Evaluation of the Activity of Amino Chalcone Against <em>Staphylococcus</em> Strains Harboring Efflux Pumps Article Swipe
Isydório Alves Donato
,
Cristina Rodrigues dos Santos Barbosa
,
Antônio Henrique Bezerra
,
Suieny Rodrigues Bezerra
,
Ray Silva de Almeida
,
Cícera Datiane de Morais Oliveira‐Tintino
,
Isaac Moura Araújo
,
Ewerton Yago de Sousa Rodrigues
,
Maria Yasmin Cândido de Oliveira
,
Francisco Ferdinando Mesquita Cajazeiras
,
Jeferson Luiz Dias
,
Jesyka Macêdo Guedes
,
Jéssica Híade Silva Cristino
,
Emmanuel Silva Marinho
,
Márcia Machado Marinho
,
Hélcio Silva dos Santos
,
Henrique Douglas Melo Coutinho
,
Saulo Relison Tintino
,
Irwin Rose Alencar de Menezes
,
Francisco Assis Bezerra da Cunha
·
YOU?
·
· 2025
· Open Access
·
· DOI: https://doi.org/10.20944/preprints202509.2110.v1
YOU?
·
· 2025
· Open Access
·
· DOI: https://doi.org/10.20944/preprints202509.2110.v1
The emergence of efflux-mediated resistance in Staphylococcus aureus has limited the effectiveness of conventional antibiotics, highlighting the need for novel adjuvant compounds. This study investigated the synthetic chalcone CMA4DMA as a potential modulator of bacterial resistance associated with the NorA efflux pump. In vitro anti-microbial assays showed that CMA4DMA displayed no intrinsic antibacterial effect (MIC ≥ 1024 µg/mL) but significantly reduced the minimum inhibitory concentration of norfloxacin and ethidium bromide in both wild-type SA1199 and NorA-overexpressing SA1199B strains. Fluorescence assays demonstrated increased intracellular accumulation of ethidium bromide without affecting membrane permea-bility, supporting an efflux-inhibitory mechanism. Molecular docking analysis revealed that CMA4DMA binds to the same site as norfloxacin in the NorA protein, engaging in hydrophobic and hydrogen-bond interactions with key residues, consistent with direct inhibition. In silico ADMET predictions indicated favorable oral absorption and distri-bution, though possible rapid metabolism and risks of hepatotoxicity and cardiotoxici-ty warrant caution for further development. Overall, CMA4DMA effectively restored antibiotic susceptibility in resistant S. aureus strains and showed a consistent inhibitory effect when compared with studies involving other efflux systems, reinforcing its po-tential as a promising scaffold for the development of new bacterial resistance modu-lators.
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Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.20944/preprints202509.2110.v1
- https://www.preprints.org/frontend/manuscript/e286b34ac35b612705c7c3c04ecc00f9/download_pub
- OA Status
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- OpenAlex ID
- https://openalex.org/W4414552648
All OpenAlex metadata
Raw OpenAlex JSON
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https://openalex.org/W4414552648Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.20944/preprints202509.2110.v1Digital Object Identifier
- Title
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Evaluation of the Activity of Amino Chalcone Against <em>Staphylococcus</em> Strains Harboring Efflux PumpsWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2025Year of publication
- Publication date
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2025-09-25Full publication date if available
- Authors
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Isydório Alves Donato, Cristina Rodrigues dos Santos Barbosa, Antônio Henrique Bezerra, Suieny Rodrigues Bezerra, Ray Silva de Almeida, Cícera Datiane de Morais Oliveira‐Tintino, Isaac Moura Araújo, Ewerton Yago de Sousa Rodrigues, Maria Yasmin Cândido de Oliveira, Francisco Ferdinando Mesquita Cajazeiras, Jeferson Luiz Dias, Jesyka Macêdo Guedes, Jéssica Híade Silva Cristino, Emmanuel Silva Marinho, Márcia Machado Marinho, Hélcio Silva dos Santos, Henrique Douglas Melo Coutinho, Saulo Relison Tintino, Irwin Rose Alencar de Menezes, Francisco Assis Bezerra da CunhaList of authors in order
- Landing page
-
https://doi.org/10.20944/preprints202509.2110.v1Publisher landing page
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https://www.preprints.org/frontend/manuscript/e286b34ac35b612705c7c3c04ecc00f9/download_pubDirect link to full text PDF
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YesWhether a free full text is available
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greenOpen access status per OpenAlex
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https://www.preprints.org/frontend/manuscript/e286b34ac35b612705c7c3c04ecc00f9/download_pubDirect OA link when available
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| abstract_inverted_index.inhibition. | 124 |
| abstract_inverted_index.norfloxacin | 66, 107 |
| abstract_inverted_index.predictions | 128 |
| abstract_inverted_index.reinforcing | 175 |
| abstract_inverted_index.Fluorescence | 78 |
| abstract_inverted_index.accumulation | 83 |
| abstract_inverted_index.antibiotics, | 14 |
| abstract_inverted_index.conventional | 13 |
| abstract_inverted_index.demonstrated | 80 |
| abstract_inverted_index.development. | 149 |
| abstract_inverted_index.highlighting | 15 |
| abstract_inverted_index.interactions | 117 |
| abstract_inverted_index.investigated | 24 |
| abstract_inverted_index.modu-lators. | 189 |
| abstract_inverted_index.antibacterial | 52 |
| abstract_inverted_index.concentration | 64 |
| abstract_inverted_index.effectiveness | 11 |
| abstract_inverted_index.hydrogen-bond | 116 |
| abstract_inverted_index.intracellular | 82 |
| abstract_inverted_index.significantly | 59 |
| abstract_inverted_index.Staphylococcus | 6 |
| abstract_inverted_index.anti-microbial | 44 |
| abstract_inverted_index.distri-bution, | 134 |
| abstract_inverted_index.hepatotoxicity | 142 |
| abstract_inverted_index.permea-bility, | 90 |
| abstract_inverted_index.susceptibility | 155 |
| abstract_inverted_index.cardiotoxici-ty | 144 |
| abstract_inverted_index.efflux-mediated | 3 |
| abstract_inverted_index.efflux-inhibitory | 93 |
| abstract_inverted_index.NorA-overexpressing | 75 |
| cited_by_percentile_year | |
| countries_distinct_count | 0 |
| institutions_distinct_count | 20 |
| citation_normalized_percentile.value | 0.57089597 |
| citation_normalized_percentile.is_in_top_1_percent | False |
| citation_normalized_percentile.is_in_top_10_percent | False |