Abstract
Psammaplin A, a natural bromotyrosine derivative from an associated form of two sponges (Poecillastra sp. and Jaspis sp.) was found to possess the antimicrobial effect on the Gram-positive bacteria, especially on methicillin-resistant Staphylococcus aureus (MRSA). The minimal inhibitory concentration of psammaplin A against twenty one MRSAs ranged from 0.781 to 6.25 microg/ml, while that of ciprofloxacin was 0.391-3.125 microg/ml. Psammaplin A could not bind to penicillin binding protein, but inhibited the DNA synthesis and the DNA gyrase activity with the respective 50% (DNA synthesis) and 100% (DNA gyrase) inhibitory concentration 2.83 and 100 microg/ml. These results indicate that psammaplin A has a considerable antibacterial activity, although restricted to a somewhat narrow range of bacteria, probably by inhibiting DNA gyrase.
MeSH terms
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Animals
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Anti-Bacterial Agents / metabolism
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Anti-Bacterial Agents / pharmacology*
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Bacterial Proteins*
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Carrier Proteins / metabolism
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Colony Count, Microbial
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DNA, Bacterial / biosynthesis
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Disulfides*
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Enzyme Inhibitors / metabolism
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Enzyme Inhibitors / pharmacology*
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Hexosyltransferases*
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Methicillin Resistance
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Muramoylpentapeptide Carboxypeptidase / metabolism
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Penicillin-Binding Proteins
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Peptidyl Transferases*
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Phenylpropionates / metabolism
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Phenylpropionates / pharmacology*
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Porifera / chemistry*
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Staphylococcus aureus / drug effects*
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Topoisomerase II Inhibitors*
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Tyrosine* / analogs & derivatives*
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Carrier Proteins
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DNA, Bacterial
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Disulfides
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Enzyme Inhibitors
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Penicillin-Binding Proteins
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Phenylpropionates
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Topoisomerase II Inhibitors
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psammaplin A
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Tyrosine
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Peptidyl Transferases
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Hexosyltransferases
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Muramoylpentapeptide Carboxypeptidase