奇楠内生真菌Fusarium sp.HP-2次生代谢产物研究

Studies on the secondary metabolites from the endophytic fungus Fusarium sp.HP-2 of “Qi-Nan” eaglewood

目的研究奇楠内生真菌Fusariumsp．HP-2次生代谢产物及其生物活性。方法采用多种柱色谱技术对菌株发酵产物进行分离纯化；通过化合物的理化常数和波谱数据分析鉴定化合物的结构；分别采用滤纸片琼脂扩散法、MTT法和Elman比色法，对化合物的体外抗菌活性、细胞毒活性及乙酰胆碱酯酶抑制活性进行测试。结果从奇楠内生真菌Fusariumsp．HP-2发酵产物中分离鉴定了8个化合物，分别为：对羟基苯乙醇（1）、2-羟基．3．对羟基苯基丙酸甲酯（2）、N-（2．苯乙基）乙酰胺（3）、5α，8α-表二氧-（20S，22E，24R）-麦角甾-6，22-二烯-3β-醇（4）、千层塔烯二醇（5）、fusamaphthoquinoneA（6）、（＋）-solaninol（7）和2，3-dihydro-5-hydroxy-8-methoxy-2，4-Dimethylnaphtho[1，2-b]furan-6，9-dione（8）。化合物4和8对人慢性髓原白血病细胞株K-562和人肝癌细胞株BEL-7402有抑制作用，化合物6～8有乙酰胆碱酯酶抑制活性，化合物7和8具有抗青枯雷尔菌（Ralstonia solanacearum）的活性。结论奇楠内生真菌Fusariumsp．HP-2能代谢产生具有多种生物活性的化合物；首次报道萘醌类化合物6和7的乙酰胆碱酯酶抑制活性，以及化合物7与8的抗植物病原菌活性。

Objective To study the bioactive constituents from the endophytic fungus Fusarium sp. HP-2 of ＂Qi-Nan＂ eaglewood. Methods The compounds were isolated and purified by various column chromatographic techniques, and their structures were identified through a combined analysis of physicochemical properties and spectroscopic evidence. The antimicrobial and cytotoxicity activities in vitro of the compounds were evaluated by paper disc diffusion method and MTT method, respectively. Moreover, the compounds were also tested for inhibitory activity against acetylcholinesterase using the Ellman colorinetric method. Results Eight compounds were isolated from the endophytic fungus Fusarium sp. HP-2 of ＂Qi-Nan＂ eaglewood, and their structures were determined as 4-（2-hydroxyethyl）phenol （1）, methyl-2-hydroxy-3-（4-hydroxyhenyl）propanoate （2）, N-（2-phenylethyl） acetamide （3）, 5α, 8α- epidioxy-（20S,22E,24R）-ergosta-6,22-dien-3β-ol （4）, serratenediol （5）, fusarnaphthoquinone A （6）, （＋）-solaninol （7） and 2,3-dihydro-5-hydroxy-8-methoxy-2, 4-dimethylnaphtho[1,2-b]furan-6, 9-dione （8）. Compound 4 and 8 exhibited cytotoxic activities in vitro against K-562 and BEL-7402 tumor cell line. Compound 6-8 showed the inhibitory activities against acetylcholinesterase, in addition, comound 7 and 8 revealed inhibitory effect against Ralstonia solanacearum. Conclusion The endophytic fungus Fusarium sp. HP-2 of ＂Qi-Nan＂ eaglewood could produce the compounds with many biological activities. Furthermore, the inhibitory activities against acetylcholinesterase of naphthoquinone compounds 6 and 7 were reported for the first time as well as the inhibitory activities against plant-pathogenic bacteria of naphthoquinone compounds 7 and 8.