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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 3-phenylbenzofuranones from a fungus Pestalotiopsis sp. (ZJ-2009-7-6) from the soft coral of the Xisha Islands, South China Sea. Methods A new 3-phenylbenzofuranones new natural product, pestalalactone (1), was isolated and identified by a variety of chromatographic methods and modern spectroscopic methods. The compounds were characterized by 1H-NMR Different conformational changes under different solvent and solvent conditions; in addition, the compound anti-barnacle larvae Balanua amphitrite adhesion and antibacterial activity were evaluated. Results A new natural product, pestalalactone (1), was isolated and identified. The compound was found to coexist in the form of two insensitive anomers (1a / 1b). The results of 1H NMR showed that the dominant conformation existed in deuterated pyridine and deuterated chloroform as 1a, and the dominant conformation in deuterated methanol, deuterated acetone and deuterated dimethyl sulfoxide was 1b, while the change in temperature (25-80 ° C) does not cause a change in the conformation of the compound. The compound showed strong anti-barnacle larvae B.amphitrite attachment activity with an EC50 value of 2.30 μg / mL; at the same time, the compound also showed strong antibacterial activity, in particular, minimal inhibitory activity against Staphylococcus aureus 0.45 μg · mL-1. Conclusions A new natural product, pestalalactone (1), with important anti-barnacle larvae attachment and antibacterial activities, was found from one soft-source fungus in the Xisha Islands, indicating that the marine microorganisms from Xisha Islands have important medicinal properties Value and application development prospects.