6533b857fe1ef96bd12b3b54
RESEARCH PRODUCT
Effects of some isoxazolpyrimidine derivatives on nitric oxide and eicosanoid biosynthesis
María Luisa FerrándizCarlos PeinadorJ. M. QuintelaMaría J. MoreiraMaría José AlcarazIsabel GuillénRicardo RigueraAmalia UbedaA. Vidalsubject
Leukocyte migrationNeutrophilsBlotting WesternPharmacologyNitric OxideLeukotriene B4DinoprostonePhospholipases AGeneral Biochemistry Genetics and Molecular BiologyNitric oxideMicechemistry.chemical_compoundSuperoxidesOral administrationAnimalsHumansCyclooxygenase InhibitorsGeneral Pharmacology Toxicology and PharmaceuticsNitriteOxazolesInhibitory effectCyclooxygenase 2 InhibitorsPancreatic ElastaseSuperoxideElastaseMembrane ProteinsGeneral MedicineIsoenzymesPhospholipases A2PyrimidinesBiochemistrychemistryCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesLuminescent MeasurementsCyclooxygenase 1EicosanoidsFemalelipids (amino acids peptides and proteins)Eicosanoid biosynthesisdescription
Abstract The inhibitory effect of some isoxazolpyrimidine derivatives on iNOS and COX-2 endotoxin induction in mouse peritoneal macrophages has been studied. Three of these compounds inhibited nitrite and PGE2 accumulation in a concentration dependent-manner at μM range. None of these active compounds affected iNOS, COX-2, COX-1 or PLA2 activities, although some reduced iNOS or COX-2 expression. Besides, no effect was observed on human neutrophil inflammatory responses (LTB4 biosynthesis and Superoxide or elastase release). Active compounds were assayed by oral administration in the mouse air pouch model, where they inhibited nitrite accumulation without affecting PGE 2 levels or leukocyte migration.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2000-03-04 |