红树林来源黑曲霉Aspergillus niger ZHN2-20次级代谢产物的研究

Studies on secondary metabolites from mangrove-derived fungus Aspergillus niger ZHN2-20

目的研究红树林植物榄李Lumnitzera racemosa根泥来源黑曲霉Aspergillus niger ZHN2-20的抗肿瘤活性次级代谢产物。方法利用硅胶柱层析、凝胶Sephadex LH-20柱层析、HPLC等常规化学手段对次级代谢产物进行了分离纯化;通过理化性质结合波谱学数据分析及文献对照,鉴定化合物的结构;分别以SRB和MTT法评价了化合物的细胞毒活性。结果从黑曲霉Aspergillus niger ZHN2-20的次级代谢产物中,分离鉴定了5个单体化合物,分别为：helvolic acid（1）,methyl helvolic acid（2）,（22E,24R）-ergosta-7,9（11）,22-triene-3β,5α,6β-triol（3）,cerevisterol（4）,（22E,24R）-ergosta-7,9（11）,22-triene-3β,5α-diol（5）。化合物3、5对HL-60和K-562肿瘤细胞株均表现出一定的细胞增殖抑制作用,抑制率分别为78.10%、60.50%、62.36%和49.43%。结论化合物1~3、5为首次在黑曲霉Aspergillus niger中分离得到,其中化合物2为新化合物。首次测定了化合物1~5对Hela、A-549、MGC-803、HL-60和K-562共5种肿瘤细胞株的细胞毒活性,其中化合物3、5对2株人白血病细胞显示出一定的抑制作用。

Objective To study the active secondary metabolites of AspergiLlus niger ZHN2-20, a fungus which was isolated from the mangrove sediment around the Lurnnitzera racernosa. Methods The isolation and purification of the compounds were performed by silica gel, Sephadex LH-20 and HPLC meth- ods, and their structures were determined by comparison their physicochemical characters and spectral data with literatures, and their cytotoxicities were evaluated by SRB and MTT methods respectively. Results Five compounds （1--5） were isolated from the AspergilLus niger ZHN2-20 and identified as helvolic acid （1）, methyl helvolic acid （2）, （22E, 24R）-ergosta-7, 9 （11）, 22-triene-313, 5a, 6-β-triol （3）, cerevisterol （4）, （22E, 24R）-ergosta-7, 9 （11）, 22-triene-313, 5α-diol （5）. Compounds 3 and 5 showed inhibitory activities against HL-60 and K-562 cells, with IR% values of 78. 10%, 60. 50% and 62.36~//00, 49.43~, respectively. Conclusion Compounds 1, 3 and 5 were isolated from this strain for the first time, and 2 was a new compound; the cytotoxicities of compounds 1-5 were evaluated against HeLa, A-549, MGC-803, HL-60, and K-562 cell lines for the first time, and compounds 3 and 5 exhib- ited potential inhibition against two human leukemia cell lines.