Dothiorelone derivatives from an endophyte Diaporthe pseudomangiferaea inhibit the activation of human lung fibroblasts MRC-5 cells
Dothiorelone derivatives from an endophyte Diaporthe pseudomangiferaea inhibit the activation of human lung fibroblasts MRC-5 cells
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来自内生菌 Diaporthe pseudomangiferaea 的 Dothiorelone 衍生物抑制人肺成纤维细胞 MRC-5 细胞的活化
DOI：
10.1016/j.fitote.2018.04.009
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发表时间：
2018-06-01
期刊：
影响因子：
3.4
通讯作者：
Liu, Yunbao
中科院分区：
文献类型：
--
作者：
Liu, Zhen;Zhao, Jingyi;Liu, Yunbao
从有毒的中国民间药材瓦通过核磁共振谱和质谱分析确定了它们的结构。根据比旋光度或电子圆二色性方法确定了其绝对构型。化合物1、4、9、11、14和15在10 μ M时分别抑制TFG-β诱导的人肺成纤维细胞MRC-5细胞的活化17.4%、59.2%、62.9%、41.1%、32.9%和52.1%，而阳性对照吡非尼酮在1 mM时显示53.2%的抑制率。MTT测定显示化合物13和14对BGC-823细胞显示细胞毒性，IC 50值分别为8.1和4.4 μ M。
Nine new compounds (1-6 and 16-18) and nine known compounds (7-15) were isolated from Diaporthe pseudomangiferaea, an endophytic fungus obtained from the leaves of the toxic Chinese folk medicine Tylophora ouata. Their structures were elucidated by NMR spectroscopy and MS spectrometry analyses. The absolute configurations were established according to the specific rotation or electron circular dichroism method. Compounds 1, 4, 9, 11, 14 and 15 inhibited the TFG-beta induced activation of human lung fibroblasts MRC-5 cells by 17.4%, 59.2%, 62.9%, 41.1%, 32.9% and 52.1% at 10 mu M, respectively, while positive control pirfenidone showed 53.2% inhibition rate at 1 mM. The MTT assay showed that compounds 13 and 14 displayed cytotoxicity against BGC-823 cells, with IC50 values of 8.1 and 4.4 mu M, respectively.