为研究海洋真菌萨氏曲霉(Aspergillus sydowii)MNP12010103的次级代谢产物及其抗肿瘤活性,采用活性导向方法以及大孔树脂、硅胶、Sephedax LH-20、半制备高效液相色谱等方法对其进行分离纯化,并经波谱分析对其进行结构鉴定。结果分离得到7个化合物,分别鉴定为:环(亮氨酸-脯氨酸)(化合物1),1,8-二羟基蒽醌(化合物2),5-吲哚醛(化合物3),大黄素-6-甲醚(化合物4),5-α-胆甾烷-3-酮(化合物5),尿嘧啶(化合物6),胸苷(化合物7)。其中,5-α-胆甾烷-3-酮(化合物5)为首次从微生物中分离得到;1,8-二羟基蒽醌(化合物2)为首次从海洋真菌中分离得到;化合物1、化合物3和化合物4为首次从该菌株中分离得到。化合物2抑制PANC-1细胞的IC50值为45.47μg/mL;化合物4抑制PC-3细胞的IC50值为53.97μg/mL;化合物2和化合物4浓度为100μg/mL时,对DPPH自由基的清除率均超过50%。
To study the secondary metabolites and their antitumor activity of the marine fungus Aspergillus sydowii MNP12010103,column chromatography on macroporous resin,silica gel,Sephadex-LH20,PHPLC were used to isolate the compounds from the marine fungus MNP12010103 using bioactivity guide method. The structures of these compounds were identified by spectroscopic analysis. Seven compounds obtained were identified as cyclo-( Leu-Pro)( compound 1),1,8-dihydroxy anthraquinone( compound 2),indole-5-carboxaldehyde( compound 3),physcion( compound 4),5α-cholestane-3-one( compound 5),uracil( compound 6),and thymidine( compound 7). Compound 5 was isolated from microorganism for the first time,compound 2 from marine fungus for the first time,and compound 1,3,4 from the fungi of Aspergillus sydowii for the first time. Compounds 2exhibits inhibitory activities on PANC-1 with IC50of 45. 47 μg /mL and compounds 4 shows cytotoxicity against PC-3 with IC50of 53. 97 μg /mL. The DPPH radical scavenging rate of both compound 2and compound 4 are more than 50% at a concentration of 100 μg /mL.