Use of a continous assay of oxygen consumption to evaluate the pharmacology of 5-lipoxygenase inhibitors
العنوان: | Use of a continous assay of oxygen consumption to evaluate the pharmacology of 5-lipoxygenase inhibitors |
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المؤلفون: | D. E. Griswold, W. DeWolf, L. Hillegass, P. Keller, J.J. Breton, M. Chabot-Fletcher |
المصدر: | Prostaglandins, Leukotrienes and Essential Fatty Acids. 49:929-937 |
بيانات النشر: | Elsevier BV, 1993. |
سنة النشر: | 1993 |
مصطلحات موضوعية: | Clinical Biochemistry, Drug Evaluation, Preclinical, In Vitro Techniques, Leukotriene B4, High-performance liquid chromatography, Monocytes, chemistry.chemical_compound, Oxygen Consumption, Biosynthesis, Tumor Cells, Cultured, Animals, Humans, Hydroxyurea, Lipoxygenase Inhibitors, chemistry.chemical_classification, Leukotriene, Chromatography, biology, Imidazoles, Biological activity, Cell Biology, 5,8,11,14-Eicosatetraynoic Acid, Enzyme assay, Rats, Enzyme, chemistry, Biochemistry, Enzyme inhibitor, Arachidonate 5-lipoxygenase, biology.protein |
الوصف: | A variety of assay systems have been utilized to evaluate the inhibition of the key enzyme in leukotriene (LT) biosynthesis, 5-lipoxygenase (5-LO). We have developed an assay utilizing a cytosolic preparation of 5-LO from rat basophilic leukemia (RBL-1) cells. Enzyme activity was monitored by continous measurement of oxygen consumption. High performance liquid chromatography (HPLC) analysis of products showed exclusive generation of 5-LO products. The assay proved useful for the evaluation of a variety of chemical classes of lipoxygenase inhibitors and clearly differentiated those compounds which extended the lag phase (e.g. A-64077) as opposed to the propagation phase of the enzyme activity (e.g. SK & F 105561). The data generated were in reasonable agreement with results from the assay of isolated human monocyte 5-LO and, with the exception of compounds which appear to have a significant effect on 5-LO translocation (e.g. MK-886 and Wy-49 232), inhibition of LT production by intact monocytes. This assay system proved to be a convenient and informative method to analyze inhibition of 5-LO activity. |
تدمد: | 0952-3278 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f489db31887e50bda30570fe5119472 https://doi.org/10.1016/0952-3278(93)90178-y |
حقوق: | CLOSED |
رقم الأكسشن: | edsair.doi.dedup.....4f489db31887e50bda30570fe5119472 |
قاعدة البيانات: | OpenAIRE |
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