Evaluation of the cutaneous anti-inflammatory activity of azaspiranes
| العنوان: | Evaluation of the cutaneous anti-inflammatory activity of azaspiranes |
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| المؤلفون: | D. E. Griswold, M. Chabot-Fletcher, J. J. Breton, L. D. Martin, Alison M. Badger |
| المصدر: | Inflammation Research. 47:56-61 |
| بيانات النشر: | Springer Science and Business Media LLC, 1998. |
| سنة النشر: | 1998 |
| مصطلحات موضوعية: | Male, medicine.drug_class, Administration, Topical, Immunology, Prostaglandin, Inflammation, Pharmacology, Dermatitis, Contact, Leukotriene B4, Dinoprostone, Monocytes, Anti-inflammatory, Cell Line, Mice, chemistry.chemical_compound, Piperidines, In vivo, medicine, Animals, Edema, Humans, Spiro Compounds, Peroxidase, Mice, Inbred BALB C, Arachidonate 5-Lipoxygenase, Arachidonic Acid, biology, Anti-Inflammatory Agents, Non-Steroidal, NF-kappa B, Membrane Proteins, Ear, In vitro, Isoenzymes, Biochemistry, chemistry, Prostaglandin-Endoperoxide Synthases, Myeloperoxidase, Cyclooxygenase 1, biology.protein, Tetradecanoylphorbol Acetate, Arachidonic acid, Cyclooxygenase, medicine.symptom, Immunosuppressive Agents |
| الوصف: | Objective and Design: The ability of azaspiranes to modulate the acute inflammatory response in models of skin inflammation was examined.¶Material: The in vivo experiments involved the use of 5–6 age-matched male Balb/c inbred mice (22–25 g) per treatment group and a control group of 8–10 animals. In vitro mechanistic studies used RBL-1 and U937 cells lines and freshly isolated human monocytes.¶Treatment: Arachidonic acid (AA) (2 mg/20 ul in acetone) or PMA (phorbol myristate acetate) (4 ug/20 ul) were applied topically. SK&F 106615 and SK&F 106610 were administered topically either dissolved in acetone or dimethylacetamide just after the application of the irritant. Isolated cells were treated with the compounds dissolved in DMSO.¶Methods: The thickness and influx of neutrophils into the treated ears was measured as was the effects of the azaspiranes on 5-lipoxygenase activity, cyclooxygenase activity, prostaglandin and leukotriene synthesis, and the activation of the transcription factor NF-κB.¶Results: SK&F 106615 and SK&F 106610 significantly reduced inflammation in the AA- and PMA-induced inflammation models (p < 0.05) with ED50's of 179 and 120 mg/ear for edema and myeloperoxidase, respectively. The compounds did not inhibit eicosanoid biosynthesis, have a direct effect on 5-lipoxygenase or cyclooxygenase enzymes, or inhibit NF-κB.¶Conclusions: The potent anti-inflammatory and immunomodulatory activities of the azaspiranes observed in these and other studies appear to be mediated by a novel mechanism. |
| تدمد: | 1420-908X 1023-3830 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4142e967c7617331030a30d1a27e6675 https://doi.org/10.1007/s000110050270 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....4142e967c7617331030a30d1a27e6675 |
| قاعدة البيانات: | OpenAIRE |
Find this article in full text from Springer Verlag. | تدمد: | 1420908X 10233830 |
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