Abstract
Two new norlignans, hyperiones A (1) and B (2), three new acylphloroglucinols, aspidinol C (3) and hyperaspidinols A (5) and B (6), the known compound aspidinol D (4), and the symmetrical dimeric xanthone hyperidixanthone (7) were isolated from Hypericum chinense. Their structures were established by spectroscopic analysis. In an antibacterial assay using a panel of multidrug-resistant (MDR) strains, compounds 3 and 4 exhibited promising activity against the NorA efflux protein overexpressing MDR Staphylococcus aureus strain SA-1199B with a minimum inhibitory concentration (MIC) of 2 μg/mL (8.4 μM) and 4 μg/mL (16.8 μM), respectively. The positive control antibiotic norfloxacin showed activity at MIC 32 μg/mL (100 μM).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Bacterial Proteins / drug effects
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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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Lignans / chemistry
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Lignans / isolation & purification*
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Lignans / pharmacology
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Mice
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Microbial Sensitivity Tests
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Molecular Structure
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Multidrug Resistance-Associated Proteins / drug effects
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Norfloxacin / pharmacology
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Nuclear Magnetic Resonance, Biomolecular
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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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Plant Leaves / chemistry
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Staphylococcus aureus / drug effects
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Staphylococcus aureus / metabolism*
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Tetracycline / pharmacology
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Xanthones / chemistry
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Xanthones / isolation & purification*
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Xanthones / pharmacology
Substances
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Bacterial Proteins
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Drugs, Chinese Herbal
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Lignans
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Multidrug Resistance-Associated Proteins
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Xanthones
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NorA protein, Staphylococcus
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xanthone
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Phloroglucinol
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Tetracycline
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Norfloxacin