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1.
Circ Heart Fail ; 8(3): 629-35, 2015 May.
Artículo en Inglés | MEDLINE | ID: mdl-25991805
2.
Circulation ; 114(1 Suppl): I270-4, 2006 Jul 04.
Artículo en Inglés | MEDLINE | ID: mdl-16820585

RESUMEN

BACKGROUND: We previously reported that the functional mutation of Toll-like receptor 4 (TLR4) in C3H/HeJ mice subjected to myocardial ischemia-reperfusion (MI/R) injury resulted in an attenuation of myocardial infarction size. To investigate the ligand-activating TLR4 during MI/R injury, we evaluated the effect of eritoran, a specific TLR4 antagonist, on MI/R injury, with the goal of defining better therapeutic options for MI/R injury. METHODS AND RESULTS: C57BL/6 mice received eritoran (5 mg/kg) intravenously 10 minutes before 30 minutes of in situ of transient occlusion of the left anterior descending artery, followed by 120 minutes of reperfusion. Infarct size was measured using triphenyltetrazoliumchloride staining. A c-Jun NH(2)-terminal kinase (JNK) activation was determined by Western blotting, nuclear factor (NF)-kappaB activity was detected by gel-shift assay, and cytokine expression was measured by ribonuclease protection assay. Mice treated with eritoran developed significantly smaller infarcts when compared with mice treated with vehicle alone (21.0+/-6.4% versus 30.9+/-13.9%; P=0.041). Eritoran pretreatment resulted in a reduction in JNK phosphorylation (eritoran versus vehicle: 3.98+/-0.81 versus 7.01+/-2.21-fold increase; P=0.020), less nuclear NF-kappaB translocation (2.70+/-0.35 versus 7.75+/-0.60-fold increase; P=0.00007), and a decrease in cytokine expression (P<0.05). CONCLUSIONS: We conclude that inhibition of TLR4 with eritoran in an in situ murine model significantly reduces MI/R injury and markers of an inflammatory response.


Asunto(s)
Disacáridos/uso terapéutico , Daño por Reperfusión Miocárdica/prevención & control , Fosfatos de Azúcar/uso terapéutico , Receptor Toll-Like 4/antagonistas & inhibidores , Animales , Biomarcadores , Citocinas/biosíntesis , Citocinas/genética , Disacáridos/farmacología , Evaluación Preclínica de Medicamentos , Activación Enzimática/efectos de los fármacos , Inflamación , Proteínas Quinasas JNK Activadas por Mitógenos/metabolismo , Masculino , Ratones , Ratones Endogámicos C57BL , Proteínas Quinasas Activadas por Mitógenos/metabolismo , Infarto del Miocardio/complicaciones , Infarto del Miocardio/patología , FN-kappa B/metabolismo , Fosforilación/efectos de los fármacos , Procesamiento Proteico-Postraduccional/efectos de los fármacos , Fosfatos de Azúcar/farmacología , Receptor Toll-Like 4/fisiología
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