6533b7defe1ef96bd12768af

RESEARCH PRODUCT

Influence of Dimerization of Apocynin on Its Effects in Experimental Colitis

Salvador MáñezJosé Luis RíosMarta MarínRosa M. GinerMarı A C RecioClotilde Gimeno

subject

Male0301 basic medicineDimerInterleukin-1betaPharmacologyInhibitory postsynaptic potentialMice03 medical and health scienceschemistry.chemical_compoundIn vivoAnimalsHumansMice Inbred BALB COxidase testMolecular StructurebiologyInterleukin-6Tumor Necrosis Factor-alphaMacrophagesBiphenyl CompoundsNF-kappa BAcetophenonesGeneral ChemistryColitis030104 developmental biologychemistryDiapocyninBiochemistryCyclooxygenase 2MyeloperoxidaseApocyninbiology.proteinGeneral Agricultural and Biological SciencesDimerizationNicotinamide adenine dinucleotide phosphate

description

Apocynin has been widely used as an inhibitor of the nicotinamide adenine dinucleotide phosphate oxidase (NADPH-oxidase) system and shows promise as an anti-inflammatory drug. Diapocynin, the dimeric product generated by the oxidation of apocynin in the presence of myeloperoxidase (MPO), is supposed to be its active form. In this study, diapocynin has been chemically synthesized and its activity on several inflammatory mediators in LPS-stimulated RAW 264.7 macrophages and its anti-inflammatory effect on ulcerative colitis induced by dextran sodium sulfate (DSS) in mice analyzed. We found that diapocynin showed higher inhibitory activity than apocynin. The dimer reduced ROS production, TNF-α, IL-6, and IL-1β levels and inhibited iNOS and COX-2 expression as well as decreased NO and PGE2 production induced in LPS-stimulated RAW 264.7 cells. The anti-inflammatory molecular mechanism of diapocynin was associated with the suppression of NF-κB activation. However, these results were not paralleled by in vivo st...

yearjournalcountryeditionlanguage
2017-05-16Journal of Agricultural and Food Chemistry
https://doi.org/10.1021/acs.jafc.7b00872