Abstract
The escalation of antibiotic resistance among Gram-positive pathogens presents increasing treatment challenges and requires the development of innovative therapeutic agents. Here, we present the antimicrobial properties of structurally unusual bisanthraquinone metabolites produced by a marine streptomycete and four semi-synthetic derivatives. Biological activities were measured against clinically derived isolates of vancomycin-resistant Enterococcus faecium (VRE), and methicillin-susceptible, methicillin-resistant, and tetracycline-resistant Staphylococcus aureus (MSSA, MRSA, and TRSA, respectively). The most potent antibiotic displayed MIC(50) values of 0.11, 0.23, and 0.90microM against a panel (n=25 each) of clinical MSSA, MRSA, and VRE, respectively, and was determined to be bactericidal by time-kill analysis.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Anthraquinones / chemistry
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Anthraquinones / isolation & purification
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Anthraquinones / pharmacology*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / isolation & purification
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Anti-Bacterial Agents / pharmacology*
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Cells, Cultured / drug effects
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Enterococcus faecium / drug effects*
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Gram-Positive Bacterial Infections / drug therapy*
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Gram-Positive Bacterial Infections / microbiology
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Humans
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Methicillin Resistance
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Microbial Sensitivity Tests
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Staphylococcal Infections / drug therapy*
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Staphylococcal Infections / microbiology
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Staphylococcus aureus / drug effects*
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Tetracycline Resistance
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Vancomycin Resistance
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Virginiamycin
Substances
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Anthraquinones
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Anti-Bacterial Agents
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Virginiamycin