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Antibacterial Activity and Mode of Action of Lactoquinomycin A from Streptomyces bacillaris.


ABSTRACT: This study aims to isolate and identify the structure of antibacterial compounds having potent activity on methicillin-resistant Staphylococcus aureus (MRSA) from marine actinomycetes, and also to identify their mode of action. Lactoquinomycin A (LQM-A) (compound 1) and its derivatives (2-4) were isolated from marine-derived Streptomyces bacillaris strain MBTC38, and their structures were determined using extensive spectroscopic methods. These compounds showed potent antibacterial activities against Gram-positive bacteria, with MIC values of 0.06-4 ?g/mL. However, the tested compounds exhibited weak inhibitory activity against Gram-negative bacteria, although they were effective against Salmonella enterica (MIC = 0.03-1 ?g/mL). LQM-A exhibited the most significant inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA) (MIC = 0.25-0.5 ?g/mL), with a low incidence of resistance. An in vivo dual-reporter assay designed to distinguish between compounds that inhibit translation and those that induce DNA damage was employed to assess the mode of action of LQM-A. LQM-A-induced DNA damage and did not inhibit protein synthesis. The gel mobility shift assay showed that LQM-A switched plasmid DNA from the supercoiled to relaxed form in a time- and concentration-dependent manner. These data suggest that LQM-A intercalated into double-stranded DNA and damaged DNA repair.

SUBMITTER: Chung B 

PROVIDER: S-EPMC7823745 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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Antibacterial Activity and Mode of Action of Lactoquinomycin A from <i>Streptomyces bacillaris</i>.

Chung Beomkoo B   Kwon Oh-Seok OS   Shin Jongheon J   Oh Ki-Bong KB  

Marine drugs 20201224 1


This study aims to isolate and identify the structure of antibacterial compounds having potent activity on methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) from marine actinomycetes, and also to identify their mode of action. Lactoquinomycin A (LQM-A) (compound <b>1</b>) and its derivatives (<b>2</b>-<b>4</b>) were isolated from marine-derived <i>Streptomyces bacillaris</i> strain MBTC38, and their structures were determined using extensive spectroscopic methods. These compounds showed  ...[more]

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