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Through precursor-directed biosynthesis, feeding halogenated (F-, Cl-, Br-, I-) or methoxy-substituted 4-methyl-3-hydroxyanthranilic acid (4-MHA) analogues to the acnGHLM-deleted mutant strain of Streptomyces costaricanus SCSIO ZS0073 led to the production of ten new actinomycin analogues (4-13). 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 Staphylococcus aureus, Enterococcus faecium, and Candida albicans, with low cytotoxicity.


Ziwei Yao, Changli Sun, Yuhui Xia, Fang Wang, Liwu Fu, Junying Ma, Qinglian Li, Jianhua Ju. Mutasynthesis of Antibacterial Halogenated Actinomycin Analogues. Journal of natural products. 2021 Aug 27;84(8):2217-2225

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PMID: 34270246

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