The inhibition effect and mechanism of SY0916 on pulmonary fibrosis.

Abstract

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-β1) 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-β1. 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-β1. These findings demonstrated that SY0916 could possibly be developed as a promising candidate for the treatment of pulmonary fibrosis.

• Authors: Hai-Jing Zhang, Wen-Yang Han, Shan-Ying Peng, Yang Liu, Lian-Qiu Wu, Wen-Jie Wang
• Journal: Journal of Asian natural products research (J Asian Nat Prod Res) Vol. 16 Issue 6 Pg. 658-66 ( 2014) ISSN: 1477-2213 [Electronic] England
• PMID: 24835662 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Ketones
• Piperidines
• Platelet Membrane Glycoproteins
• Receptors, G-Protein-Coupled
• SY0916
• Transforming Growth Factor beta1
• platelet activating factor receptor
• Bleomycin

Topics

• Animals
• Bleomycin (pharmacology)
• Disease Models, Animal
• Epithelial-Mesenchymal Transition (drug effects)
• Humans
• Ketones (administration & dosage, chemistry, pharmacokinetics, pharmacology)
• Male
• Molecular Structure
• Piperidines (administration & dosage, chemistry, pharmacokinetics, pharmacology)
• Platelet Membrane Glycoproteins (antagonists & inhibitors)
• Pulmonary Fibrosis (drug therapy)
• Receptors, G-Protein-Coupled (antagonists & inhibitors)
• Transforming Growth Factor beta1 (metabolism)