| 牟晓凤,边文涛,刘敏,等.一株海兔来源真菌 Aspergillus terreus丁内酯类化合物及其生物活性研究[J].中国海洋药物,2014,33(5):16-22. |
| 一株海兔来源真菌 Aspergillus terreus丁内酯类化合物及其生物活性研究 |
| Butyrolactones Isolated from a Sea Hare-derived Fungus Aspergillus terreus and their Biological Activities |
| 投稿时间：2014-05-04 修订日期：2014-05-14 |
| DOI： |
| 中文关键词: 海兔来源真菌 Aspergillus terreus 丁内酯 抗菌活性 |
| English Keywords:sea hare-derived fungus Aspergillus terreus butyrolactones antimicrobial activity |
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| 中文摘要: |
| 摘要：目的 在生物活性和化学方法指导下，从1株海兔来源真菌 Aspergillus terreus (RA29-5)中分离鉴定海洋天然产物，并对其进行生物活性评价。方法 运用硅胶柱层析、Sephadex LH-20凝胶柱层析和HPLC等方法分离纯化化合物，利用NMR等现代波谱分析方法，对化合物进行结构鉴定，并对化合物进行抗菌、卤虫致死和斑马鱼胚胎毒性活性评价。结果 鉴定了 9 个丁内酯类化合物 (1～9) 的结构；抗菌活性表明，除化合物 6 和 9 外，所有化合物对四株致病细菌白色葡萄球菌 Staphylococcus epidermidis、金黄色葡萄球菌 Staphylococcus aureus、蜡状芽孢杆菌 Bacillus subtilis 和四联球菌 Tetragenococcus halophilus 都显示一定的抗菌活性；化合物 1～4 和7均对真菌芒果叶枯菌 Pestalotia mangiferae 显示抗菌活性；特别的，化合物 7 对测试的13株致病菌都具有广谱地抗菌活性，其MIC值在1.11~8.88 μmol/L之间；此外，还对化合物的抗菌活性构效关系进行了初步探讨。结论 海兔来源真菌 A. terreus (RA29-5) 可产生结构多样的丁内酯类化合物，该类化合物具有开发成抗菌剂的潜力。 |
| English Summary: |
| Abstract: Objective To isolate and identify the marine natural compounds from a sea hare-derived fungus Aspergillus terreus (RA29-5) under the guidance of bioactivity and chemical methods, and evaluate their biological activities. Methods The pure compounds were isolated by Silica gel column chromatography, Sephadex LH-20 gel and HPLC, their structures were determined by modern spectroscopic methods, especially NMR method, the biological activities including antimicrobial activity, lethal activity of brine shrimp,and toxic activity on zebra fish embryo, were also evaluated. Results The structures of nine butyrolactones (1～9) were identified by structural analysis. The antimicrobial results indicated that all the compounds except 6 and 9 exhibited antimicrobial activity against Staphylococcus epidermidis, S. aureus, Bacillus subtilis and Tetragenococcus halophilus. Compounds 1~4 and 7 showed inhibitory activity against Pestalotia mangiferae. Especially, 7 showed strong antimicrobial activity with broad-spectrum against 13 pathogenic microorganisms with the range of MIC values of 1.11~8.88 μmol/L. Furthermore, the preliminary structure-activity relationship was also discussed. Conclusion A series of butyrolactones were isolated from sea hare-derived fungus A. terreus (RA29-5) with structural diversity, showed antimicrobial activities with the potential to be developed into antimicrobial agents. |
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