Evidence map›Paper›PMID 39204085›Full record

ArticlePharmaceuticals (Basel, Switzerland)2024

Differential Interactions of Flavonoids with the Aryl Hydrocarbon Receptor In Silico and Their Impact on Receptor Activity In Vitro.

Monique Reis de Santana, Ylanna Bonfim Dos Santos, Késsia Souza Santos, Manoelito Coelho Santos Junior, Mauricio Moraes Victor, Gabriel Dos Santos Ramos, Ravena Pereira do Nascimento, Silvia Lima Costa

Abstract read
In one paragraph

Article in Pharmaceuticals (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

6 citing papers in PubMed.

  1. Review
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Monique Reis de SantanaLaboratory of Neurochemistry and Cellular Biology, Institute of Health Sciences, Federal University of Bahia, Salvador 40231-300, Brazil.
Ylanna Bonfim Dos SantosMolecular Modeling Laboratory, Department of Health, State University of Feira de Santana, Feira de Santana 44036-900, Brazil.ORCID 0000-0002-1937-9642
Késsia Souza SantosMolecular Modeling Laboratory, Department of Health, State University of Feira de Santana, Feira de Santana 44036-900, Brazil.ORCID 0009-0001-5157-6638
Manoelito Coelho Santos JuniorMolecular Modeling Laboratory, Department of Health, State University of Feira de Santana, Feira de Santana 44036-900, Brazil.ORCID 0000-0002-3271-3529
Mauricio Moraes VictorDepartment of Organic Chemistry, Institute of Chemistry, Federal University of Bahia, Salvador 40231-300, Brazil.ORCID 0000-0003-1236-1973
Gabriel Dos Santos RamosDepartment of Organic Chemistry, Institute of Chemistry, Federal University of Bahia, Salvador 40231-300, Brazil.
Ravena Pereira do NascimentoLaboratory of Neurochemistry and Cellular Biology, Institute of Health Sciences, Federal University of Bahia, Salvador 40231-300, Brazil.ORCID 0000-0002-2915-3030
Silvia Lima CostaLaboratory of Neurochemistry and Cellular Biology, Institute of Health Sciences, Federal University of Bahia, Salvador 40231-300, Brazil.ORCID 0000-0002-8975-3871

Funding

Coordenação de Aperfeicoamento de Pessoal de Nível Superior 88887.517844/2020-00National Council for Scientific and Technological Development 312388/2021-7National Council for Scientific and Technological Development National Institute for Translational Neuroscience
6 · The paper itself

Abstract

The molecular mechanisms underlying the observed anticancer effects of flavonoids remain unclear. Increasing evidence shows that the aryl hydrocarbon receptor (AHR) plays a crucial role in neoplastic disease progression, establishing it as a potential drug target. This study evaluated the potential of hydroxy flavonoids, known for their anticancer properties, to interact with AHR, both in silico and in vitro, aiming to understand the mechanisms of action and identify selective AHR modulators. A PAS-B domain homology model was constructed to evaluate in silico interactions of chrysin, naringenin, quercetin apigenin and agathisflavone. The EROD activity assay measured the effects of flavonoids on AHR's activity in human breast cancer cells (MCF7). Simulations showed that chrysin, apigenin, naringenin, and quercetin have the highest AHR binding affinity scores (-13.14 to -15.31), while agathisflavone showed low scores (-0.57 and -5.14). All tested flavonoids had the potential to inhibit AHR activity in a dose-dependent manner in the presence of an agonist (TCDD) in vitro. This study elucidates the distinct modulatory effects of flavonoids on AHR, emphasizing naringenin's newly described antagonistic potential. It underscores the importance of understanding flavonoid's molecular mechanisms, which is crucial for developing novel cancer therapies based on these molecules.

Indexed as

AHRantagonistcancer therapynaringeninpolyphenolsTCDD

Identifiers

PMID39204085
PMCPMC11356971

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.