Dimeric Tetracenomycin Derivatives from a Taklamakan Desert-Derived Streptomyces sp. HDN154193
journal contributionposted on 22.12.2021, 06:03 by Li Xing, Yimin Chang, Xiaoqian Zhang, Xuewen Hou, Yaxin Han, Mudassir Shah, Tianjiao Zhu, Jixing Peng, Guojian Zhang, Qian Che, Dehai Li
Bitetracenomycin A (1) and its diastereomers [(±)-bitetracenomycin B, (±)-2] were discovered from the cultures of Streptomyces sp. HDN154193. Compounds 1 and (±)-2 were the first tetracenomycin dimers obtained from a natural source with sp3 methine protons at the bridge positions (C-12/12′), which also exhibited broad-spectrum antibacterial activity. The racemate (±)-2 was semisynthesized and separated into enantiomers (+)-2 and (−)-2, 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.
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spectrum antibacterial activitymic values rangingdimeric tetracenomycin derivativesalso exhibited broadenantiomers (+)-< b2 </ bracemate (±)-< b3 </ sup1 </ b(±)-< bstreptomyces </(−)-< b(< btaklamakan desertspecific rotationresistant strainsnatural sourcemethine protonsecd databridge positionsabsolute configurations9 μg