School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People's Republic of China.
Key Laboratory of Testing and Evaluation for Aquatic Product Safety and Quality, Ministry of Agriculture and Rural Affairs, Beijing 100125, People's Republic of China.
J Nat Prod. 2022 Jan 28;85(1):301-305. doi: 10.1021/acs.jnatprod.1c00735. Epub 2021 Dec 21.
Bitetracenomycin A () and its diastereomers [(±)-bitetracenomycin B, (±)-] were discovered from the cultures of sp. HDN154193. Compounds and (±)- were the first tetracenomycin dimers obtained from a natural source with sp methine protons at the bridge positions (C-12/12'), which also exhibited broad-spectrum antibacterial activity. The racemate (±)- was semisynthesized and separated into enantiomers (+)- and (-)-, and the absolute configurations were determined by specific rotation and ECD data. These metabolites exhibited potent antibacterial activity especially against drug-resistant strains (MRSA and MRCNS) with MIC values ranging from 1.0 to 1.9 μg/mL.
比替拉霉素 A () 及其非对映异构体 [(±)-比替拉霉素 B，(±)-] 是从 sp. HDN154193 的培养物中发现的。化合物 和 (±)- 是第一个从天然来源获得的四烯霉素二聚体，其桥位 (C-12/12') 上具有 sp 亚甲质子，还表现出广谱抗菌活性。外消旋体 (±)- 被半合成并分离成对映异构体 (+)- 和 (-)-，绝对构型通过比旋光度和 ECD 数据确定。这些代谢产物表现出很强的抗菌活性，特别是对耐药菌株 (MRSA 和 MRCNS)，其 MIC 值范围为 1.0 至 1.9 μg/mL。
