochrome P-450 CYP3A Inhibitors; D004220:Disulfides / Q000737:chemistry / Q000302:isolation & purification / Q000493:pharmacokinetics*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005737:Garlic / Q000737:chemistry*; D006801:Humans; D008797:Metyrapone / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry; D019810:Sodium Azide / Q000494:pharmacology; D013237:Stereoisomerism; D013454:Sulfoxides
chemical_list: D000975:Antioxidants; D065692:Cytochrome P-450 CYP3A Inhibitors; D004220:Disulfides; D004791:Enzyme Inhibitors; D013454:Sulfoxides; D019810:Sodium Azide; C048980:ajoene; D051544:Cytochrome P-450 CYP3A; D001205:Ascorbic Acid; D008797:Metyrapone