目的 研究海南东寨港秋茄内生真菌Penicillium sp. KF22次级代谢产物,并对其进行初步的活性筛选。方法 采用大米培养基,对海南东寨港秋茄内生真菌Penicillium sp. KF22进行常温静置培养,硅胶柱色谱和半制备高效液相色谱对其次级代谢产物进行分离纯化,获得单体化合物,经过MS和NMR数据分析,对比文献数据,鉴定其结构,并采用MTT法对化合物进行体外抑制肿瘤细胞生长的活性研究,采用浓度梯度稀释法进行抑菌活性测试。结果 从秋茄内生真菌Penicillium sp. KF22次级代谢产物分离得到7个聚酮类化合物,分别为:sydowinol(1),sydowinin A(2),6,6'-dinor-bipenicilisorin(3),monomethylsulochrin(4),对羟基苯乙酸甲酯(5),对羟基苯甲醛(6)和3,3'-二羟基-5,5'-二甲基二苯醚(7),X-单晶衍射结果进一步证实化合物4的结构。结论 化合物1~3为首次从青霉属真菌次级代谢产物中分离得到。化合物3对人前列腺癌细胞PC-3有中等的抑制活性,IC₅₀值为15.89 μmol·L^-1,而化合物1对人乳腺癌细胞MDA-MB-231有微弱的抑制活性,IC₅₀值为42.63 μmol·L^-1,化合物1~7对金黄色葡萄球菌(Staphyloccocus aureus ATCC29213)和大肠杆菌(Escherichia coli ATCC25922)均无抑菌活性(MIC＞50 μmol·L^-1)。

OBJECTIVE To study the secondary metabolites of the endophytic fungus Penicillium sp. KF22 isolated from Dongzhai Harbor, Hainan, and evaluate their anti-tumor and antibacterial activities of the purified compounds. METHODS This fungus was fermented statically by using rice medium at room temperature. The secondary metabolites were purified from the culture by various chromatographic purification techniques. The in vitro anti-tumor activities of the isolated compounds were tested by MTT method, and the antibacterial activities were tested by gradient dilution method. RESULTS The chemical structures were identified as sydowinol (1), sydowinin A (2), 6, 6'-dinor-bipenicilisorin (3), monomethylsulochrin (4), methyl p-hydroxyphenylacetate (5), p-hydroxybenzaldehyde (6) and 3, 3'-dihydroxy-5,5'-dimethyldiphenyl ether (7). Furthermore,the structure of compound 4 is also confirmed by X-ray diffraction. CONCLUSIONS Compounds 1-3 are isolated from the genus of Penicillium sp. for the first time. The anti-tumor activities of compounds 1-7 are evaluated against MDA-MB-231 and PC-3 cell lines. Compound 3 exhibits moderate cytotoxicity against human prostate cancer line PC-3 with an IC₅₀ value of 15.89 μmol·L^-1, while compound 1 shows weak cytotoxicity against human breast cancer cell line MDA-MB-231 with an IC₅₀ value of 42.63 μmol·L^-1. In addition, compounds 1-7 didn't show antibacterial effect against Staphyloccocus aureus ATCC29213 and Escherichia coli ATCC25922(MIC＞50 μmol·L^-1).