ArticleBiochemical pharmacology2021
Discovery of a AHR pelargonidin agonist that counter-regulates Ace2 expression and attenuates ACE2-SARS-CoV-2 interaction.
Article in Biochemical pharmacology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers, 1 of them a synthesis that pooled it.
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Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.
- Promising Antiviral Activities of Natural Flavonoids against SARS-CoV-2 Targets: Systematic Review.International journal of molecular sciences · 2021Pooled it
- NF-κB in Drug Discovery: Still an Elusive Target.Recent advances in inflammation & allergy drug discovery · 2026Article
- Prenylation of Flavanones by an Aromatic Prenyltransferase fromMolecules (Basel, Switzerland) · 2025Article
- Bile acids and their receptors in hepatic immunity.Liver research (Beijing, China) · 2025Review
- The role of aryl hydrocarbon receptor signalling in COVID-19 pathology and its therapeutic potential.Frontiers in molecular medicine · 2025Review
- Colloidal Aggregation Confounds Cell-Based Covid-19 Antiviral Screens.Journal of medicinal chemistry · 2024Article
- Role of aryl hydrocarbon receptors in infection and inflammation.Frontiers in immunology · 2024Review
- Colloidal aggregation confounds cell-based Covid-19 antiviral screens.bioRxiv : the preprint server for biology · 2023Article
- Article
- The Development of Pharmacophore Models for the Search of New Natural Inhibitors of SARS-CoV-2 Spike RBD-ACE2 Binding Interface.Molecules (Basel, Switzerland) · 2022Article
- Exploring the Relationship between G-Quadruplex Nucleic Acids and Plants: From Plant G-Quadruplex Function to Phytochemical G4 Ligands with Pharmaceutic Potential.Pharmaceutics · 2022Review
- Gut-brain communication in COVID-19: molecular mechanisms, mediators, biomarkers, and therapeutics.Expert review of clinical immunology · 2022Article
- Factors Modulating COVID-19: A Mechanistic Understanding Based on the Adverse Outcome Pathway Framework.Journal of clinical medicine · 2022Review
- GLP-1 Mediates Regulation of Colonic ACE2 Expression by the Bile Acid Receptor GPBAR1 in Inflammation.Cells · 2022Article
- Different compounds against Angiotensin-Converting Enzyme 2 (ACE2) receptor potentially containing the infectivity of SARS-CoV-2: an in silico study.Journal of molecular modeling · 2022Article
- Real-World Evidence for COVID-19 Delta Variant's Effects on the Digestive System and Protection of Inactivated Vaccines from a Medical Center in Yangzhou, China: A Retrospective Observational Study.International journal of clinical practice · 2022Observational
- Therapeutic Potential of Glycosyl Flavonoids as Anti-Coronaviral Agents.Pharmaceuticals (Basel, Switzerland) · 2021Review
Corrections and comments
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Authors and funding
16 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The severe acute respiratory syndrome (SARS)-CoV-2 is the pathogenetic agent of Corona Virus Induced Disease (COVID)19. The virus enters the human cells after binding to the angiotensin converting enzyme (ACE)2 receptor in target tissues. ACE2 expression is induced in response to inflammation. The colon expression of ACE2 is upregulated in patients with inflammatory bowel disease (IBD), highlighting a potential risk of intestinal inflammation in promoting viral entry in the human body. Because mechanisms that regulate ACE2 expression in the intestine are poorly understood and there is a need of anti-SARS-CoV-2 therapies, we have settled to investigate whether natural flavonoids might regulate the expression of Ace2 in intestinal models of inflammation. The results of these studies demonstrated that pelargonidin activates the Aryl hydrocarbon Receptor (AHR) in vitro and reverses intestinal inflammation caused by chronic exposure to high fat diet or to the intestinal braking-barrier agent TNBS in a AhR-dependent manner. In these two models, development of colon inflammation associated with upregulation of Ace2 mRNA expression. Colon levels of Ace2 mRNA were directly correlated with Tnf-α mRNA levels. Molecular docking studies suggested that pelargonidin binds a fatty acid binding pocket on the receptor binding domain of SARS-CoV-2 Spike protein. In vitro studies demonstrated that pelargonidin significantly reduces the binding of SARS-CoV-2 Spike protein to ACE2 and reduces the SARS-CoV-2 replication in a concentration-dependent manner. In summary, we have provided evidence that a natural flavonoid might hold potential in reducing intestinal inflammation and ACE2 induction in the inflamed colon in a AhR-dependent manner.
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