Abstract
Total of 22 caged xanthones were subjected to susceptibility testing of global epidemic MRSA USA300. Natural morellic acid showed the strongest potency (MIC of 12.5μM). However, its potent toxicity diminishes MRSA therapeutic potential. We synthetically modified natural morellic acid to yield 13 derivatives (3a-3m). Synthetically modified 3b retained strong potency in MRSA growth inhibition, yet the toxicity was 20-fold less than natural morellic acid, permitting the possibility of using caged xanthones for MRSA therapeutic.
Keywords:
Bacterial invasion; Caged xanthones; Methicillin resistant Staphylococcus aureus; USA300.
Copyright © 2016 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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A549 Cells
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Amino Acids / chemical synthesis
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Amino Acids / pharmacology
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Amino Acids / toxicity
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Ampicillin / pharmacology
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / pharmacology*
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Anti-Bacterial Agents / toxicity
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Bacterial Adhesion / drug effects
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Garcinia
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HEK293 Cells
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / isolation & purification
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Heterocyclic Compounds / pharmacology
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Heterocyclic Compounds / toxicity
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Heterocyclic Compounds, Bridged-Ring / chemical synthesis
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Heterocyclic Compounds, Bridged-Ring / isolation & purification
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Heterocyclic Compounds, Bridged-Ring / pharmacology*
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Heterocyclic Compounds, Bridged-Ring / toxicity
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Humans
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Methicillin-Resistant Staphylococcus aureus / drug effects*
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Methicillin-Resistant Staphylococcus aureus / physiology
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Microbial Sensitivity Tests
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Oxacillin / pharmacology
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Xanthones / chemical synthesis
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Xanthones / chemistry
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Xanthones / isolation & purification
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Xanthones / pharmacology*
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Xanthones / toxicity
Substances
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Amino Acids
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Anti-Bacterial Agents
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Heterocyclic Compounds
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Heterocyclic Compounds, Bridged-Ring
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Xanthones
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forbesione
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morellic acid
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Ampicillin
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gambogic acid
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Oxacillin