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深海真菌Aspergillus puniceus A2次级代谢产物及其药物开发潜力

Secondary metabolites of a deep-sea-derived fungus Aspergillus puniceus A2 and their potential in drug development

  • 摘要: 本研究采用硅胶柱层析、高效液相色谱等方法对深海真菌Aspergillus puniceus A2发酵产物进行了化学成分分离纯化,通过核磁共振等现代波谱学方法,同时结合相关文献进行数据分析,鉴定化合物的结构。从A. puniceus A2中分离鉴定出6个呫吨酮并双呋喃环类化合物,化学结构分别确定为Austocystin I(1)、Austocystin G(2)、6-methoxyl Austocystin A(3)、Austocystin F(4)、F02ZA-1593B2(5)、Austocystin A(6),化合物1~6均为首次从该真菌中分离得到。通过细胞毒性和抗炎活性评价发现化合物1、2、4和6在20 μmol/L浓度时,对肝星状细胞LX2显示出毒性作用,提示其可能有抗肝纤维化的作用;化合物2、3、5和6在20 μmol/L浓度时,能显著抑制LPS诱导小鼠单核巨噬细胞RAW264.7细胞分泌NO,显示出一定的抗炎活性。

     

    Abstract: The fermentation product of a deep-sea-derived fungus Aspergillus puniceus A2 was isolated and purified with silica gel column and highperformance liquid chromatography, which isolated 6 compounds. The chemical structures of the 6 compounds were identified as Austocystin I(1), Austocystin G(2), 6-methoxyl Austocystin A(3), Austocystin F(4), F02ZA-1593B2(5), and Austocystin A(6) by NMR spectrum analysis and compared with literature data. All the isolated compounds were reported firstly in this fungus.Among them, compounds 1, 2, 4 and 6 showed toxic effects on hepatic stellate cells LX2 at the concentration of 20 μmol/L, suggesting that they may have anti-hepatic fibrosis effects.Compounds 2, 3, 5 and 6 inhibited significantly the LPS-induced NO secretion in mouse monocyte macrophage RAW264.7 at 20 μmol/L, showing anti-inflammatory activity.

     

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