水母雪莲内生真菌Aspergillus sp.TPXq的次级代谢产物研究  

Secondary Metabolites from the Endophyte Fungus Aspergillus sp.Tpxq

作　　者：佟永春[1,2] 何蕾[2] 樊佳佳[2] 刘雅茹[1] 孙奕[2] 

机构地区：[1]中国医科大学公共基础学院,辽宁沈阳110001 [2]中国中医科学院中药研究所,北京100700

出　　处：《南京中医药大学学报》2016年第4期367-370,共4页Journal of Nanjing University of Traditional Chinese Medicine

基　　金：国家自然科学基金(81502968)

摘　　要：目的研究藏药水母雪莲内生真菌Aspergillus sp.TPXq的次级代谢产物。方法菌种采用震荡培养箱扩大培养,经反复硅胶柱色谱、Sephadex LH-20凝胶柱色谱、开放ODS柱色谱、高效液相色谱等方法进行分离纯化;并根据化合物的理化性质及波谱数据鉴定结构。结果从来自藏药水母雪莲的一株内生真菌Aspergillus sp.TPXq的培养液中分离得到8个环二肽和1个生物碱类化合物。分别鉴定为3-异丁基-吡咯并哌嗪-2,5-二酮（Ⅰ）、3-异戊基-吡咯并哌嗪-2,5-二酮（Ⅱ）、3-仲丁基-吡咯并哌嗪-2,5-二酮（Ⅲ）、3-苄基-吡咯并哌嗪-2,5-二酮（Ⅳ）、3-苄基-6-对羟基苄基-2,5二酮（Ⅴ）、3,6-二甲基哌嗪-2,5-二酮（Ⅵ）、3-异丁基-6-异丙基哌嗪-2,5-二酮（Ⅶ）、3-异丁基-6-苄基哌嗪-2,5-二酮（Ⅷ）、Chaetominine（Ⅸ）。结论其中化合物Ⅳ~Ⅷ为曲霉属Aspergillus.sp真菌中首次分离得到。细胞毒测试结果表明,以上化合物Ⅰ~Ⅷ对于A549和MCF-7肿瘤细胞均显示弱细胞毒活性（〉50μg/mL）,化合物Ⅸ对A549和MCF-7肿瘤细胞均具有显著的细胞毒活性,IC50值分别为0.18μg/mL和0.89μg/mL。OBJECTIVE To study the secondary metabolites of an endophytic fungus Aspergillus sp.TPXq isolated from Saussurea medusa.METHODS The strain was cultured in a large-scale by using the shaking incubator.The secondary metabolites were isolated by chromatography methods such as silica gel,Sephadex LH-20 columns,ODS flash column and HPLC,etc.The structures of these compounds were identified by their physico-chemical constants and the NMR data.RESULTS Eight Cyclodipeptides and one alkaloidwere seperated from secondary metabolites of an endophytic fungus Aspergillus sp.TPXq isolated were fromSaussurea medusa.,and their stuctures were identified as 3-isobutylpyrrolopiperazine-2,5-dione（Ⅰ）,3-isopropyl-pyrrolopiperazine-2,5-dione（Ⅱ）,3-seco-butyl-pyrrolopiperazine-2,5-dione（Ⅲ）,3-benzyl-pyrrolopiperazine-2,5-dione（Ⅳ）,3-benzyl-6-（p-hydroxy benzyl）piperazine-2,5-dione（Ⅴ）,3,6-dimethylpiperazine-2,5-dione（Ⅵ）,3-isobutyl-6-isopropylpiperazine-2,5-dione（Ⅶ）,3-isobutyl-6-benzylpiperazine-2,5-dione（Ⅷ）,Chaetominine（Ⅸ）,by analysis of physiochemical and NMR data.CONCLUSION Among them,compounds Ⅳ ~ Ⅷ were isolated from Alterraria.sp for the first time.CompoundsⅨ showed significant cytotoxic activity against A549 and MCF-7tumor cells,the IC50 values are 0.18μg/mL and 0.89μg/mL,respectively.However,compoundsⅠ~Ⅷ exhibited very weak cytotoxicity（〉50μg/mL）against these cell lines.

关 键 词：内生真菌 曲霉属 次级代谢产物 环二肽 生物碱 

分 类 号：R284.1[医药卫生—中药学]