State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300000, China.
High-Throughput Molecular Drug Screening Centre, Tianjin International Joint Academy of Biomedicine, Tianjin 300070, China.
Molecules. 2021 Jul 26;26(15):4491. doi: 10.3390/molecules26154491.
Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive interstitial lung disease with multiple causes, characterized by excessive myofibrocyte aggregation and extracellular matrix deposition. Related studies have shown that transforming growth factor-β1 (TGF-β1) is a key cytokine causing fibrosis, promoting abnormal epithelial-mesenchymal communication and fibroblast-to-myofibroblast transition. Fedratinib (Fed) is a marketed drug for the treatment of primary and secondary myelofibrosis, targeting selective JAK2 tyrosine kinase inhibitors. However, its role in pulmonary fibrosis remains unclear. In this study, we investigated the potential effects and mechanisms of Fed on pulmonary fibrosis in vitro and in vivo. In vitro studies have shown that Fed attenuates TGF-β1- and IL-6-induced myofibroblast activation and inflammatory response by regulating the JAK2/STAT3 signaling pathway. In vivo studies have shown that Fed can reduce bleomycin-induced inflammation and collagen deposition and improve lung function. In conclusion, Fed inhibited inflammation and fibrosis processes induced by TGF-β1 and IL-6 by targeting the JAK2 receptor.
特发性肺纤维化(IPF)是一种多病因的慢性、进行性间质性肺疾病,其特征是肌成纤维细胞过度聚集和细胞外基质沉积。相关研究表明,转化生长因子-β1(TGF-β1)是导致纤维化的关键细胞因子,它促进异常上皮-间充质通讯和纤维母细胞向肌成纤维细胞转化。Fedratinib(Fed)是一种已上市的用于治疗原发性和继发性骨髓纤维化的药物,靶向选择性 JAK2 酪氨酸激酶抑制剂。然而,其在肺纤维化中的作用尚不清楚。在这项研究中,我们研究了 Fed 在体外和体内对肺纤维化的潜在作用和机制。体外研究表明,Fed 通过调节 JAK2/STAT3 信号通路来减轻 TGF-β1 和 IL-6 诱导的肌成纤维细胞激活和炎症反应。体内研究表明,Fed 可以减少博来霉素诱导的炎症和胶原沉积,改善肺功能。总之,Fed 通过靶向 JAK2 受体抑制 TGF-β1 和 IL-6 诱导的炎症和纤维化过程。