&lt;i&gt;In Vitro&lt;/i&gt; Synergism and Anti-biofilm Activity of Quercetin–Pivaloxymethyl Conjugate against &lt;i&gt;Staphylococcus aureus&lt;/i&gt; and &lt;i&gt;Enterococcus&lt;/i&gt; Species

Kim, Mi Kyoung; Lee, Taegum; Jung, Minji; Park, Ki Ho; Chong, Youhoon

doi:10.1248/cpb.c18-00380

Cited by 18 publications

(10 citation statements)

References 15 publications

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“…Quercetin was able to eradicate pre-prepared S. aureus biofilms at -1 50 mg ml , which completely inhibited biofilm production (87.7%) in a dose-dependent manner. A contemporary study demonstrated the inhibitory effect of quercetin on both clinical and reference -1 isolates of S. aureus (250-500µg ml ) (da Costa Júnior et al, 2018) and another study reported that quercetin crippled biofilm production in S. aureus isolates when applied at various -1 concentrations (1-50 mg ml ) (Kim et al, 2018) which is consistent with our findings. Comparable results show that quercetin also demonstrated reliable antibiofilm activity against S. mutans, which may be used for treating dental caries (Zeng et al, 2019).…”

Section: O N L I N E C O P ÿsupporting

confidence: 92%

Quercetin mediated inhibition of Staphylococcus aureus biofilms and the impact of the isolate phenotype and genotype

Eldrehmy¹,

Abdel-Hafez²,

Alghamdi³

et al. 2021

JEB

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Aim: This study was designed to assess the antibiofilm activity of quercetin on characterized S. aureus isolates. Methodology: This study evaluated 36 S. aureus isolates, each of which was identified using Gram staining, culture, biochemical, and PCR assays. Isolates were cultured and their biofilm production was evaluated using Congo red agar (CRA) plates, microtiter plate tests and PCR, and the effects of quercetin were examined. Results: The CRA results revealed that eight (22.3%) S. aureus isolates were strongly positive for biofilm production and an additional 18 isolates (50%) showed moderate biofilm capacity. The remaining 10 isolates were negative (27.7%) for biofilm production. S. aureus isolates were divided into strong positive, intermediate, and negative groups, 27.8%, 44.5%, and 27.7%, respectively. Scanning electron microscopy showed that the biofilm-producing isolates appeared as aggregates of cells within a heavy matrix. In addition, PCR assay identified IcaA and IcaD (66.6% for both) biofilm production genes in most isolates and IcaC (61.1%), IcaB, FnbB (33.3% for both), and Fib (22.2%) in several other strains. Quercetin significantly inhibited biofilm activity in biofilm producing S. aureus isolates in a dose-dependent manner, with an inhibition rate of 29.6-87.7%. Interpretation: Biofilm production is dependent on Ica gene phenotype and strains with an IcaABCD or IcaABD phenotype produce more biofilm than strains with IcaAD phenotype. Quercetin significantly inhibited S. aureus biofilm production, irrespective of Ica phenotype.

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Section: O N L I N E C O P ÿsupporting

confidence: 92%

Quercetin mediated inhibition of Staphylococcus aureus biofilms and the impact of the isolate phenotype and genotype

Eldrehmy¹,

Abdel-Hafez²,

Alghamdi³

et al. 2021

JEB

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“…As mentioned above, quercetin and its derivatives more easily disrupt the membrane of gram-positive bacteria compared with that of gram-negative bacteria. In addition, previous studies showed that quercetin and its derivatives inhibit hemolysis and biofilm formation in S. aureus by reducing alpha-toxin secretion [26][27][28][29] , which might explain the S. aureus-specific anti-biofilm effect of di-F-Q. On the other hand, quercetin is also known to inhibit the aqr quorum-sensing system which modules biofilm formation in S. aureus 28 .…”

Section: Resultsmentioning

confidence: 97%

Strain-specific anti-biofilm and antibiotic-potentiating activity of 3′,4′-difluoroquercetin

Kho

Kim

Jung

et al. 2020

Sci Rep

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Antibacterial properties of 3′,4′-difluoroquercetin (di-F-Q), a fluorine-substituted stable quercetin derivative, were investigated. Even though di-F-Q itself did not show interesting antibacterial activity, treatment of the Staphylococcus aureus strains with di-F-Q resulted in a dose-dependent reduction in biofilm formation with IC 50 values of 1.8 ~ 5.3 mg/L. Also, the antibacterial activity of ceftazidime (CAZ) against carbapenem-resistant Pseudomonas aeruginosa (CRPA) showed eightfold decrease upon combination with di-F-Q. Assessment of the antimicrobial activity of CAZ in combination with di-F-Q against 50 clinical isolates of P. aeruginosa confirmed 15.7% increase in the percentages of susceptible P. aeruginosa isolates upon addition of di-F-Q to CAZ. Further mechanistic studies revealed that di-F-Q affected the antibiotics efflux system in CRPA but not the β-lactamase activity. Thus, di-F-Q was almost equally effective as carbonyl cyanide m-chlorophenyl hydrazine in inhibiting antibiotic efflux by P. aeruginosa. In vivo evaluation of the therapeutic efficacy of CAZ-(di-F-Q) combination against P. aeruginosa showed 20% of the mice treated with CAZ-(di-F-Q) survived after 7 days in IMP carbapenemase-producing multidrug-resistant P. aeruginosa infection group while no mice treated with CAZ alone survived after 2 days. Taken together, di-F-Q demonstrated unique strain-specific antimicrobial properties including anti-biofilm and antibiotic-potentiating activity against S. aureus and P. aeruginosa, respectively. Quercetin (Fig. 1) is one of the most famous flavonoids, and it is characterized by broad spectrum biological activity including antioxidant, anti-inflammatory, antiviral, and anticancer effects 1. Quercetin has also been reported to have a potential as an antibacterial agent 1 , and its anti-biofilm activity against clinical isolates of gram-positive bacteria, albeit low 2 , is noteworthy. However, several unfavorable physicochemical properties of quercetin such as low chemical stability limits its pharmaceutical use. Previously, in order to tackle this problem, we prepared 3′,4′-difluoroquercetin (di-F-Q, Fig. 1) through bioisosteric replacement of the catecholic hydroxyl groups of quercetin with fluorine atoms, which showed significantly improved chemical stability as well as anticancer activity compared with quercetin 3. In this context, antibacterial properties of di-F-Q appears worth investigating and, in this study, we attempted to evaluate antibacterial, anti-biofilm, and antibiotic-potentiating activity of di-F-Q. Materials and methods Materials. Dimethyl sulfoxide (DMSO), crystal violet and phosphate buffered saline (PBS) were purchased from Merck (St. Louis, MO, USA). Mueller-Hinton broth (MHB) and tryptic soy broth (TSB) were obtained from BD Biosciences (San Jose, CA, USA) and Fisher Scientific (Pittsburgh, PA, USA), respectively.

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“…The anti-biofilm activities of quercetin in biofilm formation and biofilmrelated infections were also investigated in Streptococcus mutans and Enterococcus faecalis, and results indicated the potential of quercetin in application for antimicrobial infection and anti-caries therapies for human health [50,51]. Furthermore, nanoparticles decorated quercetin and quercetin conjugated microparticles showed more effective anti-biofilm activities [52], opening up a novel approach to develop therapeutic agent in prevention of microbial infections.…”

Section: Quercetinmentioning

confidence: 99%

Developing natural products as potential anti-biofilm agents

et al. 2019

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Biofilm is a natural form of bacterial growth ubiquitously in environmental niches. The biofilm formation results in increased resistance to negative environmental influences including resistance to antibiotics and antimicrobial agents. Quorum sensing (QS) is cell-to-cell communication mechanism, which plays an important role in biofilm development and balances the environment when the bacteria density becomes high. Due to the prominent points of biofilms implicated in infectious disease and the spread of multi-drug resistance, it is urgent to discover new antibacterial agents that can regulate biofilm formation and development. Accumulated evidences demonstrated that natural products from plants had antimicrobial and chemo-preventive properties in modulation of biofilm formation in the last two decades. This review will summarize recent studies on the discovery of natural anti-biofilm agents from plants with clear-cut mechanisms or identified molecular addresses, as well as some herbs with unknown mechanisms or unidentified bioactive ingredients. We also focus on the progression of techniques on the extraction and identification of natural anti-biofilm substances. Besides, anti-biofilm therapeutics undergoing clinical trials are discussed. These newly discovered natural anti-biofilm agents are promising candidates which could provide novel strategies for biofilm-associated infections.

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<i>In Vitro</i> Synergism and Anti-biofilm Activity of Quercetin–Pivaloxymethyl Conjugate against <i>Staphylococcus aureus</i> and <i>Enterococcus</i> Species

Cited by 18 publications

References 15 publications

Quercetin mediated inhibition of Staphylococcus aureus biofilms and the impact of the isolate phenotype and genotype

Quercetin mediated inhibition of Staphylococcus aureus biofilms and the impact of the isolate phenotype and genotype

Strain-specific anti-biofilm and antibiotic-potentiating activity of 3′,4′-difluoroquercetin

Developing natural products as potential anti-biofilm agents

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