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1.
Respir Res ; 16: 12, 2015 Feb 05.
Artículo en Inglés | MEDLINE | ID: mdl-25652132

RESUMEN

BACKGROUND: Chronic obstructive pulmonary disease (COPD) is characterised by chronic pulmonary inflammation punctuated by periods of viral exacerbations. Recent evidence suggests that the combination of roflumilast with corticosteroids may improve the compromised anti-inflammatory properties of corticosteroids in COPD. We analyzed differential and combination anti-inflammatory effects of dexamethasone and roflumilast N-oxide in human bronchial epithelial cells (HBECs) stimulated with viral toll like receptor (TLR) agonists. METHODS: Lung tissue and HBECs were isolated from healthy (n = 15), smokers (n = 12) and smokers with COPD (15). TLR3 expression was measured in lung tissue and in HBECs. IL-8 secretion was measured in cell cultures after TLR3 stimulation with poly I:C 10 µg/mL. RESULTS: We found that TLR3 expression was increased by 1.95 fold (protein) and 2.5 fold (mRNA) in lung tissues from smokers with COPD and inversely correlated with lung function. The TLR3 agonist poly I:C 10 µg/mL increased the IL-8 release in HBECs that was poorly inhibited by dexamethasone in smokers (24.5%) and smokers with COPD (21.6%). In contrast, roflumilast showed similar inhibitory effects on IL-8 release in healthy (58.8%), smokers (56.6%) and smokers with COPD (50.5%). The combination of roflumilast N-oxide and dexamethasone showed additive inhibitory effects. Mechanistically, roflumilast N-oxide when combined with dexamethasone increased the expression of MKP1, and enhanced the inhibitory effects on phospho-p38, AP1 and NFκB activities which may explain the additive anti-inflammatory effects. CONCLUSIONS: Altogether, our data provide in vitro evidence for a possible clinical utility to add roflumilast on top of inhaled corticosteroid in COPD.


Asunto(s)
Corticoesteroides/farmacología , Aminopiridinas/farmacología , Antiinflamatorios/farmacología , Benzamidas/farmacología , Bronquios/efectos de los fármacos , Dexametasona/farmacología , Resistencia a Medicamentos , Células Epiteliales/efectos de los fármacos , Poli I-C/farmacología , Enfermedad Pulmonar Obstructiva Crónica/tratamiento farmacológico , Receptor Toll-Like 3/agonistas , Anciano , Bronquios/inmunología , Bronquios/metabolismo , Estudios de Casos y Controles , Células Cultivadas , Ciclopropanos/farmacología , Quimioterapia Combinada , Células Epiteliales/inmunología , Células Epiteliales/metabolismo , Femenino , Humanos , Interleucina-8/inmunología , Interleucina-8/metabolismo , Masculino , Persona de Mediana Edad , Enfermedad Pulmonar Obstructiva Crónica/genética , Enfermedad Pulmonar Obstructiva Crónica/inmunología , Enfermedad Pulmonar Obstructiva Crónica/metabolismo , Transducción de Señal/efectos de los fármacos , Fumar/efectos adversos , Receptor Toll-Like 3/genética , Receptor Toll-Like 3/inmunología , Receptor Toll-Like 3/metabolismo
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