1种西沙群岛软珊瑚来源真菌中新天然产物pestalalactone的化学与生物活性研究  

Research on chemistry and biological activities of a new natural product pestalalactone from a soft coral-derived fungus collected from Xisha Islands

作　　者：张秀丽[1] 邢倩[1] 马洁[1,2] 王聪 郑纪勇[2] 邵长伦[1] 

机构地区：[1]中国海洋大学海洋药物教育部重点实验室医药学院,山东青岛266003 [2]中国船舶重工集团公司第七二五研究所海洋腐蚀与防护重点实验室,山东青岛266061

出　　处：《中国海洋药物》2016年第4期1-5,共5页Chinese Journal of Marine Drugs

基　　金：国家自然科学基金项目(41322037);国家海洋局海洋公益性行业科研专项(201405038);科技部973计划资助项目(2014CB643305)资助

摘　　要：目的从1株中国南海西沙群岛软珊瑚来源的真菌Pestalotiopsis sp.（ZJ-2009-7-6）中分离鉴定具有生物活性的3-苯基苯并呋喃酮化合物。方法运用多种色谱分离手段和现代波谱分析方法分离和鉴定化合物,最终得到了1个3-苯基苯并呋喃酮类新天然产物pestalalactone（1）,并通过核磁共振氢谱研究了该化合物在不同温度、不同溶剂条件下的优势构象变化;此外,还对化合物的抗藤壶幼虫Balanua amphitrite附着和抗细菌活性进行了评价。结果分离鉴定了1个新天然产物pestalalactone（1）,发现该化合物以2种不可拆分的阻转异构体的形式（1a/1b）并存。核磁共振氢谱研究结果表明,在氘代吡啶和氘代氯仿中以1a优势构象存在,在氘代甲醇、氘代丙酮和氘代二甲亚砜中的优势构象却是1b,而温度的变化（25～80℃）并不引起该化合物构象的变化。该化合物显示出强的抗藤壶幼虫B.amphitrite附着活性,其EC50值为2.30μg/mL;同时也显示出较强的抗细菌活性,特别是对金黄色葡萄球菌Staphylococcus aureus的最小抑制活性为0.45μg·mL-1。结论从1株西沙群岛软珊瑚来源真菌中发现了1个具有重要抗藤壶幼虫B.amphitrite附着和抗菌活性的新天然产物pestalalactone（1）,表明西沙群岛来源的海洋微生物具有重要的药用研究价值和应用开发前景。Objective To isolate and identify bioactive marine natural compounds 3-sustituted phthalides from the fungus Pestalotiopsis sp.（ZJ-2009-7-6）derived from the soft-coral Sarcophytonsp.collected from Xisha Islands.Methods pestalalactone（1）,one 3-phenyl phthalide,was obtained by a series of chromatographic methods and its structure was identified by modern spectroscopic analysis.The conformation changes of 1 were also studied under the different conditions of temperature and solvents.Additionally,the antifouling and antimicrobial activities of compound 1 were also evaluated.Results One new natural product,pestalalactone（1）,was obtained which existed as two inseparable atropisomers（1a/1b）.Interestingly,the study of 1 H NMR indicated that the conformation1 awas preferred in the deuterated solvents of pyridine and chloroform while the conformation 1bwas preferred in the deuterated solvents of methanol,acetone and dimethyl sulfoxide.However,the variation of temperature between 25℃and 80℃ did not change the preferred conformation of 1aand1 b.What＇s more,the compound not only showed strong activity against the larval settlement of barnacle Balanus amphitrite with an EC50 value of 2.30μg/mL but also exhibited strong antibacterial activity,especially for staphylococcus aureus with the MIC value of 0.45μg/mL.Conclusion One new natural compound,pestalalactone（1）with potent antifouling and antibacterial activities was obtained from a soft coral-derived fungus collected from Xisha Islands.This indicated that the marine microorganisms from Xisha Islands had important research values and application and development prospects in the field of medicinal drugs.

关 键 词：海洋天然产物 PESTALOTIOPSIS sp. 阻转异构体 防污损活性 抗菌活性 

分 类 号：R931[医药卫生—生药学]