红树林来源耐酸真菌Aspergillus fumigatus OUCMDZ5210次生代谢产物的研究

目的 对源自泰国红树林底泥中的耐酸真菌Aspergillus fumigatus OUCMDZ 5210的次生代谢产物进行化学成分和生物活性的研究。方法 综合利用硅胶柱色谱、凝胶柱色谱和半制备高效液相色谱等多种方法对耐酸真菌Aspergillus fumigatus OUCMDZ5210的次生代谢产物进行分离；采用核磁共振谱（NMR）、质谱（MS）、紫外光谱（UV）等现代波谱学技术对分离得到的化合物进行结构鉴定；以人慢性髓性白血病细胞K562及人结肠癌细胞HCT116两株肿瘤细胞为研究模型，采用MTT法和CCK-8法对所分离的化合物进行细胞毒活性评价。结果 从耐酸真菌Aspergillus fumigatus OUCMDZ5210的次级代谢产物中分离得到6个吲哚二酮哌嗪类生物碱：tryprostatins B(1)，fumitremorgin C(2)，spirotryprostatin A(3), spirotryprostatin.B(4), 6-methoxyspirotryprostatin B (5), 8,9-dihydroxyspirotrypr-ostatin A(6)以及1个酰胺类化合物cephalimysin B(7)。结论 生物活性初步评价结果显示，化合物3和6对人结肠癌细胞HCT116以及人慢性髓性白血病细胞K562具有不同程度的抑制活性。

Studies on secondary metabolite of aciduric fungus Aspergillus fumigatus OUCMDZ5210 derived from Thai mangrove

Objective In order to find secondary metabolites with structural specificity and significant cytotoxic activity, the secondary metabolites of the aciduric fungus Aspergillus fumigatus OUCMDZ5210, an aciduric fungus derived from Thai mangrove sediment and their bioactivities were investigated. Methods Using Silica gel column chromatography, Sephadex LH-20 and HPLC, the secondary metabolites of Aspergillus fumigatus OUCMDZ5210 were isolated. The structures of those compounds were identified by several modern spectroscopy techniques including NMR, MS, UV. The cytotoxicities of those compounds against two cancer cell lines K562 and HCT-116 were evaluated by MTT and CCK-8 methods. Results Seven compounds were isolated from the secondary metabolites of Aspergillus fumigatus OUCMDZ5210: tryprostatinsB(1), fumitremorginC(2), spirotryprostatinA(3), spirotryprostatinB(4), 6-methoxyspirotryprostatinB(5), 8,9-dihydroxyspirotryprostatinA(6), cep-halimysin B(7). Conclusion Preliminary evaluation of biological activity showed that compounds 3 and 6 had different degrees of inhibitory activities against human colon cancer cell HCT116 and human chronic myelogenous leukemia cell K562.