Inhibition of tolbutamide 4-methylhydroxylation by a series of non-steroidal anti-inflammatory drugs in V79-NH cells expressing human cytochrome P4502C10
| العنوان: | Inhibition of tolbutamide 4-methylhydroxylation by a series of non-steroidal anti-inflammatory drugs in V79-NH cells expressing human cytochrome P4502C10 |
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| المؤلفون: | W.M. Zweers-Zeilmaker, V.J. Feron, G.J. Horbach, W.A. Kappers, E.M. de Groene, Livio Kleij, Renger F. Witkamp |
| المساهمون: | TNO Voeding |
| المصدر: | Scopus-Elsevier Xenobiotica, 12, 26, 1231-1239 |
| مصطلحات موضوعية: | Ketoprofen, Health, Toxicology and Mutagenesis, Flurbiprofen, Gene Expression, Pharmacology, Toxicology, Biochemistry, hydroxylation, Mixed Function Oxygenases, Cytochrome P-450 Enzyme System, Sulfaphenazole, Cricetinae, nonsteroid antiinflammatory agent, animal, genetics, Drug Interactions, Enzyme Inhibitors, Lung, Fenoprofen, biology, Chemistry, Anti-Inflammatory Agents, Non-Steroidal, article, cell line, General Medicine, tolbutamide 4-hydroxylase, Phenylbutazone, Enzyme inhibitor, Aryl Hydrocarbon Hydroxylases, medicine.drug, tolbutamide 4 hydroxylase, Naproxen, Diclofenac, cytochrome P450, Tolbutamide, enzyme inhibitor, Transfection, Methylation, Cricetulus, medicine, Animals, Humans, mixed function oxidase, human, Cytochrome P-450 CYP2C9, CYP2C9 protein, human, drug interaction, Cytochrome P450, unspecific monooxygenase, Drug interaction, flurbiprofen, hamster, biology.protein, genetic transfection, metabolism |
| الوصف: | 1. To study the role of cytochrome P4502C10 in the metabolism of the non-steroidal antiinflammatory drugs (NSAIDs) diclofenac, phenylbutazone, fenoprofen, ibuprofen, flurbiprofen, ketoprofen and naproxen, a cell line was developed stably expressing CYP2C10 cDNA. A retroviral vector construct, containing a human CYP2C10 cDNA, was transfected in V79-NH Chinese hamster lung cells by calcium phosphate co-precipitation. Sublines stably expressing human cytochrome P450 cDNA were established by selection with the neomycin analogue G418. 2. Enzymatic activity of CYP2C10 was detected by 4-methylhydroxylation of tolbutamide. This activity was inhibited to background levels by preincubation with the CYP2C9/10 inhibitor sulphaphenazole. 3. Preincubations with the NSAIDs ketoprofen, phenylbutazone, flurbiprofen and diclofenac (all 250 microM) caused a decrease in 4-methylhydroxylation of tolbutamide (500 microM), significantly different from control values (p0.05). Inhibition of this activity was not seen in preincubations with the NSAIDs fenoprofen, ibuprofen and naproxen (250 microM). 4. The V79-NH CYP2C10 cell line we have developed has been shown to be a useful tool to predict drug-drug interactions. |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4511f98391472303c7d8500847a4f19b http://www.scopus.com/inward/record.url?eid=2-s2.0-0030340419&partnerID=MN8TOARS |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....4511f98391472303c7d8500847a4f19b |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |