Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China.
Hainan Key Laboratory of Conservation and Utilization of Tropical Agricultural Bioresources, Hainan Institute of Tropical Agricultural Resources, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China.
Mar Drugs. 2021 Nov 5;19(11):624. doi: 10.3390/md19110624.
Marine actinomycetes are prolific chemical sources of complex and novel natural products, providing an excellent chance for new drug discovery. The chemical investigation of the marine-derived sp. ITBB-ZKa6, from Zhaoshu island, Hainan, led to the discovery of two unique antimycin-type depsipeptides, zhaoshumycins A () and B (), along with the isolation of the four known neoantimycins A (), F (), D (), and E (). The structures of the new compounds and were elucidated on the basis of the analysis of diverse spectroscopic data and biogenetic consideration. Zhaoshumycins A () and B () represent a new class of depsipeptides, featuring two neoantimycin monomers (only neoantimycin D or neoantimycins D and E) linked to a 1,4-disubstituted benzene ring via an imino group. Initial toxicity tests of - in MCF7 human breast cancer cells revealed that compounds and possess weak cytotoxic activity. Further structure-activity relationship analysis suggested the importance of the NH group at C-34 in and for cytotoxicity in MCF7 cells.
海洋放线菌是复杂和新颖天然产物的丰富化学来源，为新药发现提供了极好的机会。对海南赵树岛海洋来源的 sp. ITBB-ZKa6 的化学研究发现了两种独特的安密霉素型去肽，分别为 zhaoshumycins A () 和 B ()，同时还分离出了四种已知的 neoantimycins A (), F (), D () 和 E ()。新化合物和的结构是根据各种光谱数据分析和生物发生考虑得出的。Zhaoshumycins A () 和 B () 代表了一类新的去肽，其特征在于两个 neoantimycin 单体（仅 neoantimycin D 或 neoantimycins D 和 E）通过亚氨基连接到 1,4-取代的苯环上。在 MCF7 人乳腺癌细胞中的毒性测试表明，化合物和具有较弱的细胞毒性活性。进一步的结构-活性关系分析表明，化合物和中 C-34 上的 NH 基团对于 MCF7 细胞的细胞毒性很重要。
Zotero 插件