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

FEBS Letters

Herencia, Felipe²  Guillén, Isabel²  Charris, Jaime E.¹  Dominguez, José N.¹  Ubeda, Amalia²  Ferrándiz, M.Luisa²  Lobo, Gricela M.¹  Alcaraz, M.José² 

[1]Laboratory of Organic Synthesis, Faculty of Pharmacy, Central University of Venezuela, Caracas 1051, Venezuela

[2]Department of Pharmacology, University of Valencia, 46100 Burjassot, Spain

关键词: Chalcone;    Inducible nitric oxide synthase;    Cyclooxygenase-2;    Mouse peritoneal macrophage;    Lipopolysaccharide;    Mouse air pouch;    NO;    nitric oxide;    iNOS;    inducible NO synthase;    LPS;    lipopolysaccharide;    COX;    cyclooxygenase;    PG;    prostaglandin;    IFNγ;    interferon-γ;    NF-κB;    nuclear factor κB;    TNFα;    tumor necrosis factor-α;    MTT;    3-(4;    5-dimethylthiazol-2-yl)-2;    5-diphenyltetrazolium bromide;    IC50;    inhibitory concentration 50%;    AG;    aminoguanidine;    DEX;    dexamethasone;    NADPH;    nicotinamide adenine dinucleotide phosphate reduced form;   

DOI  :  10.1016/S0014-5793(99)00707-3

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

In 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.

【 授权许可】

Unknown