Abstract
Bioassay-directed fractionation using multidrug-resistant (MDR) Staphylococcus aureus resulted in the isolation of four new polyprenylated benzophloroglucinol derivatives, sampsoniones N-Q (1-4), and four known compounds, 7-epiclusianone (5) and sampsoniones B, L, and R, from the roots of Hypericum sampsonii. The structures of these compounds were established by analysis of spectroscopic data, and the structures of 4 and 5 were determined by single-crystal X-ray diffraction crystallography. In the bioassay, 7-epiclusianone (5) showed promising activity with a minimum inhibitory concentration (MIC) of 7.3 microM against the NorA overexpressing MDR S. aureus strain SA-1199B; the positive control antibiotic norfloxacin showed activity at MIC 100 microM.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Benzophenones / chemistry
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Benzophenones / isolation & purification
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Benzoquinones / chemistry
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Benzoquinones / isolation & purification
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Crystallography, X-Ray
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Drug Resistance, Multiple, Bacterial / drug effects
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Drugs, Chinese Herbal / chemistry
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Drugs, Chinese Herbal / isolation & purification*
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Drugs, Chinese Herbal / pharmacology*
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Hypericum / chemistry*
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Methicillin Resistance / drug effects
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Microbial Sensitivity Tests
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Molecular Conformation
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Molecular Structure
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Norfloxacin / pharmacology
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Phloroglucinol / analogs & derivatives*
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Phloroglucinol / chemistry
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Phloroglucinol / isolation & purification*
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Phloroglucinol / pharmacology
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Plants, Medicinal / chemistry*
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Staphylococcus aureus / drug effects*
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Staphylococcus aureus / genetics
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Staphylococcus aureus / metabolism
Substances
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7-epiclusianone
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Anti-Bacterial Agents
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Benzophenones
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Benzoquinones
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Drugs, Chinese Herbal
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Phloroglucinol
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Norfloxacin