Calcium-chelating alizarin and other anthraquinones inhibit biofilm formation and the hemolytic activity of Staphylococcus aureus

Staphylococcal biofilms are problematic and play a critical role in the persistence of chronic infections because of their abilities to tolerate antimicrobial agents. Thus, the inhibitions of biofilm formation and/or toxin production are viewed as alternative means of controlling Staphylococcus aure...

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Bibliographic Details
Published in:Scientific reports 2016-01, Vol.6 (1), p.19267-19267, Article 19267
Main Authors: Lee, Jin-Hyung, Kim, Yong-Guy, Yong Ryu, Shi, Lee, Jintae
Format: Article
Language:English
Subjects:
Aniline Compounds - pharmacology
Anthraquinone
Anthraquinones - pharmacology
Anti-Bacterial Agents - pharmacology
Antimicrobial agents
Biofilms
Biofilms - drug effects
Calcium
Cell aggregation
Gene Expression Profiling
Gene Expression Regulation, Bacterial - drug effects
Hemolysis - drug effects
Holin
Microbial Sensitivity Tests
Pathogens
Staphylococcus aureus
Staphylococcus aureus - drug effects
Staphylococcus aureus - physiology
Staphylococcus epidermidis - drug effects
Staphylococcus epidermidis - physiology
Transcription
Transcriptome
Virulence
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Summary:Staphylococcal biofilms are problematic and play a critical role in the persistence of chronic infections because of their abilities to tolerate antimicrobial agents. Thus, the inhibitions of biofilm formation and/or toxin production are viewed as alternative means of controlling Staphylococcus aureus infections. Here, the antibiofilm activities of 560 purified phytochemicals were examined. Alizarin at 10 μg/ml was found to efficiently inhibit biofilm formation by three S. aureus strains and a Staphylococcus epidermidis strain. In addition, two other anthraquinones purpurin and quinalizarin were found to have antibiofilm activity. Binding of Ca(2+) by alizarin decreased S. aureus biofilm formation and a calcium-specific chelating agent suppressed the effect of calcium. These three anthraquinones also markedly inhibited the hemolytic activity of S. aureus, and in-line with their antibiofilm activities, increased cell aggregation. A chemical structure-activity relationship study revealed that two hydroxyl units at the C-1 and C-2 positions of anthraquinone play important roles in antibiofilm and anti-hemolytic activities. Transcriptional analyses showed that alizarin repressed the α-hemolysin hla gene, biofilm-related genes (psmα, rbf, and spa), and modulated the expressions of cid/lrg genes (the holin/antiholin system). These findings suggest anthraquinones, especially alizarin, are potentially useful for controlling biofilm formation and the virulence of S. aureus.
ISSN:2045-2322
2045-2322
DOI:10.1038/srep19267