从珊瑚来源真菌 Aspergillus tritici SP2-8-1 中分离得到的细胞毒性和抗菌化合物。
Cytotoxic and Antibacterial Compounds from the Coral-Derived Fungus Aspergillus tritici SP2-8-1.
机构信息
Key Laboratory of Urban Environment and Health, Institute of Urban Environment, Chinese Academy of Sciences, Xiamen 361021, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
出版信息
Mar Drugs. 2017 Nov 7;15(11):348. doi: 10.3390/md15110348.
Three novel compounds, 4-methyl-candidusin A (), aspetritone A () and aspetritone B (), were obtained from the culture of a coral-derived fungus SP2-8-1, together with fifteen known compounds (-). Their structures, including absolute configurations, were assigned based on NMR, MS, and time-dependent density functional theory (TD-DFT) ECD calculations. Compounds and exhibited better activities against methicillin-resistant strains of (MRSA) ATCC 43300 and MRSA CGMCC 1.12409 than the positive control chloramphenicol. Compound displayed stronger anti-MRSA and lower cytotoxic activities than , and showed stronger antibacterial activities against strains of , , and than the other compounds. Compounds and exhibited significantly stronger cytotoxic activities against human cancer cell lines HeLa, A549, and Hep G2 than the other compounds. Preliminary structure-activity relationship studies indicated that prenylation of terphenyllin or candidusin and the tetrahydrobenzene moiety in anthraquinone derivatives may influence their bioactivity.
从珊瑚来源的真菌 SP2-8-1 的培养物中获得了三个新化合物，4-甲基-candidusin A()、aspetritone A()和 aspetritone B()，以及十五个已知化合物(-)。基于 NMR、MS 和时变密度泛函理论（TD-DFT）ECD 计算，确定了它们的结构，包括绝对构型。化合物和对耐甲氧西林金黄色葡萄球菌（MRSA）ATCC 43300 和 MRSA CGMCC 1.12409 的活性优于阳性对照氯霉素。化合物显示出比更强的抗 MRSA 和更低的细胞毒性活性，比其他化合物对、和的抗菌活性更强。化合物和对人癌细胞系 HeLa、A549 和 Hep G2 的细胞毒性活性明显强于其他化合物。初步的结构-活性关系研究表明，三萜烯或 candidusin 的 prenylation 和蒽醌衍生物中的四氢苯部分可能影响它们的生物活性。
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