Evaluation of isoeugenol in inhibition of Staphylococcus aureus efflux pumps and their toxicity using Drosophila melanogaster model

Júnior, Dárcio Luiz de Sousa; Cordeiro, Paula; Barbosa, Cristina Rodrigues dos Santos; Muniz, Débora Feitosa; Silveira, Zildene de Sousa; Macêdo, Nair Silva; Neto, Luiz Jardelino de Lacerda; Freitas, Thiago Sampaio de; Santos, Joycy Francely Sampaio dos; Coutinho, Henrique Douglas Melo; Oliveira, Lígia Cláudia Castro de; Cunha, Francisco Assis Bezerra da

doi:10.1016/j.lfs.2021.119940

Cited by 6 publications

(3 citation statements)

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“…It is known that the strains SA-K4414 and SA-K4100 of S. aureus express efflux pump [ 75 ] and β-lactamase-mediated resistance mechanisms. Our findings suggest, however, that the QacA/B and QacC efflux pumps, expressed respectively by SA-K4414 and SA-K4100, do not interfere with the activity of β-lactams, considering that the association with these antibiotics caused no significant change in the MIC.…”

Section: Resultsmentioning

confidence: 99%

Efflux Pump (QacA, QacB, and QacC) and β-Lactamase Inhibitors? An Evaluation of 1,8-Naphthyridines against Staphylococcus aureus Strains

et al. 2023

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The bacterial species Staphylococcus aureus presents a variety of resistance mechanisms, among which the expression of β-lactamases and efflux pumps stand out for providing a significant degree of resistance to clinically relevant antibiotics. The 1,8-naphthyridines are nitrogen heterocycles with a broad spectrum of biological activities and, as such, are promising research targets. However, the potential roles of these compounds on bacterial resistance management remain to be better investigated. Therefore, the present study evaluated the antibacterial activity of 1,8-naphthyridine sulfonamides, addressing their ability to act as inhibitors of β-lactamases and efflux pump (QacA/B and QacC) against the strains SA-K4414 and SA-K4100 of S. aureus. All substances were prepared at an initial concentration of 1024 μg/mL, and their minimum inhibitory concentrations (MIC) were determined by the broth microdilution method. Subsequently, their effects on β-lactamase- and efflux pump-mediated antibiotic resistance was evaluated from the reduction of the MIC of ethidium bromide (EtBr) and β-lactam antibiotics, respectively. The 1,8-naphthyridines did not present direct antibacterial activity against the strains SA-K4414 and SA-K4100 of S. aureus. On the other hand, when associated with antibiotics against both strains, the compounds reduced the MIC of EtBr and β-lactam antibiotics, suggesting that they may act by inhibiting β-lactamases and efflux pumps such as QacC and QacA/B. However, further research is required to elucidate the molecular mechanisms underlying these observed effects.

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Section: Resultsmentioning

confidence: 99%

Efflux Pump (QacA, QacB, and QacC) and β-Lactamase Inhibitors? An Evaluation of 1,8-Naphthyridines against Staphylococcus aureus Strains

et al. 2023

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“…Eugenol and isoeugenol caused high larval mortality, dissuaded oviposition of females, and reduced egg hatchability of Tuta absoluta Meyrick (Lepidoptera: Gelechiidae) [ 29 ]. Isoeugenol caused mortality of Drosophila melanogaster Meigen (Diptera; Drosophilidae) and higher volumes of this compound decreased the flying capacity of flies [ 30 ].…”

Section: Resultsmentioning

confidence: 99%

Volatile chemical composition of Octoblepharum albidum Hedw. (Bryophyta) from the Brazilian Amazon

et al. 2022

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Bryophytes have a variety of bioactive compounds that can be used in biotechnological processes. The objective of this study was to know the volatile chemical composition of Octoblepharum albidum Hedw. from the Amazon and investigate its association with possible bioactive effects on insects. The volatile concentrate of O. albidum was obtained by micro-scale simultaneous distillation–extraction and analyzed by gas chromatography coupled to mass spectrometry and the identification of the compounds was based on system libraries and specialized literature. Twelve organic compounds (92.44% of the total) were identified. Hexadecanoic acid, oleic acid, E-isoeugenol, 1-octen-3-ol, and stearic acid were the major compounds. Most of the compounds have already been reported from bryophytes, while others have an unprecedented occurrence in the group. All identified compounds have biological activities reported in the literature and may participate in plant defense mechanisms against insects, causing mortality or developmental inhibition. In this study, we describe for the first time the volatile chemical composition of O. albidum from Brazil and provide evidence that this species is a source of bioactive compounds. The identified compounds have been reported in the literature to cause mortality or affect the biological parameters of insects, what suggests the possibility of their usage in the formulation of bioinsecticides.

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“…This is mainly due to the spread of multidrug-resistant strains that carry resistance mechanisms, such as efflux pumps [41]. This concern has driven the search for compounds that can act in the inhibition of this efflux system or in the potentiation of the antibiotic activity of drugs currently used in the clinic, restoring their bactericidal potential [42,43].…”

Section: Efflux Pumps and Resistancereversing Bioactive Compoundsmentioning

confidence: 99%

Synthesis, spectroscopic characterization, and antibacterial activity of chalcone (2E)‐1‐(3′‐aminophenyl)‐3‐(4‐dimethylaminophenyl)‐prop‐2‐en‐1‐one against multiresistant Staphylococcus aureus carrier of efflux pump mechanisms and β‐lactamase

Silva¹,

Donato²,

Bezerra³

et al. 2023

Fundamemntal Clinical Pharma

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BackgroundThe bacterium Staphylococcus aureus has stood out for presenting a high adaptability, acquiring resistance to multiple drugs. The search for natural or synthetic compounds with antibacterial properties capable of reversing the resistance of S. aureus is the main challenge to be overcome today. Natural products such as chalcones are substances present in the secondary metabolism of plants, presenting important biological activities such as antitumor, antidiabetic, and antimicrobial activity.ObjectivesIn this context, the aim of this work was to synthesize the chalcone (2E)‐1‐(3'‐aminophenyl)‐3‐(4‐dimethylaminophenyl)‐prop‐2‐en‐1‐one with nomenclature CMADMA, confirm its structure by nuclear magnetic resonance (NMR), and evaluate its antibacterial properties.MethodsThe synthesis methodology used was that of Claisen‐Schmidt, and spectroscopic characterization was performed by NMR. For microbiological assays, the broth microdilution methodology was adopted in order to analyze the antibacterial potential of chalcones and to analyze their ability to act as a possible inhibitor of β‐lactamase and efflux pump resistance mechanisms, present in S. aureus strain K4100.ResultsThe results obtained show that CMADMA does not show direct antibacterial activity, expressing a MIC of ≥1024 μg/mL, or on the enzymatic mechanism of β‐lactamase; however, when associated with ethidium bromide in efflux pump inhibition assays, CMADMA showed promising activity by reducing the MIC of the bromide from 64 to 32 μg/mL.ConclusionWe conclude that the chalcone synthesized in this study is a promising substance to combat bacterial resistance, possibly acting in the inhibition of the QacC efflux pump present in S. aureus strain K4100, as evidenced by the reduction in the MIC of ethidium bromide.

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Evaluation of isoeugenol in inhibition of Staphylococcus aureus efflux pumps and their toxicity using Drosophila melanogaster model

Cited by 6 publications

References 48 publications

Efflux Pump (QacA, QacB, and QacC) and β-Lactamase Inhibitors? An Evaluation of 1,8-Naphthyridines against Staphylococcus aureus Strains

Efflux Pump (QacA, QacB, and QacC) and β-Lactamase Inhibitors? An Evaluation of 1,8-Naphthyridines against Staphylococcus aureus Strains

Volatile chemical composition of Octoblepharum albidum Hedw. (Bryophyta) from the Brazilian Amazon

Synthesis, spectroscopic characterization, and antibacterial activity of chalcone (2E)‐1‐(3′‐aminophenyl)‐3‐(4‐dimethylaminophenyl)‐prop‐2‐en‐1‐one against multiresistant Staphylococcus aureus carrier of efflux pump mechanisms and β‐lactamase

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