Brain Korea 21 PLUS Project for Medical Sciences, Department of Biochemistry and Molecular Biology, Severance Medical Research Institute, Yonsei University College of Medicine, Seoul, Korea.
College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul, Korea.
J Med Food. 2020 Jun;23(6):633-640. doi: 10.1089/jmf.2019.4670. Epub 2020 Apr 20.
Idiopathic pulmonary fibrosis (IPF) is a chronic fibrosing interstitial lung disease with a poor prognosis similar to that of malignancy. The causes of IPF are not clearly known, and there is no effective therapy to date. In this study, the natural compound plumbagin, which was isolated from root extract, was screened for p300 inhibitory activity. Plumbagin specifically inhibited the activity of p300 toward histone acetyltransferases. Plumbagin treatment significantly suppressed transforming growth factor--induced profibrotic target-gene expression and proliferation of fibroblast cell lines. Moreover, plumbagin significantly inhibited bleomycin-induced pulmonary fibrosis in mice. Taken together, these data demonstrate the inhibitory effects of plumbagin on lung fibrosis and its promise as a therapeutic agent for IPF.
特发性肺纤维化（IPF）是一种慢性纤维性间质性肺疾病，预后不良，类似于恶性肿瘤。IPF 的病因尚不清楚，目前尚无有效的治疗方法。在这项研究中，从根提取物中分离出来的天然化合物白花丹醌被筛选出具有抑制 p300 的活性。白花丹醌特异性抑制 p300 对组蛋白乙酰转移酶的活性。白花丹醌处理显著抑制转化生长因子-β诱导的成纤维细胞系的促纤维化靶基因表达和增殖。此外，白花丹醌显著抑制博来霉素诱导的小鼠肺纤维化。综上所述，这些数据表明白花丹醌对肺纤维化有抑制作用，并有望成为治疗特发性肺纤维化的药物。
