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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 Eutypella scoparia and its anti-tumor activity in the South China Sea. Methods Silica gel column, reversed-phase silica gel column, gel column and thin-layer preparative iso-chromatographic techniques were used for the separation and purification by recrystallization and structural elucidation by spectroscopic analysis. The effects of glioma cells SF-268, breast cancer cells MCF-7 , Large cell lung cancer cell NCI-H460 as the test cell line, using MTT method compounds in vitro antitumor activity. Results Ten compounds were isolated and identified from the fermentations. Six of them were isopimara-8 (14), 15-diene (1), libertellenone A (2) and scopararane B , Diaporthein A (4), diaporthein B (5) and 11-deoxydiaporthein A (6). Four ergosterol compounds were ergosterol (7), ergosterol (8), ergosterol ) And beer sterol (10). The IC50 of compound 5 against three tumor cell lines was 9.2, 4.4 and 9μmol / L, respectively. Conclusion Compounds 1, 2 and 6 ~ 10 were isolated from the genus Fungus for the first time. Compound 5 showed significant cytotoxic activity.