土茯苓内生芒果球座菌的次级代谢产物及其抗肿瘤活性研究

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。

Secondary metabolites of endophytic Guignardia mangiferae from Smilax glabra and their antitumor activities

Objective To study the secondary metabolites of the endophytic fungus Guignardia mangiferae from Smilax glabra and their antitumor activities.Methods The compounds were isolated by various column chromatographies on silica gel,reversed silica gel,Sephadex LH-20,preparative TLC,and so on.Their structures were identified by extensive analysis of their spectroscopic data.The inhibitory effects of compounds 1—7 on SF-268,MCF-7,and NCI-H460 cell lines were tested in vitro by SRB method.Results Twelve compounds were isolated from the extract of 100 L liquid fermentation broth and ten of them were identified as 15-hydroxyl tricycloalternarene 5b(1),guignardiaene D(2),guignardiaene C(3),guignardone A(4),guignardone B(5),3-(4-methylphenoxy)propanoic acid(6),nonane-2,4-diol(7),ergosterol keone(8),tyrosol(9),and p-hydroxybenzaldehyde(10).The meroterpenes 1—5 showed inhibitory effects on SF-268,while compounds 6 and 7 showed inhibitory effects on MCF-7 selectively.Conclusion Compounds 6—10 are isolated from fungus of the genus Guignardia Viala et Ravaz for the first time and compounds 6 and 7 are firstly reported as natural products.