In our previous studies, the marine-derived fungus Emericellopsis maritima BC17 was found to produce new eremophilane-type sesquiterpenoids on solid media. In order to explore its potential to produce more metabolites, E. maritima BC17 was subjected to a one strain-many compounds (OSMAC) analysis leading to the discovery of three new eremophilanes (1-3) and fourteen known derivatives (4-17) in the liquid media Czapek Dox and PDB. Their structures were established by extensive analyses of the 1D and 2D NMR, and HRESIMS data, as well as ECD data for the assignment of their absolute configurations. Antitumoral and antimicrobial activities of the isolated metabolites 1, 3, 11, and 15 were investigated. PR toxin 3-deacetyl (15) exhibited cytotoxic activity against HepG2, MCF-7, A549, A2058 and Mia PaCa-2 human cancer cell lines with IC50 values ranging from 2.5 to 14.7 µM. In addition, 15 exhibited selective activity against methicillin-sensitive Staphylococcus aureus ATCC29213 at the highest concentration tested of 128 µg/mL.

中文翻译：

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通过改变培养条件从海洋源性真菌 Emericellopsis maritima BC17 中发现新的 eremophilane：细胞毒性和抗菌活性评估


在我们之前的研究中，发现海洋来源的真菌 Emericellopsis maritima BC17 在固体培养基上产生新的 eremophilane 型倍半萜类化合物。为了探索其产生更多代谢物的潜力，对 E. maritima BC17 进行了单菌株多化合物 (OSMAC) 分析，结果发现了三种新的 eremophilane (1-3) 和 14 种已知衍生物 (4-17)在液体介质 Czapek Dox 和 PDB 中。它们的结构是通过对 1D 和 2D NMR、HRESIMS 数据以及用于分配其绝对构型的 ECD 数据进行广泛分析而确定的。研究了分离的代谢物 1、3、11 和 15 的抗肿瘤和抗菌活性。 PR 毒素 3-de乙酰 (15) 对 HepG2、MCF-7、A549、A2058 和 Mia PaCa-2 人类癌细胞系表现出细胞毒活性，IC50 值范围为 2.5 至 14.7 µM。此外，15 种在最高测试浓度 128 µg/mL 下表现出针对甲氧西林敏感金黄色葡萄球菌 ATCC29213 的选择性活性。