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目的研究土茯苓内生芒果球座菌Guignardia mangiferae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、凝胶柱和制备薄层色谱等色谱技术进行分离纯化,通过现代波谱技术进行结构鉴定;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SRB法对化合物进行体外抗肿瘤活性研究。结果从土茯苓内生芒果球座菌的100 L液体发酵提取物中分离得到12个化合物,经波谱数据分析鉴定其中10个化合物,分别为15-hydroxyl tricycloalternarene 5b(1)、guignardiaene D(2)、guignardiaene C(3)、guignardone A(4)、guignardone B(5)、3-(4-甲苯氧基)-丙酸(6)、2,4-壬二醇(7)、麦角甾酮(8)、酪醇(9)、对羟基苯甲醛(10)。杂合萜类化合物1~5对SF-268细胞具有选择性的抑制作用,化合物6、7对MCF-7细胞具有选择性的抑制作用。结论化合物6~10均为首次从该属真菌中得到,其中化合物6、7为新的天然产物。
Objective To study the secondary metabolites of Guignardia mangiferae and their anti-tumor activities. Methods Silica gel column, reversed-phase silica gel column, gel column and preparative TLC were used for separation and purification. Structural identification was carried out by modern spectroscopic techniques. The glioma cell line SF-268, breast cancer cell line MCF-7, The large cell lung cancer cell NCI-H460 was used as the test cell line, and the anti-tumor activity of the compound was studied by SRB method in vitro. Results Twelve compounds were isolated from 100 L liquid fermentations of endophytic M. tumefaciens endophytic bacteria. Ten compounds were identified by spectral data analysis and identified as 15-hydroxyl tricycloalternarene 5b (1), guignardiaene D (2) , Guignardiaene C (3), guignardone A (4), guignardone B (5), 3- (4-toluoxy) 8), tyrosol (9), p-hydroxybenzaldehyde (10). Heterozygote terpenoids 1 to 5 showed selective inhibitory effects on SF-268 cells, while compounds 6 and 7 showed selective inhibitory effects on MCF-7 cells. Conclusions Compounds 6 to 10 are all obtained from the fungi for the first time, of which compounds 6 and 7 are new natural products.