State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China.
Institute of Ocean Research, Ningbo Institute of Marine Medicine, Peking University, Ningbo 315010, China.
Mar Drugs. 2022 Nov 13;20(11):712. doi: 10.3390/md20110712.
Chemical examination of a marine sponge-associated fungus resulted in the isolation of ten undescribed eremophilanes, namely copteremophilanes A-J (-), along with two new glycosides, 5-glycopenostatin F () and 5-glucopenostatin I (). Their structures were determined by extensive spectroscopic data, in association with ECD data and chemical conversions for configurational assignments. Analogs , , and represent a group of uncommon skeletons of eremophilanes with an aromatic ring and a methyl migration from C-5 to C-9, and analogs and are characteristic of a PKS scaffold bearing a glucose unit. The incorporation of a chlorinated phenylacetic unit in - is rarely found in nature. Analog showed neuroprotective effect, whereas exhibited selective inhibition against human non-small cell lung cancer cells (A549). This study enriched the chemical diversity of eremophilanes and extended their bioactivities to neuroprotection.
海洋海绵共生真菌的化学成分研究分离得到了十个未描述的埃罗菲烷类化合物，分别为 copteremophilanes A-J (-)，以及两个新的糖苷，5-糖基 penostatin F ()和 5-葡萄糖基 penostatin I ()。通过广泛的光谱数据分析，结合 ECD 数据和构型分配的化学转化，确定了它们的结构。类似物,, 和 代表了一组罕见的埃罗菲烷类化合物，具有芳香环和从 C-5 到 C-9 的甲基迁移，类似物 和 是具有葡萄糖单元的 PKS 支架的特征。在 - 中引入氯化苯乙酸单元在自然界中很少见。类似物 表现出神经保护作用，而 对人非小细胞肺癌细胞 (A549) 表现出选择性抑制作用。本研究丰富了埃罗菲烷类化合物的化学多样性，并将其生物活性扩展到神经保护。
