目的研究南海海洋真菌帚状弯孢聚壳Eutypella scoparia的次级代谢产物及其抗肿瘤活性。方法采用硅胶柱、反相硅胶柱、凝胶柱和薄层制备等色谱技术和重结晶进行分离纯化,通过波谱分析进行结构鉴定以神经胶质瘤细胞SF-268、乳腺癌细胞MCF-7、大细胞肺癌细胞NCI-H460为供试细胞株,采用MTT法对化合物进行体外抗肿瘤活性研究。结果从发酵物中分离并鉴定了10个化合物,其中6个为海松烷型二萜,分别为isopimara-8(14),15-diene(1)、libertellenone A(2)、scopararane B(3)、diaporthein A(4)、diaporthein B(5)、11-deoxydiaporthein A(6)4个为麦角甾醇类化合物,分别为麦角甾酮(7)、麦角甾醇(8)、过氧化麦角甾醇(9)、啤酒甾醇(10),其中化合物5对3种肿瘤细胞株的IC50分别为9.2、4.4、9.9μmol/L。结论化合物1、2和6～10均为首次从该属真菌中分离得到,化合物5具有显著的细胞毒活性。

Objective To study the secondary metabolites of the marine fungus Eutypella scoparia from the South China Sea and their antitumor activities.Methods The compounds were isolated by various chromatographic methods(silica gel,reverse silica gel,Sephadex-LH20,preparative TLC,and so on) and recrystallization.Their structures were identified by extensive analysis of their spectroscopic data.The inhibitory effects of these compounds on SF-268,MCF-7,and NCI-H460 cell lines were observed in vitro by MTT method.Results Ten compounds(six pimarane diterpenes and four steroids) were isolated from the culture and identified as isopimara-8(14),15-diene(1),libertellenone A(2),scopararane B(3),diaporthein A(4),diaporthein B(5),11-deoxydiaporthein A(6),(22E,24R)-ergosta-4,6,8(14)-22-tetraen-3-one(7),ergosterol(8),ergosterol peroxide(9),and cerevisterol(10).Compound 5 has the notable cytotoxic activities on SF-268,MCF-7,and NCI-H460 cell growth with IC50 values of 9.2,4.4,and 9.9 μmol/L,respectively.Conclusion Compounds 1,2,and 6—10 are isolated from the fungi of Eutypella(Nits.) Sacc.for the first time and compound 5 demonstrates the significant inhibition on above three cell lines.

中国科学院知识创新工程重要方向项目(KSCX2-YW-G-073,KSCX2-EW-G-12B);广东省科技计划项目(2010B030600010);广东省科学院优秀青年科技人才基金