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1.
J Asian Nat Prod Res ; 16(6): 658-66, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24835662

RESUMO

SY0916 is a new platelet-activating factor receptor antagonist developed by our institute. In this study, the inhibitory effect of SY0916 on pulmonary fibrosis was investigated in epithelial-mesenchymal transition (EMT) induced by transforming growth factor beta 1 (TGF-ß1) in vitro and a pulmonary fibrosis animal model induced by bleomycin (BLM). The results showed that SY0916 could inhibit the EMT of A549 cells induced with TGF-ß1. In vivo, SY0916 administration significantly ameliorated the BLM-mediated histological changes, reduced main biochemical parameters related to pulmonary fibrosis such as hydroxyproline and glutathione, and also notably attenuated the expression of key pro-fibrotic mediator, TGF-ß1. These findings demonstrated that SY0916 could possibly be developed as a promising candidate for the treatment of pulmonary fibrosis.


Assuntos
Transição Epitelial-Mesenquimal/efeitos dos fármacos , Cetonas/farmacologia , Piperidinas/farmacologia , Glicoproteínas da Membrana de Plaquetas/antagonistas & inibidores , Fibrose Pulmonar/tratamento farmacológico , Receptores Acoplados a Proteínas G/antagonistas & inibidores , Fator de Crescimento Transformador beta1/metabolismo , Animais , Bleomicina/farmacologia , Modelos Animais de Doenças , Humanos , Cetonas/administração & dosagem , Cetonas/química , Cetonas/farmacocinética , Masculino , Estrutura Molecular , Piperidinas/administração & dosagem , Piperidinas/química , Piperidinas/farmacocinética
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