Abstract
Berberine is a substituted dibenzo[a,g]quinolizin-7-ium derivative whose modest antibiotic activity is derived from its disruptive impact on the function of the essential bacterial cell division protein FtsZ. The present study reveals that the presence of a biphenyl substituent at either the 2- or 12-position of structurally-related dibenzo[a,g]quinolizin-7-ium derivatives significantly enhances antibacterial potency versus Staphylococcus aureus and Enterococcus faecalis. Studies with purified S. aureus FtsZ demonstrate that both 2- and 12-biphenyl dibenzo[a,g]quinolizin-7-ium derivatives act as enhancers of FtsZ self-polymerization.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology
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Bacterial Proteins / antagonists & inhibitors
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Bacterial Proteins / metabolism
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Berberine / chemistry
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Cytoskeletal Proteins / antagonists & inhibitors
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Cytoskeletal Proteins / metabolism
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Enterococcus faecalis / drug effects
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Microbial Sensitivity Tests
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Quinolizines / chemical synthesis
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Quinolizines / chemistry*
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Quinolizines / pharmacology
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Staphylococcus aureus / drug effects
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Staphylococcus aureus / metabolism
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Cytoskeletal Proteins
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FtsZ protein, Bacteria
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Quinolizines
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Berberine