文章摘要
珊瑚真菌Aspergillus sp. OUCMDZ-3658产生的生物碱
Alkaloids from Aspergillus sp. OUCMDZ-3658 associated with soft coral
投稿时间:2015-04-17  修订日期:2015-04-29
DOI:
中文关键词: 珊瑚真菌,活性产物,生物碱,α-糖苷酶抑制
英文关键词: coral fungi  bioactive natural products  alkaloids  α-glucosidase inhibition
基金项目:国家高技术研究发展计划(863计划);国家自然科学基金项目(面上项目,重点项目,重大项目)
作者单位E-mail
朱伟明 中国海洋大学医药学院 weimingzhu@ouc.edu.cn 
王文玲 中国海洋大学医药学院  
王立平 贵州省、中国科学院天然产物化学重点实验室  
王聪 中国海洋大学医药学院  
刘海珊 中国海洋大学医药学院  
郝杰杰 中国海洋大学医药学院  
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中文摘要:
      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)、9H-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56.4 μmol/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 1.11 mmol/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。
英文摘要:
      Objective To identify the active secondary metabolites of the coral fungus Aspergillus sp. OUCMDZ-3658 from XiSha Islands. Methods The isolations and purifications of compounds were performed by means of solvent extraction, column chromatography over silica gel, Sephadex LH-20 and HPLC. And their structures were elucidated through the analysis of MS, NMR, [α]D and CD. The bioactivities were assayed by MTT, paper diffusion and the α-glucosidase inhibition methods. Results From the cultures of Aspergillus sp. OUCMDZ-3658, we isolated thirteen alkaloids (1-13) and a fusidane-type triterpenoid (14). 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-2 (10), 9H-pyrido[3,4-b]indole-3-carboxylic acid (11), (–)-cyclopenol (12), pyripyropene A (13) and helvolic acid (14), respectively. Compounds 8 and 9 showed weak antibacterial activity against Enterobacter aerogenes while compound 10 showed weak antifungal activity against Candida albican with MIC values of 33.0, 30.4 and 56.4 μmol/L, respectively. Compounds 3 and 4 displayed comparable α-glucosidase inhibition to acarbose (positive control) with the IC50 values of 0.87, 1.14 and 1.11 mmol/L, respectively. Conclusion This paper reported the α-glucosidase inhibition of fumiquinazolines D (3) and F (4) for the first time and thus afforded the new structure-type for screening of α-glucosidase inhibitors.
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