6533b859fe1ef96bd12b7892

RESEARCH PRODUCT

Potential Antipsoriatic Avarol Derivatives as Antioxidants and Inhibitors of PGE2 Generation and Proliferation in the HaCaT Cell Line

Maria AmigóMaya MitovaSalvatore De RosaMaría Carmen TerencioC. IodiceMiguel Payá

subject

KeratinocytesPharmaceutical ScienceAntioxidantsDinoprostoneAnalytical ChemistryInhibitory Concentration 50Structure-Activity Relationshipchemistry.chemical_compoundDrug DiscoverymedicineHumansStructure–activity relationshipCytotoxicityPharmacologyL-Lactate DehydrogenaseSuperoxideCell growthOrganic ChemistryFree Radical ScavengersSalicylatesIn vitroHaCaTmedicine.anatomical_structureItalyComplementary and alternative medicinechemistryBiochemistryCell cultureMolecular MedicineKeratinocyteSesquiterpenes

description

The synthesis and structure-activity relationships for a series of 14 new avarol derivatives as antioxidants and inhibitors of cell proliferation and PGE(2) generation in human keratinocytes are described. Compound 6 (thiosalicylic derivative) was the most potent inhibitor of superoxide generation in human neutrophils and also potently inhibited PGE(2) generation in the human keratinocyte HaCaT cell line. Compound 7(3'-methylaminoavarone) presented the best antiproliferative profile, by the inhibition of (3)H-thymidine incorporation in HaCaT cells, with potency similar to the reference compound anthralin. None of the avarol derivatives showed any sign of cytotoxicity measured as LDH release in treated keratinocytes. The potency and pharmacological profile of derivatives are also discussed.

yearjournalcountryeditionlanguage
2004-07-16Journal of Natural Products
https://doi.org/10.1021/np049873n