| 韩巧英,杨 帆,甘建红,等.海绵共附生真菌Penicillium chrysogenum次级代谢产物的化学成分及生物活性研究[J].中国海洋药物,2018,37(6):15-22. |
| 海绵共附生真菌Penicillium chrysogenum次级代谢产物的化学成分及生物活性研究 |
| Study on the Chemistry and Bioactivity of Secondary Metabolites from Sponge-Derived Fungus Penicillium Chrysogenum |
| 投稿时间：2018-05-23 修订日期：2018-07-11 |
| DOI： |
| 中文关键词: 隋氏蒂壳海绵 海洋真菌 活性化合物 次级代谢产物 生物分子相互作用 |
| English Keywords:T. swinhoei marine fungus bioactive compounds secondary metabolites biomolecular interactions |
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| 中文摘要: |
| 目的 对分离自西沙隋氏蒂壳海绵共附生真菌Penicilliumchrysogenum的次级代谢产物进行化学成分及其生物活性研究，以期发现结构特异并且活性良好的次级代谢产物。方法 对隋氏蒂壳海绵共附生真菌Penicilliumchrysogenum用真菌2号培养基发酵，发酵后的菌丝体采用溶剂提取、萃取和现代色谱分离纯化手段，再运用现代核磁波谱技术并结合高分辨质谱鉴定化合物结构。基于微阵列技术的表面等离子体共振成像（SPRi）系统，检测化合物与肿瘤相关蛋白的相互作用，并提供化合物与肿瘤相关蛋白的结合动力学数据。结果 通过分离隋氏蒂壳海绵共附生真Penicilliumchrysogenum的菌丝体提取物，从中分离鉴定了7个单体化合物，鉴定结果为conidiogenone（1）、2-acetylquinazolin-4(3H)-one（2）、15β-hydroxyl-(22E,24R)-ergosta-3,5,8,22-tetraen-on（3）、ergosta-4,6,8(14),22-tetraen-3-one（4）、
2-((2E,4E)-hexa-2,4-dienoyl)-5,6-dihydroxy-4,6-dimethylcyclohex-4-ene-1,3-dione（5）、(22E)-5α,8α-epidioxyergosta-6,22-dien-3β-ol（6）、2-(1-hydroxyethyl)quinazolin-4(3H)-one（7）。结论 化合物3和6是从Penicillium属内第一次分离得到，化合物4是从真菌Penicilliumchrysogenum中第一次分离得到，化合物5与肿瘤蛋白VEGFR-1、FGFR有亲和作用，KD的数值分别为7.78×10-3和1.44×10-1 μmol/L。 |
| English Summary: |
| Objective The secondary metabolites of the strain Penicilliumchrysogenum, an epiphytic fungus isolated from the Xisha sponge T.swinhoei and their bioactivity were studied, in order to find secondary metabolites with structural specificity and strong activities. Methods The fungus Penicilliumchrysogenum was fermented with Fungus No.2 medium, the mycelium was extracted and purified by modern chromatography method. The structures of isolated compounds were identified by modern spectroscopic techniques combined with HRMS. The interaction of compounds with tumor-associated proteins was detected with the surface plasmon resonance imaging (SPRi) system, based on microarray technology, which also provides kinetic data. Results Seven compounds were isolated from the mycelium of strain Penicilliumchrysogenum, which was isolated from the sponge T.swinhoei.They were identified as conidiogenone (1), 2-acetylquinazolin-4(3H)-one (2), 15β-hydroxyl-(22E,24R)-ergosta-3,5,8,22-tetraen-one (3), ergosta-4,6,8(14),22-tetraen-3-one (4), 2-((2E,4E)-hexa-2,4-dienoyl)-5,6-dihydroxy-4,6-dimethylcyclohex-4-ene-1,3-dione (5), (22E)-5α,8α-epidioxyergosta-6,22-dien-3β-ol (6) and 2-(1-hydroxyethyl)quinazolin-4(3H)-one (7). Conclusion Compounds 3 and 6 were initially isolated from the genus Penicillium and compound 4 was isolated from the Penicilliumchrysogenum for the first time. Compound 5 had affinity with VEGFR-1 and FGFR. The KD values were 7.78×10-3 and 1.44×10-1 μmol/L. |
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