6533b86cfe1ef96bd12c8c48
RESEARCH PRODUCT
Anti-inflammatory activity of 5-O-demethylnobiletin, a polymethoxyflavone isolated from Sideritis tragoriganum.
Esperanza BasMiguel Cerdá-nicolásM. Carmen RecioJosé Luis RíosRosa M. GinerSalvador Máñezsubject
medicine.drug_classNeutrophilsAnti-Inflammatory AgentsPharmaceutical ScienceInflammationPharmacologyCarrageenanAnti-inflammatoryPhospholipases AAnalytical ChemistryLipoxygenasechemistry.chemical_compoundMiceDrug DiscoverymedicineAnimalsHumansRats WistarCells CulturedPharmacologyInflammationPhospholipase AbiologyOrganic ChemistryElastaseEarmedicine.diseaseFlavonesCarrageenanRatsComplementary and alternative medicineBiochemistrychemistryArachidonate 5-lipoxygenasebiology.proteinMolecular MedicineSideritisTetradecanoylphorbol AcetateFemalemedicine.symptomInfiltration (medical)description
We have studied the effect of 5- O-demethylnobiletin ( 1) on both the inflammation of mouse ears induced by repeated application of 12- O-tetradecanoylphorbol 13-acetate (TPA) and the acute mouse paw oedemas induced by carrageenan and phospholipase A (2) (PLA (2)), and determined its activity on 5-lipoxygenase (5-LOX) and elastase release/activity. Compound 1 reduced the oedema formation, cell infiltration, and tissue damage in the inflammation induced by TPA in mouse ears, along with the acute oedema induced by carrageenan in mouse paws and the acute PLA (2)-induced oedema in mouse paws. The flavone inhibited leukotriene B (4) formation in rat neutrophils and elastase release in human neutrophils, but did not reduce the expression of cyclooxygenase-2 (COX-2) in murine RAW 264.7 macrophages. These experimental results suggest that 1 may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2006-11-01 | Planta medica |