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RESEARCH PRODUCT

Novel anti-inflammatory chalcone derivatives inhibit the induction of nitric oxide synthase and cyclooxygenase-2 in mouse peritoneal macrophages

Amalia UbedaGricela LoboM. José AlcarazJaime CharrisIsabel GuillénM.luisa FerrándizJosé N. DomínguezFelipe Herencia

subject

LipopolysaccharidesChalconeLipopolysaccharidemedicine.drug_classBiophysicsNitric Oxide Synthase Type IILipopolysaccharidePharmacologyBiochemistryDinoprostoneAnti-inflammatoryNitric oxideMicechemistry.chemical_compoundChalconeStructural BiologyGeneticsmedicineAnimalsCyclooxygenase-2Mouse air pouchInducible nitric oxide synthaseMolecular BiologyNitritesDose-Response Relationship DrugbiologyAnti-Inflammatory Agents Non-SteroidalZymosanZymosanProstanoidMouse peritoneal macrophageCell BiologyIsoenzymesNitric oxide synthasechemistryBiochemistryCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesEnzyme InductionMacrophages Peritonealbiology.proteinFemaleCyclooxygenaseNitric Oxide Synthase

description

AbstractIn a previous work, we tested a series of chalcone derivatives as possible anti-inflammatory compounds. We now investigate the effects of three of those compounds, CH1, CH8 and CH12, on nitric oxide and prostanoid generation in mouse peritoneal macrophages stimulated with lipopolysaccharide and in the mouse air pouch injected with zymosan, where they showed a dose-dependent inhibition with inhibitory concentration 50% values in the μM range. This effect was not the consequence of a direct inhibitory action on enzyme activities. Our results demonstrated that chalcone derivatives inhibited de novo inducible nitric oxide synthase and cyclooxygenase-2 synthesis, being a novel therapeutic approach for inflammatory diseases.

https://doi.org/10.1016/s0014-5793(99)00707-3