海洋真菌Aspergillus niger XJJ-3中萘并吡喃酮类化合物结构及生物活性  

Structures and activities of naphthopyrones from marine fungus Aspergillus niger XJJ-3

作　　者：姜薇[1,2] 蒋航成 韦歆 徐家俊 单体壮 潘英 JIANG Wei;JIANG Hang-Cheng;WEI Xin;XU Jia-Jun;SHAN Ti-Zhuang;PAN Ying(School of Environmental Science and Engineering,Yangzhou University,Yangzhou,Jiangsu 22512 7,China;Jiangsu Cancer Hospital,Jiangsu Institute of Cancer Research,The Affiliated Cancer Hospital of Nanjing Medical University,Nanjing,Jiangsu 210009,China;School of Pharmacy,Wenzhou Medical University,Wenzhou,Zhejiang 325035,China)

机构地区：[1]扬州大学环境科学与工程学院,江苏扬州225127 [2]温州医科大学药学院,浙江温州325035 [3]江苏省肿瘤医院江苏省肿瘤防治研究所南京医科大学附属肿瘤医院,江苏南京210009

出　　处：《微生物学通报》2018年第9期1897-1903,共7页Microbiology China

基　　金：江苏省高校自然科学基金(15KJB170020);浙江省药学重中之重一级学科开放基金(201707);扬州大学培育基金(2017CXJ050)

摘　　要：【背景】萘并吡喃酮类化合物生物活性多样,是真菌Aspergillusniger中特征次生代谢产物。【目的】研究分离自海洋滩涂土壤的真菌Aspergillus niger XJJ-3中萘并吡喃酮类化合物结构及其抗菌和卤虫致死活性。【方法】以TLC分析为导向,综合运用多种色谱和光谱方法分离和鉴定萘并吡喃酮类化合物。采用微量稀释法测试化合物的抗菌和卤虫致死活性。【结果】从真菌A.niger大米发酵产物中共分离得到6个萘并吡喃酮类化合物,鉴定为RubrofusarinB(1)、Flavasperone (2)、Aurasperone A (3)、Asperpyrones C (4)、Asperpyrones B (5)和Fonsecinone A (6)。抗菌活性实验结果表明,化合物1-6对致病菌S. aureus ATCC33591、29213、E. faecium ATCC35667和V.parahemolyticus表现出不同程度的抑制活性,其中化合物2和4对S.aureus ATCC33591表现出较强抑制活性(MIC分别为43.7μmol/L和21.9μmol/L),化合物3对E.faecium ATCC35667抑制活性较强(MIC为21.9μmol/L)。卤虫致死活性实验结果表明,化合物1-6均表现出一定的卤虫致死活性,其中化合物2和3活性显著(LD50分别为35.0μmol/L和8.8μmol/L)。【结论】菌株XJJ-3可产生结构丰富的萘并吡喃酮类化合物,化合物1-6存在不同程度的抗菌和卤虫致死活性,该研究可为抗菌和细胞毒类药物的研发提供参考。[Background] Naphthopyrones possess various bioactivities that are characteristic secondary metabolites of the fungus Aspergillus niger. [Objective] To illuminate the structures and activities ofnaphthopyrones from fungus A. niger isolated from mud flat. [Methods] Guided by TLC analysis, we used combined chromatographic and spectrographic techniques to identify naphthopyrones. The activities against pathogen bacteria and Artemia salina were tested by micro-dilution method. [Results] Six naphthopyrones： Rubrofusarin B （1）, Flavasperone （2）, Aurasperone A （3）, Asperpyrones C （4）, Asperpyrones B （5） and Fonsecinone A （6） were isolated from A. niger. In bioassays, compounds 1 through 6 showed different levels of antibacterial activities against pathogen bacteria. Flavasperone （2） and Asperpyrones C （4） showed potent antibacterial activities against S. aureus ATCC33591 with MIC values 43.7 and 21.9 μmol/L, respectively. Aurasperone A （3） exhibited significant activities against E. faecium ATCC35667 with MIC values 21.9 μmol/L. Compounds 1 through 6 displayed toxicity on brine shrimps larvae, the LD50 values of Flavasperone （2） and Aurasperone A （3） were 35.0 and 8.8 pmol/L, respectively. [Conclusion] Diverse naphthopyrones were produced by strain XJJ-3. Compounds 1 through 6 showed different levels of activities against pathogen bacteria and Artemia salina. This study may provide reference for the development of antibacterial and cytotoxic drugs.

关 键 词：海洋真菌 黑曲霉 萘并吡喃酮 抗菌活性 卤虫致死活性 

分 类 号：Q936[生物学—微生物学]