Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>

<i>Staphylococcus aureus</i> (<i>S. aureus</i>) represents an important pathogen of clinical relevance, causing a wide variety of symptoms. The broad distribution of multidrug-resistant strains necessarily demands new antibacterial agents for the treatment of <i>S. aure...

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Main Authors: Federica Dell’Annunziata, Veronica Folliero, Francesca Palma, Valeria Crudele, Emiliana Finamore, Giuseppina Sanna, Aldo Manzin, Anna De Filippis, Massimiliano Galdiero, Gianluigi Franci
Format: Article
Language:English
Published: MDPI AG 2022-08-01
Series:Applied Sciences
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Online Access:https://www.mdpi.com/2076-3417/12/17/8691
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author Federica Dell’Annunziata
Veronica Folliero
Francesca Palma
Valeria Crudele
Emiliana Finamore
Giuseppina Sanna
Aldo Manzin
Anna De Filippis
Massimiliano Galdiero
Gianluigi Franci
author_facet Federica Dell’Annunziata
Veronica Folliero
Francesca Palma
Valeria Crudele
Emiliana Finamore
Giuseppina Sanna
Aldo Manzin
Anna De Filippis
Massimiliano Galdiero
Gianluigi Franci
author_sort Federica Dell’Annunziata
collection DOAJ
description <i>Staphylococcus aureus</i> (<i>S. aureus</i>) represents an important pathogen of clinical relevance, causing a wide variety of symptoms. The broad distribution of multidrug-resistant strains necessarily demands new antibacterial agents for the treatment of <i>S. aureus</i> infections. The aim of this study was to assess the antibacterial activity of plant-derived compounds, pure 4,5″-dihydroxy-anthraquinone-2-carboxylic acid (Rhein), against standard and clinical isolated <i>S. aureus</i> strains. The hemolysis and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assays were used to determine the cytotoxicity on human erythrocytes and bronchial epithelial cells after treatment with Rhein. The antibacterial effect was assessed via disk diffusion test, broth microdilution methods, time-killing assays and live–dead evaluation (50–0.39 µg/mL). Rhein effect on the hemolytic activity of α-toxin and catalase were estimated. Moreover, crystal violet (CV) assay evaluated its impact on biofilm biomass. The compound exhibited 50% cytotoxic concentration (CC<sub>50</sub>) and 50% hemolysis concentration (EC<sub>50</sub>) of 43.6 and >50 µg/mL, respectively. The minimum inhibitory concentration (MIC) of Rhein was 12.5 µg/mL for all tested strains, exerting bacteriostatic action. MIC and sub-MIC concentrations of Rhein significantly reduced hemolytic and catalase activities, impairing the major virulence factors of <i>S. aureus</i> strains. Rhein also reduced biofilm biomass in a dose-dependent manner, reaching rates of about 50% eradication at a dose of 50 µg/mL. These findings suggest that Rhein could represent a promising therapeutic option for the treatment of <i>S. aureus</i> infections.
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spelling doaj.art-a3ab8a57d6894efc82807871ef16fe1c2023-11-23T12:45:08ZengMDPI AGApplied Sciences2076-34172022-08-011217869110.3390/app12178691Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>Federica Dell’Annunziata0Veronica Folliero1Francesca Palma2Valeria Crudele3Emiliana Finamore4Giuseppina Sanna5Aldo Manzin6Anna De Filippis7Massimiliano Galdiero8Gianluigi Franci9Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”, 80138 Naples, ItalyDepartment of Experimental Medicine, University of Campania “Luigi Vanvitelli”, 80138 Naples, ItalyDepartment of Experimental Medicine, University of Campania “Luigi Vanvitelli”, 80138 Naples, ItalySection of Microbiology and Virology, University Hospital “Luigi Vanvitelli”, 80138 Naples, ItalySection of Microbiology and Virology, University Hospital “Luigi Vanvitelli”, 80138 Naples, ItalyMicrobiology and Virology Unit, Department of Biomedical Sciences, University of Cagliari, 09042 Monserrato, ItalyMicrobiology and Virology Unit, Department of Biomedical Sciences, University of Cagliari, 09042 Monserrato, ItalyDepartment of Experimental Medicine, University of Campania “Luigi Vanvitelli”, 80138 Naples, ItalyDepartment of Experimental Medicine, University of Campania “Luigi Vanvitelli”, 80138 Naples, ItalyDepartment of Medicine, Surgery and Dentistry “Scuola Medica Salernitana”, University of Salerno, 84081 Baronissi, Italy<i>Staphylococcus aureus</i> (<i>S. aureus</i>) represents an important pathogen of clinical relevance, causing a wide variety of symptoms. The broad distribution of multidrug-resistant strains necessarily demands new antibacterial agents for the treatment of <i>S. aureus</i> infections. The aim of this study was to assess the antibacterial activity of plant-derived compounds, pure 4,5″-dihydroxy-anthraquinone-2-carboxylic acid (Rhein), against standard and clinical isolated <i>S. aureus</i> strains. The hemolysis and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assays were used to determine the cytotoxicity on human erythrocytes and bronchial epithelial cells after treatment with Rhein. The antibacterial effect was assessed via disk diffusion test, broth microdilution methods, time-killing assays and live–dead evaluation (50–0.39 µg/mL). Rhein effect on the hemolytic activity of α-toxin and catalase were estimated. Moreover, crystal violet (CV) assay evaluated its impact on biofilm biomass. The compound exhibited 50% cytotoxic concentration (CC<sub>50</sub>) and 50% hemolysis concentration (EC<sub>50</sub>) of 43.6 and >50 µg/mL, respectively. The minimum inhibitory concentration (MIC) of Rhein was 12.5 µg/mL for all tested strains, exerting bacteriostatic action. MIC and sub-MIC concentrations of Rhein significantly reduced hemolytic and catalase activities, impairing the major virulence factors of <i>S. aureus</i> strains. Rhein also reduced biofilm biomass in a dose-dependent manner, reaching rates of about 50% eradication at a dose of 50 µg/mL. These findings suggest that Rhein could represent a promising therapeutic option for the treatment of <i>S. aureus</i> infections.https://www.mdpi.com/2076-3417/12/17/8691<i>Staphylococcus aureus</i>Rheinnatural productantibacterial activityantibiofilm activity
spellingShingle Federica Dell’Annunziata
Veronica Folliero
Francesca Palma
Valeria Crudele
Emiliana Finamore
Giuseppina Sanna
Aldo Manzin
Anna De Filippis
Massimiliano Galdiero
Gianluigi Franci
Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>
Applied Sciences
<i>Staphylococcus aureus</i>
Rhein
natural product
antibacterial activity
antibiofilm activity
title Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>
title_full Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>
title_fullStr Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>
title_full_unstemmed Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>
title_short Anthraquinone Rhein Exhibits Antibacterial Activity against <i>Staphylococcus aureus</i>
title_sort anthraquinone rhein exhibits antibacterial activity against i staphylococcus aureus i
topic <i>Staphylococcus aureus</i>
Rhein
natural product
antibacterial activity
antibiofilm activity
url https://www.mdpi.com/2076-3417/12/17/8691
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