Abstract
Xanthorrizol (1) and 4-(1',5'-dimethylhex-4'-enyl)-2-methylphenol (2) were identified as the principal antimicrobial components of a CH(2)Cl(2)-MeOH (1:1) extract derived from Iostephane heterophylla. Compound 2 is a new natural product, but has been synthesized. Both compounds exhibited low level activity (MICs of 16-32 microg/mL) against methicillin-resistant staphylococci and vancomycin-resistant enterococci. They were either inactive or poorly active against Gram-negative bacteria and yeast. Mechanistic studies performed in Escherichia coli imp suggested nonspecific inhibition of DNA, RNA, and protein synthesis by both of these compounds. Compound 1 was tested in an in vivo model; it did not provide protection to mice infected with Staphylococcus aureus.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Anti-Bacterial Agents
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Anti-Infective Agents / chemistry
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Anti-Infective Agents / isolation & purification*
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Anti-Infective Agents / pharmacology
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Antifungal Agents / chemistry
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Antifungal Agents / isolation & purification*
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Antifungal Agents / pharmacology
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Asteraceae / chemistry*
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Candida albicans / drug effects
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DNA / biosynthesis
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DNA / drug effects
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Disease Models, Animal
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Drug Resistance, Microbial
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Enterococcus faecium / drug effects
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Escherichia coli / drug effects
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Female
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Magnetic Resonance Spectroscopy
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Mexico
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Mice
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Mice, Inbred Strains
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Microbial Sensitivity Tests
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Phenols / chemistry
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Phenols / isolation & purification*
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Phenols / pharmacology
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Plant Roots / chemistry
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Plants, Medicinal / chemistry*
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Protein Biosynthesis
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Proteins / drug effects
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RNA / biosynthesis
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RNA / drug effects
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Spectrophotometry, Ultraviolet
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Staphylococcus aureus / drug effects
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Vancomycin / pharmacology
Substances
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4-(1',5'-dimethylhex-4'-enyl)-2-methylphenol
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Anti-Bacterial Agents
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Anti-Infective Agents
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Antifungal Agents
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Phenols
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Proteins
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xanthorrhizol
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RNA
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Vancomycin
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DNA