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Inflamm Res ; 66(2): 141-155, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27778057

RESUMO

OBJECTIVE AND DESIGN: This study attempted to clarify the roles of endothelins and mechanisms associated with ETA/ETB receptors in mouse models of colitis. MATERIALS AND METHODS: Colitis was induced by intracolonic administration of 2,4,6-trinitrobenzene sulfonic acid (TNBS, 1.5 mg/animal) or dextran sulfate sodium (DSS, 3%). After colitis establishment, mice received Atrasentan (ETA receptor antagonist, 10 mg/kg), A-192621 (ETB receptor antagonist, 20 mg/kg) or Dexamethasone (1 mg/kg) and several inflammatory parameters were assessed, as well as mRNA levels for ET-1, ET-2 and ET receptors. RESULTS: Atrasentan treatment ameliorates TNBS- and DSS-induced colitis. In the TNBS model was observed reduction in macroscopic and microscopic score, colon weight, neutrophil influx, IL-1ß, MIP-2 and keratinocyte chemoattractant (KC) levels, inhibition of adhesion molecules expression and restoration of IL-10 levels. However, A192621 treatment did not modify any parameter. ET-1 and ET-2 mRNA was decreased 24 h, but ET-2 mRNA was markedly increased at 48 h after TNBS. ET-2 was able to potentiate LPS-induced KC production in vitro. ETA and ETB receptors mRNA were increased at 24, 48 and 72 h after colitis induction. CONCLUSIONS: Atrasentan treatment was effective in reducing the severity of colitis in DSS- and TNBS-treated mice, suggesting that ETA receptors might be a potential target for inflammatory bowel diseases.


Assuntos
Colite/imunologia , Antagonistas do Receptor de Endotelina A/farmacologia , Endotelina-2/imunologia , Pirrolidinas/farmacologia , Animais , Atrasentana , Células Cultivadas , Colite/induzido quimicamente , Colite/tratamento farmacológico , Colite/patologia , Colo/efeitos dos fármacos , Colo/imunologia , Colo/patologia , Citocinas/imunologia , Sulfato de Dextrana , Selectina E/imunologia , Antagonistas do Receptor de Endotelina A/uso terapêutico , Antagonistas do Receptor de Endotelina B/farmacologia , Endotelina-1/genética , Endotelina-1/imunologia , Endotelina-2/genética , Leucócitos/efeitos dos fármacos , Leucócitos/imunologia , Masculino , Camundongos Endogâmicos BALB C , Infiltração de Neutrófilos/efeitos dos fármacos , Selectina-P/imunologia , Peroxidase/imunologia , Pirrolidinas/uso terapêutico , RNA Mensageiro/metabolismo , Receptor de Endotelina A/genética , Receptor de Endotelina A/imunologia , Receptor de Endotelina B/genética , Receptor de Endotelina B/imunologia , Ácido Trinitrobenzenossulfônico
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