Reference - Detail
| RRC ID | 74479 |
|---|---|
| Author | Togami K, Kanehira Y, Tada H. |
| Title | Possible involvement of pirfenidone metabolites in the antifibrotic action of a therapy for idiopathic pulmonary fibrosis. |
| Journal | Biol Pharm Bull |
| Abstract |
Pirfenidone (PFD) is the first and only clinically used antifibrotic drug for the treatment of idiopathic pulmonary fibrosis (IPF). This study evaluated the antifibrotic effects of two metabolites of PFD, 5-hydroxypirfenidone (PFD-OH) and 5-carboxypirfenidone (PFD-COOH), on WI-38 cells in an in vitro lung fibroblast model. The inhibitory effects of PFD-OH and PFD-COOH on transforming growth factor-β1 (TGF-β1)-induced collagen synthesis in WI-38 cells were evaluated by measuring intracellular hydroxyproline, a major component of the protein collagen. PFD-OH and PFD-COOH at 300 and 1000 µM concentrations significantly decreased the TGF-β1-induced hydroxyproline content in WI-38 cells. These results indicate that PFD-OH and PFD-COOH have antifibrotic activities, which inhibit collagen synthesis in fibroblasts. This study suggests that the concentrations of PFD and its metabolites should be considered in clinical therapy for IPF. |
| Volume | 36(10) |
| Pages | 1525-7 |
| Published | 2013-1-1 |
| DOI | 10.1248/bpb.b13-00452 |
| PII | DN/JST.JSTAGE/bpb/b13-00452 |
| PMID | 24088250 |
| MeSH | Anti-Inflammatory Agents, Non-Steroidal / metabolism Anti-Inflammatory Agents, Non-Steroidal / pharmacology Anti-Inflammatory Agents, Non-Steroidal / therapeutic use* Cell Line Collagen / biosynthesis* Fibroblasts / drug effects* Fibroblasts / metabolism Humans Hydroxyproline / metabolism Idiopathic Pulmonary Fibrosis / drug therapy* Idiopathic Pulmonary Fibrosis / metabolism Lung / drug effects* Lung / metabolism Lung / pathology Pyridones / metabolism Pyridones / pharmacology Pyridones / therapeutic use* Transforming Growth Factor beta1 / metabolism* |
| IF | 1.863 |
| Resource | |
| Human and Animal Cells | WI-38 |