海洋真菌Aspergillus sp.HH-3中1个新的抗肿瘤硫代二酮哌嗪类化合物

A new antitumor thiodiketopiperazine from the marine-derived fungus Aspergillus sp.HH-3

目的 研究海泥真菌Aspergillus sp. HH-3的次级代谢产物及其抗肿瘤活性。方法 使用硅胶色谱柱、LH-20凝胶色谱等对代谢粗提物进行分离纯化;运用核磁共振(NMR)、质谱(MS)等方法并结合文献报道数据确定化合物的结构;采用CCK-8法评价化合物对3种肿瘤细胞A549、HepG2、He La的抑制活性。结果从Aspergillus sp. HH-3中分离获得6个化合物,包括1个新的硫代二酮哌嗪类化合物aspersin(1)与5个已知化合物dehydroxymethylbis(dethio)bis(methylthio)gliotoxin(2)、trypacidin(3)、monomethylsubchrin(4)、verruculogen(5)及chaetominine(6)。化合物1、2和6显示一定的肿瘤细胞抑制活性。结论 化合物1为新的硫代二酮哌嗪类化合物;化合物1、2和6具有肿瘤细胞毒活性。

Objective To study the cytotoxic secondary metabolites of the marine-derived fungus Aspergillus sp.HH-3.Methods The crude metabolite was purified by silica gel and sephadex LH-20 chromatography.The structures of the compounds were elucidated by MS and NMR analysis.The cytotoxities of the compounds against three tumor cells(A549,HepG2,HeLa)were evaluated using CCK-8 method.Results Six compounds were isolated from the marine-derived fungus Aspergillus sp.HH-3 including one new compound aspersin(1),and five known ones dehydroxymethylbis(dethio)bis(methylthio)gliotoxin(2),trypacidin(3),monomethylsubchrin(4),verruculogen(5)and chaetominine(6).Compounds 1,2,and 6 showed moderate cytotoxic activities against tumour cells of A549,HepG2 and HeLa.Conclusion Compound 1 is a new thiodiketopiperazine.Compounds 1,2,and 6 exhibit moderate antitumor activity.