一种内生真菌拟芒果隔孢丛赤壳(Diaporthe pseudomangiferaea)产生的地麦角新酮衍生物抑制人胚肺成纤维细胞 MRC-5 的激活。
Dothiorelone derivatives from an endophyte Diaporthe pseudomangiferaea inhibit the activation of human lung fibroblasts MRC-5 cells.
机构信息
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
出版信息
Fitoterapia. 2018 Jun;127:7-14. doi: 10.1016/j.fitote.2018.04.009. Epub 2018 Apr 14.
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-β 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 μM, 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 IC values of 8.1 and 4.4 μM, respectively.
从毒性中药天仙藤的内生真菌假隔盘孢（Diaporthe pseudomangiferaea）中分离得到了 9 个新化合物（1-6 和 16-18）和 9 个已知化合物（7-15）。通过 NMR 光谱和 MS 光谱分析确定了它们的结构。根据比旋光度或电子圆二色性法确定了绝对构型。化合物 1、4、9、11、14 和 15 在 10 μM 时分别抑制 TFG-β 诱导的人肺成纤维细胞 MRC-5 细胞的激活率为 17.4%、59.2%、62.9%、41.1%、32.9%和 52.1%，而阳性对照药吡非尼酮在 1 mM 时的抑制率为 53.2%。MTT 试验表明，化合物 13 和 14 对 BGC-823 细胞具有细胞毒性，IC 值分别为 8.1 和 4.4 μM。
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