Mutasynthesis of Antibacterial Halogenated Actinomycin Analogues.

J Nat Prod

CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, People's Republic of China.

Published: August 2021

Through precursor-directed biosynthesis, feeding halogenated (F-, Cl-, Br-, I-) or methoxy-substituted 4-methyl-3-hydroxyanthranilic acid (4-MHA) analogues to the -deleted mutant strain of SCSIO ZS0073 led to the production of ten new actinomycin analogues (-). Several of the actinomycin congeners displayed impressive antimicrobial activities, with MIC values spanning 0.06-64 μg/mL to clinically derived antibiotic resistant pathogens, including , , and , with low cytotoxicity.

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http://dx.doi.org/10.1021/acs.jnatprod.1c00294DOI Listing

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