红树林来源耐酸真菌Aspergillus fumigatus OUCMDZ-5210次生代谢产物的研究

Studies on secondary metabolite of aciduric fungus Aspergillus fumigatus OUCMDZ-5210 derived from Thailand mangrove

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(HPLC)等多种方法对耐酸真菌Aspergillus fumigatus OUCMDZ-5210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 OUCMDZ-5210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。

Objective To find secondary metabolites with structural specificity and significant cytotoxic activity,the secondary metabolites of the aciduric fungus Aspergillus fumigatus OUCMDZ-5210,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 OUCMDZ-5210 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 OUCMDZ-5210: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.