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目的探究来源于西沙群岛的珊瑚真菌Aspergillus sp.OUCMDZ-3658的活性天然产物。方法利用柱色谱及高效液相色谱等手段对发酵产物进行分离、纯化,运用质谱、核磁共振、圆二色谱和比旋光等方法鉴定化合物的结构,采用MTT法、药敏纸片法和α-糖苷酶抑制评价化合物的生物活性。结果从珊瑚真菌OUCMDZ-3658的发酵产物中分离获得了13个生物碱(1-13)和1个fusidane型三萜(14),其结构依次鉴定为fumiquinazolines A(1)和C(2)、fumiquinazolines D(3)和F(4)、chaetominine(5)、pseurotins A1(6)和A2(7)、fumitremorgin C(8)、cyclouyprostatin A(9)、12β-hydroxy-13α-methoxyverruculogen TR-2(10)、9 H-pyrido[3,4-b]indole-3-carboxylic acid(11)、(–)-cyclopenol(12)、pyripyropene A(13)以及烟曲霉酸helvolic acid(14)。化合物8和9对产气杆菌、化合物10对白色念珠菌有弱抑制活性,MIC值分别为33.0、30.4和56.4μmol/L;化合物3和4对α-糖苷酶有抑制作用,活性与阳性药阿卡波糖相当,IC50值分别为0.87、1.14和1.11mmol/L。结论本文首次报道了fumiquinazolines D(3)和F(4)的α-糖苷酶抑制活性,为α-糖苷酶抑制剂的发现提供了新的结构类型。
Objective To investigate the active natural product of Aspergillus sp. OUCMDZ-3658 from Xisha Islands. Methods The compounds were isolated and purified by column chromatography and high performance liquid chromatography (HPLC). The structures of the compounds were identified by mass spectrometry, nuclear magnetic resonance, circular dichroism and specific rotation. MTT assay, Glycosidase inhibition evaluates the biological activity of the compound. Results Thirteen alkaloids (1-13) and one fusidane type triterpene (14) were isolated from the fermentation product of coral fungus OUCMDZ-3658 and their structures were identified as fumiquinazolines A (1) and C (2) fumiquinazolines D (3) and F (4), chaetominine (5), pseurotins A1 (6) and A2 (7), fumitremorgin C (8), cyclouyprostatin A (9), 12β-hydroxy-13α-methoxyverruculogen TR- 10), 9 H-pyrido [3,4-b] indole-3-carboxylic acid (11), (-) - cyclopenol (12), pyripyropene A (13) and fulguric acid (14). Compounds 8 and 9 had weak inhibitory activity on A. albicans against Aerobacter aerogenes and Compound 10, with MICs of 33.0, 30.4 and 56.4 μmol / L, respectively. Compounds 3 and 4 had inhibitory effects on α-glucosidase, and activity and positive drug Acarbose equivalent, IC50 values were 0.87,1.14 and 1.11mmol / L. Conclusions This paper reports for the first time the α-glucosidase inhibitory activity of fumiquinazolines D (3) and F (4) and provides a new structural class for the discovery of α-glucosidase inhibitors.