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目的对1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HPLC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合物结构鉴定,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10个asterriquinone类单体化合物(1~10),其化学结构分别鉴定为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)、ochrindole A(7)、asterriquinone C-1(8)、asterriquinone C-1methyl ether(9)、terrequinone(10);其中1、2、3为新化合物。针对HeLa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, identify and study the antitumor activity of a secondary metabolite of Aspergillus sclerotiorum XJW-56 isolated from the South China Sea sediment. Methods The fermentation products of fungi Aspergillus sclerotiorum XJW-56 were isolated by solvent extraction, column chromatography and preparative HPLC. The structures of the compounds were identified by NMR, MS and other spectroscopic techniques. The structures of the compounds were characterized by SRB and MTT Antitumor activity of compounds. Results Ten asterriquinone monomer compounds (1 ~ 10) were isolated from the fermentation products and their chemical structures were identified as petromurin C methyl ether (1), petromurin D methyl ether (2), asterriquinol D try methyl ether (3), asterriquinol D methyl ether (4), petromurin C (5), petromurin D (6), ochrindole A (7), asterriquinone C-1 2,3 are new compounds. The antitumor activity test of HeLa cells showed that only compounds 2, 3 and 7 ~ 10 showed different degrees of cytotoxicity. Conclusions Three (1-3) new compounds were found, of which the new compounds 2 and 3 had weak anti-tumor activity.