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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4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1.11~8.88μmol/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。
OBJECTIVE To isolate and identify marine natural products from Aspergillus terreus (RA29-5), a fungus originated from sea urchin, under the guidance of bioactivity and chemical methods, and evaluate its biological activity. Methods The compounds were isolated and purified by silica gel column chromatography, Sephadex LH-20 column chromatography and HPLC. The structures of the compounds were identified by using modern spectral analysis methods such as NMR. The compounds were also tested for antibacterial activity, brine shrimp killing and zebrafish Evaluation of embryotoxicity. Results The structures of nine butyrolactone compounds (1 ~ 9) were identified. The antibacterial activity of all the compounds against four pathogenic bacteria, Staphylococcus epidermidis, Staphylococcus aureus, Both Bacillus subtilis and Tetragenococcus halophilus showed some antibacterial activity. Compounds 1 to 4 and 7 showed antibacterial activity against the fungal strain Pestalotia mangiferae. In particular, compound 7 tested 13 strains of the disease The antibacterial activity of the compounds was broad-spectrum. The MIC values ranged from 1.11 to 8.88 μmol / L. In addition, the structure-activity relationship of the compounds was also discussed. Conclusion A. terreus (RA29-5), a fungus derived from sea-rabbit, can produce a variety of butyrolactone compounds with the potential to develop into antibacterial agents.