Effect of terpinolene against the resistant Staphylococcus aureus strain, carrier of the efflux pump QacC and β-lactamase gene, and its toxicity in the Drosophila melanogaster model

Scherf, Jackelyne Roberta; Santos, Cristina Paludo; Freitas, Thiago Sampaio de; Rocha, Janaína Esmeraldo; Macêdo, Nair Silva; Lima, Jessyca Nayara Mascarenhas; Coutinho, Henrique Douglas Melo; Cunha, Francisco Assis Bezerra da

doi:10.1016/j.micpath.2020.104528

Cited by 9 publications

(12 citation statements)

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“…In addition, highly conserved residues Y59 and W62 in TMS 3 were found to be functionally important as substitutions resulted in a significant reduction in the ability of QacC to confer resistance to benzalkonium and other compounds [ 145 ]. The qacC gene [ 130 , 150 ] can be carried on small rolling-circle replicating plasmids [ 151 , 152 ] and large low-copy-number multiresistance plasmids; its promoter is known to differ between these plasmids systems [ 130 ]. QacC expression is not modulated by a transcriptional regulator [ 141 ] and currently there is no high-resolution structure available for QacC protein.…”

Section: Prototypical Characterised Efflux Pumps In Staphylococcimentioning

confidence: 99%

Efflux Pump Mediated Antimicrobial Resistance by Staphylococci in Health-Related Environments: Challenges and the Quest for Inhibition

Dashtbani-Roozbehani

Brown

2021

Antibiotics

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The increasing emergence of antimicrobial resistance in staphylococcal bacteria is a major health threat worldwide due to significant morbidity and mortality resulting from their associated hospital- or community-acquired infections. Dramatic decrease in the discovery of new antibiotics from the pharmaceutical industry coupled with increased use of sanitisers and disinfectants due to the ongoing COVID-19 pandemic can further aggravate the problem of antimicrobial resistance. Staphylococci utilise multiple mechanisms to circumvent the effects of antimicrobials. One of these resistance mechanisms is the export of antimicrobial agents through the activity of membrane-embedded multidrug efflux pump proteins. The use of efflux pump inhibitors in combination with currently approved antimicrobials is a promising strategy to potentiate their clinical efficacy against resistant strains of staphylococci, and simultaneously reduce the selection of resistant mutants. This review presents an overview of the current knowledge of staphylococcal efflux pumps, discusses their clinical impact, and summarises compounds found in the last decade from plant and synthetic origin that have the potential to be used as adjuvants to antibiotic therapy against multidrug resistant staphylococci. Critically, future high-resolution structures of staphylococcal efflux pumps could aid in design and development of safer, more target-specific and highly potent efflux pump inhibitors to progress into clinical use.

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Section: Prototypical Characterised Efflux Pumps In Staphylococcimentioning

confidence: 99%

Efflux Pump Mediated Antimicrobial Resistance by Staphylococci in Health-Related Environments: Challenges and the Quest for Inhibition

Dashtbani-Roozbehani

Brown

2021

Antibiotics

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“…However, Agus [ 107 ] stated that terpinolene is among the most toxic monoterpenes along with α-terpineol and linalool. According to Scherf et al [ 108 ], terpinolene was toxic to Drosophila melanogaster , with an LC 50 of 34.60 μL.L −1 at 12 h of exposure.…”

Section: Resultsmentioning

confidence: 99%

Phytochemical Profile, Preliminary Toxicity, and Antioxidant Capacity of the Essential Oils of Myrciaria floribunda (H. West ex Willd.) O. Berg. and Myrcia sylvatica (G. Mey) DC. (Myrtaceae)

et al. 2022

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The essential oils (EOs) of Myrciaria floribunda (Mflo) and Myrcia sylvatica (Msyl) (Myrtaceae) were obtained by hydrodistillation. The analysis of volatile constituents was performed by GC/MS. Preliminary toxicity was assessed on Artemia salina Leach. The antioxidant capacity was measured by the ABTS•+ and DPPH• radical inhibitory activities. The results indicate that the Mflo EO had the highest yield (1.02%), and its chemical profile was characterized by high levels of hydrocarbon (65.83%) and oxygenated (25.74%) monoterpenes, especially 1,8-cineole (23.30%), terpinolene (22.23%) and α-phellandrene (22.19%). Regarding the Msyl EO, only hydrocarbon (51.60%) and oxygenated (46.52%) sesquiterpenes were identified in the sample, with (Z)-α-trans-bergamotene (24.57%), α-sinensal (13.44%), and (Z)-α-bisabolene (8.33%) at higher levels. The EO of Mflo exhibited moderate toxicity against A. salina (LC50 = 82.96 ± 5.20 µg.mL−1), while the EO of Msyl was classified as highly toxic (LC50 = 2.74 ± 0.50 µg.mL−1). In addition, relative to Trolox, the EOs of Mflo and Msyl showed significant inhibitory effects (p < 0.0001) against the DPPH• radical. This study contributes to the expansion of chemical and biological knowledge on the EOs of Myrtaceae species from the Amazon region.

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“…A recent study carried out with the SA K4100 strain showed positive results regarding the inhibition of β‐lactamase. The study of Scherf et al [13] shows that the association of the compound Terpinolene with the antibiotic Oxacillin reduced the MIC of the antibiotic from 161.26 to 71.83 μg/mL, indicating an antibiotic activity increased by approximately five times, possibly due to the inhibition of β‐lactamase. Several natural and synthetic products have been identified as potential inhibitors of β‐lactamase.…”

Section: Discussionmentioning

confidence: 99%

“…Studies show that plasmids can share more than one type of resistance mechanism, where these mobile genetic elements can transfer to other bacteria genes responsible for cross-resistance to β-lactam antibiotics and quaternary compounds through the dissemination of efflux pump genes [38][39][40] A recent study carried out with the SA K4100 strain showed positive results regarding the inhibition of βlactamase. The study of Scherf et al [13] shows that the association of the compound Terpinolene with the antibiotic Oxacillin reduced the MIC of the antibiotic from 161.26 to 71.83 μg/mL, indicating an antibiotic activity increased by approximately five times, possibly due to the inhibition of β-lactamase. Several natural and synthetic products have been identified as potential inhibitors of β-lactamase.…”

Section: Staphylococcus Aureusmentioning

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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Effect of terpinolene against the resistant Staphylococcus aureus strain, carrier of the efflux pump QacC and β-lactamase gene, and its toxicity in the Drosophila melanogaster model

Cited by 9 publications

References 30 publications

Efflux Pump Mediated Antimicrobial Resistance by Staphylococci in Health-Related Environments: Challenges and the Quest for Inhibition

Efflux Pump Mediated Antimicrobial Resistance by Staphylococci in Health-Related Environments: Challenges and the Quest for Inhibition

Phytochemical Profile, Preliminary Toxicity, and Antioxidant Capacity of the Essential Oils of Myrciaria floribunda (H. West ex Willd.) O. Berg. and Myrcia sylvatica (G. Mey) DC. (Myrtaceae)

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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