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 Jul 6;17(7):400. doi: 10.3390/md17070400.
Ochrazepines A-D (-), four new conjugates dimerized from 2-hydroxycircumdatin C () and aspyrone () by a nucleophilic addition to epoxide, were isolated from the fermentation broth of the coral-associated strain LCJ11-102. Their structures including absolute configurations were determined based on spectroscopic analysis and chemical methods. Compounds - were also obtained by the semisynthesis from a nucleophilic addition of 2-hydroxycircumdatin C () to aspyrone (). New compound exhibited cytotoxic activity against 10 human cancer cell lines while new compounds and selectively inhibited U251 (human glioblastoma cell line) and compound was active against A673 (human rhabdomyoma cell line), U87 (human glioblastoma cell line), and Hep3B (human liver cancer cell line) with IC (half maximal inhibitory concentration) values of 2.5-11.3 μM among 26 tested human cancer cell lines.
从珊瑚共生菌株 LCJ11-102 的发酵液中分离得到了 4 个新的二聚体化合物 Ochrazepines A-D(-)，它们是由 2-羟基环大麻素 C()和阿斯泊酮()通过环氧化物的亲核加成反应形成的。基于光谱分析和化学方法确定了它们的结构包括绝对构型。还通过 2-羟基环大麻素 C()对阿斯泊酮()的亲核加成反应的半合成得到了化合物-。新化合物对 10 个人类癌细胞系表现出细胞毒性活性，而新化合物和选择性抑制 U251（人神经胶质瘤细胞系），化合物对 A673（人横纹肌瘤细胞系）、U87（人神经胶质瘤细胞系）和 Hep3B（人肝癌细胞系）具有活性，在 26 种测试的人类癌细胞系中，IC（半最大抑制浓度）值为 2.5-11.3 μM。
