In vitro e in silico evaluation of the inhibition of Staphylococcus aureus efflux pumps by caffeic and gallic acid

Santos, Joycy Francely Sampaio dos; Tintino, Saulo Relison; Freitas, Thiago S.; Campina, Fábia F.; Menezes, Irwin Rose de Alencar; Siqueira-Júnior, José P.; Coutinho, Henrique Douglas Melo; Cunha, Francisco Assis Bezerra da

doi:10.1016/j.cimid.2018.03.001

Cited by 88 publications

(32 citation statements)

References 64 publications

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“…Berberine is a plant alkaloid and has efflux pump inhibitor (EPI) property against the S. aureus NorA, but it was able to intercalate with DNA interfering with the fluorescence of EtBr [ 45 ]. Similar phenomenon has been reported by Dos Santos et al [ 46 ] in that phenolic compounds caffeic acid and gallic acid could inhibit the drug efflux in S. aureus , and they could interfere with the fluorescent of EtBr by intercalating with DNA.…”

Section: Resultssupporting

confidence: 86%

Determination of Drug Efflux Pump Efficiency in Drug-Resistant Bacteria Using MALDI-TOF MS

Lin

Hsu

et al. 2020

Antibiotics

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Multidrug efflux pumps play an essential role in antibiotic resistance. The conventional methods, including minimum inhibitory concentration and fluorescent assays, to monitor transporter efflux activity might have some drawbacks, such as indirect evidence or interference from color molecules. In this study, MALDI-TOF MS use was explored for monitoring drug efflux by a multidrug transporter, and the results were compared for validation with the data from conventional methods. Minimum inhibitory concentration was used first to evaluate the activity of Escherichia coli drug transporter AcrB, and this analysis showed that the E. coli overexpressing AcrB exhibited elevated resistance to various antibiotics and dyes. Fluorescence-based studies indicated that AcrB in E. coli could decrease the accumulation of intracellular dyes and display various efflux rate constants for different dyes, suggesting AcrB’s efflux activity. The MALDI-TOF MS analysis parameters were optimized to maintain a detection accuracy for AcrB’s substrates; furthermore, the MS data showed that E. coli overexpressing AcrB led to increased ions abundancy of various dyes and drugs in the extracellular space at different rates over time, illustrating continuous substrate efflux by AcrB. This study concluded that MALDI-TOF MS is a reliable method that can rapidly determine the drug pump efflux activity for various substrates.

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Section: Resultssupporting

confidence: 86%

Determination of Drug Efflux Pump Efficiency in Drug-Resistant Bacteria Using MALDI-TOF MS

Lin

Hsu

et al. 2020

Antibiotics

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“…Linoleic acid isolated from ethanolic extracts of Portulaca oleracea showed efflux inhibitory potential at 64 mg L −1 concentration, equivalent to reserpine when quantified against MRSA (RN4220/pUL5054: erythromycin resistant, over-expressing MsrA ABC EP, Chan et al, 2015). In search of the drug-resistance reversal agents, dos Santos et al (2018) assessed caffeic acid and gallic acid against four strains of S. aureus ; 1199 as a wild type strain, 1199B as NorA harboring fluroquinolone resistant, IS-58 possessing TetK pump and RN4220 possessing MrsA pump. The study confirmed caffeic acid as a potent AMR-reversal agent, as it effectively inhibited MrsA and NorA EPs from S. aureus strains RN4220 and 1190B, respectively (dos Santos et al, 2018).…”

Section: Phytotherapeutics–the Potent Efflux Pump Inhibitorsmentioning

confidence: 99%

“…In search of the drug-resistance reversal agents, dos Santos et al (2018) assessed caffeic acid and gallic acid against four strains of S. aureus ; 1199 as a wild type strain, 1199B as NorA harboring fluroquinolone resistant, IS-58 possessing TetK pump and RN4220 possessing MrsA pump. The study confirmed caffeic acid as a potent AMR-reversal agent, as it effectively inhibited MrsA and NorA EPs from S. aureus strains RN4220 and 1190B, respectively (dos Santos et al, 2018). In another interesting study, Kakarla et al (2016) reported LmrS inhibitory activities of Cuminum cyminum .…”

Section: Phytotherapeutics–the Potent Efflux Pump Inhibitorsmentioning

confidence: 99%

Inhibiting Bacterial Drug Efflux Pumps via Phyto-Therapeutics to Combat Threatening Antimicrobial Resistance

et al. 2018

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Antibiotics, once considered the lifeline for treating bacterial infections, are under threat due to the emergence of threatening antimicrobial resistance (AMR). These drug-resistant microbes (or superbugs) are non-responsive to most of the commonly used antibiotics leaving us with few treatment options and escalating mortality-rates and treatment costs. The problem is further aggravated by the drying-pipeline of new and potent antibiotics effective particularly against the drug-resistant strains. Multidrug efflux pumps (EPs) are established as principal determinants of AMR, extruding multiple antibiotics out of the cell, mostly in non-specific manner and have therefore emerged as potent drug-targets for combating AMR. Plants being the reservoir of bioactive compounds can serve as a source of potent EP inhibitors (EPIs). The phyto-therapeutics with noteworthy drug-resistance-reversal or re-sensitizing activities may prove significant for reviving the otherwise fading antibiotics arsenal and making this combination-therapy effective. Contemporary attempts to potentiate the antibiotics with plant extracts and pure phytomolecules have gained momentum though with relatively less success against Gram-negative bacteria. Plant-based EPIs hold promise as potent drug-leads to combat the EPI-mediated AMR. This review presents an account of major bacterial multidrug EPs, their roles in imparting AMR, effective strategies for inhibiting drug EPs with phytomolecules, and current account of research on developing novel and potent plant-based EPIs for reversing their AMR characteristics. Recent developments including emergence of in silico tools, major success stories, challenges and future prospects are also discussed.

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“…Caffeic acid can be found in many plant products: coffee beverages, argan oil, oats, wheat, rice, and olive oil [ 3 , 23 ]. It has been reported that CA showed antimicrobial potential and/or synergistic effects with antibiotics against S. aureus, S. epidermidis, K. pneumoniae, S. marcescens, P. mirabilis, E. coli, P. aeruginosa, B. cereus, M. luteus, L. monocytogenes, and C. albicans strains [ 20 , 24 – 27 ].…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial Potential of Caffeic Acid againstStaphylococcus aureusClinical Strains

Kępa

Miklasińska-Majdanik

Wojtyczka

et al. 2018

BioMed Research International

146

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Phenolic compounds constitute one of the most promising and ubiquitous groups with many biological activities. Synergistic interactions between natural phenolic compounds and antibiotics could offer a desired alternative approach to the therapies against multidrug-resistant bacteria. The objective of the presented study was to assess the antibacterial potential of caffeic acid (CA) alone and in antibiotic-phytochemical combination against Staphylococcus aureus reference and clinical strains isolated from infected wounds. The caffeic acid tested in the presented study showed diverse effects on S. aureus strains with the minimum inhibitory concentration (MIC) varied from 256 μg/mL to 1024 μg/mL. The supplementation of Mueller-Hinton agar (MHA) with 1/4 MIC of CA resulted in augmented antibacterial effect of erythromycin, clindamycin, and cefoxitin and to the lesser extent of vancomycin. The observed antimicrobial action of CA seemed to be rather strain than antibiotic dependent. Our data support the notion that CA alone exerts antibacterial activity against S. aureus clinical strains and has capacity to potentiate antimicrobial effect in combination with antibiotics. The synergy between CA and antibiotics demonstrates its potential as a novel antibacterial tool which could improve the treatment of intractable infections caused by multidrug-resistant strains.

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In vitro e in silico evaluation of the inhibition of Staphylococcus aureus efflux pumps by caffeic and gallic acid

Cited by 88 publications

References 64 publications

Determination of Drug Efflux Pump Efficiency in Drug-Resistant Bacteria Using MALDI-TOF MS

Determination of Drug Efflux Pump Efficiency in Drug-Resistant Bacteria Using MALDI-TOF MS

Inhibiting Bacterial Drug Efflux Pumps via Phyto-Therapeutics to Combat Threatening Antimicrobial Resistance

Antimicrobial Potential of Caffeic Acid againstStaphylococcus aureusClinical Strains

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