Pharmacological activities of allylbenzene and allylanisole phenylpropanoids: Inhibition of antibiotic resistance targets and toxicity profile in a Drosophila melanogaster model

Lopes, Thais Pereira; Barbosa, Cristina Rodrigues dos Santos; Macêdo, Nair Silva; Scherf, Jackelyne Roberta; Santos, Maria Apoliana Costa dos; Freitas, Thiago Sampaio de; Ribeiro-Filho, Jaime; Coutinho, Henrique Douglas Melo; Siyadatpanah, Abolghasem; Wilairatana, Polrat; Cunha, Francisco Assis Bezerra da; Pinheiro, Alysson Pontes

doi:10.1016/j.jksus.2022.101995

Cited by 1 publication

(3 citation statements)

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“…In the studies by Scherf et al [13] and Lopes et al [27], also no activity was shown against the K4100 and K4414 strains of the compounds terpinolene and phenylprapanoid, respectively, showing a MIC of ≥1024 μg/mL in both studies. As in the aforementioned studies, the data found in this work are important, because according to Bhardwaj and Mohanty [32], an ideal pump inhibitor should not exhibit any type of antibacterial activity.…”

Section: Discussionmentioning

confidence: 87%

“…Next, we present data indicating the presence of the enzymatic mechanism β‐lactamase and efflux pump in the K4100 strain of S. aureus . The same assays performed to verify the presence of the resistance mechanisms cited were also performed by Scherf et al [13] and Lopes et al [27].…”

Section: Resultsmentioning

confidence: 99%

“…Lopes et al [27] investigated the inhibitory potential of phenylpropanoids against K4414 strain of S. aureus . The results of their work demonstrate that the phenylpropanoids allylbenzene and allylanisole potentiated the antibiotic activity of Penicillin, reducing the MIC of this drug from 512 to 256 and 128 μg/mL, respectively, thus suggesting that these compounds act as possible inhibitors of this enzymatic mechanism.…”

Section: Discussionmentioning

confidence: 99%

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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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Section: Discussionmentioning

confidence: 87%

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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