曲霉属真菌Aspergillus sclerotiorum XJW-56中抗肿瘤活性次级代谢产物研究

The cytotoxic secondary metabolites from the South China Sea derived fungus Aspergillus sclerotiorum XJW-56

目的对l株分离自南海沉淀物的曲霉属真菌Aspergillus sclerotiorum XJW-56的次级代谢产物进行分离、鉴定及抗肿瘤活性研究。方法采用溶剂萃取、柱色谱层析及制备HPI，C等方法对真菌Aspergillus sclerotiorum XJW-56的发酵产物进行化学分离，通过NMR、MS等波谱学技术并参阅文献进行化舍物结构鉴定，采用SRB和MTT法评价化合物的抗肿瘤活性。结果从发酵产物中分离得到lO个asterriquinone类单体化合物（1-10），其化学结构分别鉴定为petromurin Cmethyl ether（1）、petromurin Dmethylether（2）、as-terriquinol Dtrymethyl ether（3）、asterriquinol D methyl ether（4）、petromurin C（5）、petromurin D（6）、ochrindole A（7）、asterriquinone C-1（8）、asterriquinone C-1 methylether（9）、terrequinone（10）；其中1、2、3为新化合物。针对Hel，a细胞进行抗肿瘤活性测试结果显示只有化合物2、3、7-10表现出不同程度的细胞毒作用。结论发现新结构化合物3个（1-3），其中新结构化合物2和3具有弱的抗肿瘤活性。

Objective To isolate and identify the antitumor components of the South China Sea derived fungus Aspergillus sclerotiorurn XJW-56. Methods The extracts of the fungus were purified by repeated normal and reverse phase column chromatography and preparative HPLC guided by the bioassay re-suits. Their structures were established by physicochemical properties and spectroscopic analysis. Their proliferation inhibition activities were evaluated by MTT and SRB methods. Results Ten com- pounds were identified as petromurin C methyl ether （1）, petromurin D methyl ether （2）, asterriquinol D trymethyl ether （3）, asterriquinol D methyl ether （4）, petromurin C （5）, petromurin D （6）, ochrin-dole A （7）, asterriquinone C-1 （8）, asterriquinone C-1 methyl ether （9）, and terrequinone （10）. A-mong them, compounds 1-3 were new structures. The eytotoxities of compounds 1-10 were tested on HeLa cell line. Conclusion Three new compounds （1-3） were isolated and two of them （2-3） showed cy- totoxities.