دورية أكاديمية
Induction of cytochrome P450 (CYP)1A1, CYP1A2, and CYP3A4 but not of CYP2C9, CYP2C19, multidrug resistance (MDR-1) and multidrug resistance associated protein (MRP-1) by prototypical inducers in human hepatocytes.
العنوان: | Induction of cytochrome P450 (CYP)1A1, CYP1A2, and CYP3A4 but not of CYP2C9, CYP2C19, multidrug resistance (MDR-1) and multidrug resistance associated protein (MRP-1) by prototypical inducers in human hepatocytes. |
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المؤلفون: | Runge D; Klinik für Innere Medizin I, Martin Luther Universität Halle-Wittenberg, Halle, 06097, Federal Republic of Germany., Köhler C, Kostrubsky VE, Jäger D, Lehmann T, Runge DM, May U, Stolz DB, Strom SC, Fleig WE, Michalopoulos GK |
المصدر: | Biochemical and biophysical research communications [Biochem Biophys Res Commun] 2000 Jun 24; Vol. 273 (1), pp. 333-41. |
نوع المنشور: | Journal Article; Research Support, U.S. Gov't, P.H.S. |
اللغة: | English |
بيانات الدورية: | Publisher: Elsevier Country of Publication: United States NLM ID: 0372516 Publication Model: Print Cited Medium: Print ISSN: 0006-291X (Print) Linking ISSN: 0006291X NLM ISO Abbreviation: Biochem Biophys Res Commun Subsets: MEDLINE |
أسماء مطبوعة: | Publication: <2002- >: San Diego, CA : Elsevier Original Publication: New York, Academic Press. |
مواضيع طبية MeSH: | Aryl Hydrocarbon Hydroxylases* , Steroid 16-alpha-Hydroxylase*, Cytochrome P-450 Enzyme System/*analysis , Cytochrome P-450 Enzyme System/*biosynthesis , Liver/*drug effects , Liver/*enzymology, ATP Binding Cassette Transporter, Subfamily B, Member 1/analysis ; ATP Binding Cassette Transporter, Subfamily B, Member 1/genetics ; ATP-Binding Cassette Transporters/analysis ; ATP-Binding Cassette Transporters/genetics ; Blotting, Western ; Cell Size/drug effects ; Cells, Cultured ; Cytochrome P-450 CYP1A1/biosynthesis ; Cytochrome P-450 CYP1A1/metabolism ; Cytochrome P-450 CYP1A2/biosynthesis ; Cytochrome P-450 CYP1A2/metabolism ; Cytochrome P-450 CYP2C19 ; Cytochrome P-450 CYP2C9 ; Cytochrome P-450 CYP2E1/metabolism ; Cytochrome P-450 CYP3A ; Cytochrome P-450 Enzyme System/metabolism ; Enzyme Induction/drug effects ; Epidermal Growth Factor/pharmacology ; Hepatocyte Growth Factor/pharmacology ; Humans ; Isoenzymes/analysis ; Isoenzymes/biosynthesis ; Liver/cytology ; Liver/ultrastructure ; Methylcholanthrene/pharmacology ; Mixed Function Oxygenases/biosynthesis ; Mixed Function Oxygenases/metabolism ; Multidrug Resistance-Associated Proteins ; Neoplasm Proteins/genetics ; Phenobarbital/pharmacology ; RNA, Messenger/genetics ; RNA, Messenger/metabolism ; Rifampin/pharmacology ; Steroid Hydroxylases/metabolism ; Vault Ribonucleoprotein Particles/genetics ; beta-Naphthoflavone/pharmacology |
مستخلص: | Human hepatocytes cultured serum-free for up to 6 weeks were used to study expression and induction of enzymes and membrane transport proteins involved in drug metabolism. Phase I drug metabolizing enzymes cytochrome P450 (CYP)1A1, CYP1A2, CYP2C9, CYP2C19, CYP2E1, and CYP3A4 were detected by Western blot analyses and, when appropriate, by enzymatic assays for ethoxyresorufin-O-deethylase(EROD)-activity and testosterone-6beta-hydroxylase(T6H)-activity. Expression of the membrane transporter multi-drug resistance protein (P-glycoprotein, MDR-1), multidrug resistance-associated protein (MRP-1), and lung-resistance protein (LRP) was maintained during the culture as detected by RT-PCR and Western blot analyses. Model inducers like rifampicin, phenobarbital, or 3-methylcholanthrene and beta-naphtoflavone were able to induce CYP1A or CYP3A4 as well as EROD or T6H activities for up to 30 days. CYP2C9, CYP2C19 and CYP2E1 expression was maintained but not inducible for 48 days. Also, rifampicin and phenobarbital were unable to increase MDR-1 and MRP-1 protein levels significantly. (Copyright 2000 Academic Press.) |
معلومات مُعتمدة: | CA30241 United States CA NCI NIH HHS; CA35373 United States CA NCI NIH HHS |
المشرفين على المادة: | 0 (ATP Binding Cassette Transporter, Subfamily B, Member 1) 0 (ATP-Binding Cassette Transporters) 0 (Isoenzymes) 0 (Multidrug Resistance-Associated Proteins) 0 (Neoplasm Proteins) 0 (RNA, Messenger) 0 (Vault Ribonucleoprotein Particles) 0 (major vault protein) 56-49-5 (Methylcholanthrene) 6051-87-2 (beta-Naphthoflavone) 62229-50-9 (Epidermal Growth Factor) 67256-21-7 (Hepatocyte Growth Factor) 9035-51-2 (Cytochrome P-450 Enzyme System) EC 1.- (Mixed Function Oxygenases) EC 1.14.- (Steroid Hydroxylases) EC 1.14.13.- (CYP2C9 protein, human) EC 1.14.13.- (Cytochrome P-450 CYP2C9) EC 1.14.13.- (Cytochrome P-450 CYP2E1) EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases) EC 1.14.14.1 (CYP1A2 protein, human) EC 1.14.14.1 (CYP2C19 protein, human) EC 1.14.14.1 (CYP3A protein, human) EC 1.14.14.1 (Cytochrome P-450 CYP1A1) EC 1.14.14.1 (Cytochrome P-450 CYP1A2) EC 1.14.14.1 (Cytochrome P-450 CYP2C19) EC 1.14.14.1 (Cytochrome P-450 CYP3A) EC 1.14.14.1 (Steroid 16-alpha-Hydroxylase) EC 1.14.14.55 (CYP3A4 protein, human) VJT6J7R4TR (Rifampin) YQE403BP4D (Phenobarbital) |
تواريخ الأحداث: | Date Created: 20000630 Date Completed: 20000727 Latest Revision: 20181211 |
رمز التحديث: | 20240627 |
DOI: | 10.1006/bbrc.2000.2902 |
PMID: | 10873607 |
قاعدة البيانات: | MEDLINE |
تدمد: | 0006-291X |
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DOI: | 10.1006/bbrc.2000.2902 |