| 彭书海,卢余盛,姚光山.海洋真菌Cochliobolus lunatus中环十酯肽化合物 cyclopeptolide 1的发现及其抗真菌活性研究[J].中国海洋药物,2020,39(3):21-25. |
| 海洋真菌Cochliobolus lunatus中环十酯肽化合物 cyclopeptolide 1的发现及其抗真菌活性研究 |
| Discovery and antifungal study of cyclopeptolide 1 from marine-derived fungus Cochliobolus lunatus |
| 投稿时间：2019-11-27 修订日期：2020-01-09 |
| DOI： |
| 中文关键词: Cochliobolus lunatus，环酯肽，抗真菌活性，白色念球菌 |
| English Keywords:Cochliobolus lunatus, lipopeptide, anti-fungi,Candida albicans |
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| 中文摘要: |
| 目的 利用一个菌株-多个化合物（OSMAC）方法研究海洋来源真菌Cochliobolus lunatus的次生代谢产物及其抗真菌活性。方法 利用氮源丰富的GPY培养基诱导海洋来源真菌Cochliobolus lunatus产生新的酯肽类化合物，采用正相硅胶柱层析、凝胶柱层析、半制备高效液相色谱（HPLC）等方法对化合物进行分离纯化，利用核磁共振波谱学（NMR）和X-Ray单晶衍射手段并参考文献对化合物进行结构表征，利用各种活性模型对其进行系统的生物学活性评价。结果 从海洋来源真菌分离获得环十酯肽化合物cyclopeptolide 1，并报道其晶体结构，发现其具有抗真菌活性（MIC=16 μg/mL），并与临床药物氟胞嘧啶在抗真菌实验中显示协同效应。结论 cyclopeptolide 1在抗真菌药物研发领域有望成为重要的先导化合物。 |
| English Summary: |
| Objective To investigate the secondary metabolites and their bioactivities of marine-derived filamentous fungus Cochliobolus lunatus by using the OSMAC method. Methods Nitrogen-rich GPY media was used to stimulate the fungus to produce novel lipopeptides in Cochliobolus lunatus. Combing forward column chromatography, Sephadex gel column chromatography and semi-prepared HPLC to isolate novel lipopeptides, its structure was elucidated by using NMR and X-ray crystal diffraction and compared with previously reported data. The various bioactivities were evaluated by using corresponding models. Results The compound cyclopeptolide 1 was isolated and its monocrystalline was first reported. It showed potent antifungal activities with MIC value of 16 μg/mL, and had synergistic activity with flucytosine. Conclusion Cyclopeptolide 1 is a promising compound for the development of antifungal drugs. |
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