海洋来源青霉菌Penicillium polonicum H92次级代谢产物的研究  

Studies on marine secondary metabolites of fungus Penicillium polonicum H92

作　　者：刘碧丽 丘鹰昆[2] 颜志文 吴小枫 邱彦[3] 杨嘉永 LIU Bi-li;QIU Ying-kun;YAN Zhi-wen;WU Xiao-feng;QIU Yan;YANG Jia-yong(Department of Pharmacy,The First Affiliated Hospital of Xiamen University,Xiamen 361003,China;School of Pharmaceutical Sciences,Xiamen University,Xiamen 361102,China;School of Medicine,Xiamen University,Xiamen 361102,China)

机构地区：[1]厦门大学附属厦门市第一医院药剂科,福建厦门361003 [2]厦门大学药学院,福建厦门361102 [3]厦门大学医学院,福建厦门361102

出　　处：《中国海洋药物》2021年第4期27-32,共6页Chinese Journal of Marine Drugs

基　　金：白求恩医学科学研究基金(TY110DS);厦门大学中央高校基本业务费(20720200015)资助。

摘　　要：目的对源自福建漳江口红树林底部海水沉积物的青霉菌Penicillium polonicum H92的次级代谢产物进行化学成分和生物活性研究。方法综合利用有机溶剂萃取、硅胶柱色谱、反相硅胶(ODS)柱色谱、凝胶(Sephadex LH-20)柱色谱、薄层色谱、半制备高效液相色谱等多种手段对青霉菌Penicillium polonicum H92的次生代谢产物进行分离纯化;采用质谱(MS)、核磁共振谱(NMR)、紫外光谱(UV)等现代波谱技术鉴定所分离的化学成分结构;以奥司他韦为阳性对照药物,对上述化合物进行抗流感病毒神经氨酸酶(NA)活性测试。结果从青霉菌Penicillium polonicum H92中分离得到7个次生代谢产物,其中4个喹啉酮类化合物:纯绿青霉素(1),3-甲氧基纯绿青霉素(2),纯绿青霉素醇(3),喹诺酮(4);2个二酮哌嗪类化合物:环(色-苯丙)二肽(5),Fructigenine A(6);1个生物碱:橙黄胡椒酰胺C(7)。结论生物活性初步评价结果显示,化合物2和6对流感病毒神经氨酸酶具有不同程度的抑制活性。Objective To study the chemical composition and biological activity of secondary metabolites of Penicillium polonicum H92 from seawater sediments at the bottom of mangroves in Zhangjiang Estuary, Fujian. Methods Silica gel column chromatography, reversed-phase silica gel(ODS) column chromatography, gel(Sephadex LH-20) column chromatography, thin-layer chromatography, and semi-preparative highperformance liquid chromatography were used to analyze the organic solvent extraction of Penicillium polonicum H92, and the secondary metabolites were isolated and purified. Mass spectrometry(MS), nuclear magnetic resonance(NMR), ultraviolet spectroscopy(UV) and other modern spectroscopy techniques were used to identify the structure of the separated chemical constituents. Oseltamivir was used as a positive control drug to conduct neuraminidase(NA) activity test against influenza virus with the above compounds. Results Seven secondary metabolites were isolated from Penicillium polonicum H92, and four of which were identified as quinolinone compounds as Viridicatin(1), 3-O-Methylviridicatin(2), and Viridicatol(3), 3-Hydroxy-4-(3-methoxyphenyl)-2-quinolinone(4). Compound 5 and 6 were diketopiperazines as Cyclic(L-Phe-L-Trp)(5), and Fructigenine A(6). Compoundone 7 was elucidated as an alkaloid of Aurantiomide C. Conclusion The preliminary evaluation of biological activity showed that compounds 2 and 6 had different levels of inhibitory activity against influenza virus neuraminidase.

关 键 词：青霉菌Penicillium polonicum 次生代谢产物 结构鉴定 抗流感病毒 

分 类 号：R931.77[医药卫生—生药学]