海洋海绵来源真菌 OUCMDZ-3839 的吖啶酮类化合物。

Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.

Open Studio for Druggability Research of Marine Natural Products, Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266003, China.

Mar Drugs. 2019 Apr 30;17(5):260. doi: 10.3390/md17050260.

Four new azaphilones, sclerotiorins A-D (-), as well as the dimeric sclerotiorin E () of which we first determined its absolute configuration, and 12 known analogues (-) were isolated from the fermentation broth of OUCMDZ-3839 associated with a marine sponge Paratetilla sp.. The new structures, including absolute configurations, were elucidated by spectroscopic analyses, optical rotation, ECD spectra, X-ray single-crystal diffraction, and chemical transformations. Compounds and displayed significant inhibitory activity against α-glycosidase, with IC values of 17.3 and 166.1 μM, respectively. In addition, compounds , , , - and showed moderate bioactivity against H1N1 virus.

从与海绵 Paratetilla sp. 共生的 OUCMDZ-3839 的发酵液中分离得到四个新的氮杂色酮类化合物，即 sclerotiorins A-D(-)，以及首次确定其绝对构型的二聚体 sclerotiorin E()，同时还分离得到了 12 个已知类似物(-)。通过光谱分析、旋光、ECD 光谱、X 射线单晶衍射和化学转化等方法阐明了这些新化合物的结构，包括绝对构型。化合物和对α-糖苷酶表现出显著的抑制活性，IC 值分别为 17.3 和 166.1 μM。此外，化合物、、、-和对 H1N1 病毒具有中等的生物活性。