ArticleBritish journal of pharmacology2012
Apigenin, a plant-derived flavone, activates transient receptor potential vanilloid 4 cation channel.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 70 citations in OpenAlex.
- The effects of high-intensity interval training and Iranian propolis extract on serum levels of TRPV4 and CYP2E1 proteins in patients with nonalcoholic fatty liver.La Tunisie medicale · 2024Trial
- Avicularin and Senegenin Suppress TRPV3-Associated TSLP Expression in Human Keratinocytes.Cells · 2026Article
- Discovery of a novel cannabidiol-derived transient receptor potential vanilloid 4 inhibitor to reduce pulmonary edema and lung vascular permeability in mice.Cellular & molecular biology letters · 2026Article
- A pathway to next-generation mast cell stabilizers identified through the novel Phytomedical Analytics for Research Optimization at scale data platform.Frontiers in pharmacology · 2026Article
- A pathway to next-generation mast cell stabilizers identified through the novel Phytomedical Analytics for Research Optimization at Scale data platform.bioRxiv : the preprint server for biology · 2025Article
- Review
- TMAO Impairs Mouse Aortic Vasodilation by Inhibiting TRPV4 Channels in Endothelial Cells.Journal of cardiovascular translational research · 2024Article
- Recent advances on the structure and the function relationships of the TRPV4 ion channel.Channels (Austin, Tex.) · 2024Review
- Identification and Properties of TRPV4 Mutant Channels Present in Polycystic Kidney Disease Patients.Function (Oxford, England) · 2024Article
- Role of transient receptor potential channels in the regulation of vascular tone.Drug discovery today · 2024Review
- Kinin BPharmaceutics · 2023Article
- Unconventional interactions of the TRPV4 ion channel with beta-adrenergic receptor ligands.Life science alliance · 2023Article
- The role of endothelial TRP channels in age-related vascular cognitive impairment and dementia.Frontiers in aging neuroscience · 2023Review
- Genetic- and diet-induced ω-3 fatty acid enrichment enhances TRPV4-mediated vasodilation in mice.Cell reports · 2022Article
- Physiological and Pathological Significance of Esophageal TRP Channels: Special Focus on TRPV4 in Esophageal Epithelial Cells.International journal of molecular sciences · 2022Review
- Identification and functional analysis of a biflavone as a novel inhibitor of transient receptor potential vanilloid 4-dependent atherogenic processes.Scientific reports · 2021Article
- Secondary Metabolites of Plants as Modulators of Endothelium Functions.International journal of molecular sciences · 2021Review
- Transient receptor potential vanilloid 4 channels as therapeutic targets in diabetes and diabetes-related complications.Journal of diabetes investigation · 2020Review
- TRPV4: A Physio and Pathophysiologically Significant Ion Channel.International journal of molecular sciences · 2020Review
- Role of Transient Receptor Potential Vanilloid 4 Channel in Skin Physiology and Pathology.Sultan Qaboos University medical journal · 2020Review
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeTransient receptor potential vanilloid 4 (TRPV4) is a Ca(2+) -permeable channel with multiple modes of activation. Apigenin is a plant-derived flavone, which has potential preventive effects on the development of cardiovascular disease. We set out to explore the effects of apigenin on TRPV4 channel activity and its role in vasodilatation. EXPERIMENTAL APPROACH: The effects of apigenin (0.01-30 µM) on TPRV4 channels were investigated in HEK293 cells over-expressing TRPV4, rat primary cultured mesenteric artery endothelial cells (MAECs) and isolated small mesenteric arterial segments using whole-cell patch clamp, fluorescent Ca(2+) imaging, intracellular recording and pressure myography. KEY
resultsWhole-cell patch clamp and fluorescent Ca(2+) imaging in HEK cells over-expressing TRPV4 showed that apigenin concentration-dependently stimulated the TRPV4-mediated cation current and Ca(2+) influx. In MAECs, apigenin stimulated Ca(2+) influx in a concentration-dependent manner. These increases in cation current and Ca(2+) influx were markedly inhibited by TRPV4-specific blockers and siRNAs. Furthermore, pressure myography and intracellular recording in small third-order mesenteric arteries showed that apigenin dose-dependently evoked smooth muscle cell membrane hyperpolarization and subsequent vascular dilatation, which were significantly inhibited by TRPV4-specific blockers. TRPV4 blocker or charybdotoxin (200 nM) plus apamin (100 nM) diminished the apigenin-induced dilatation. CONCLUSION AND IMPLICATIONS: This is the first study to demonstrate the selective stimulation of TRPV4 by apigenin. Apigenin was found to activate TRPV4 channels in a dose-dependent manner in HEK cells over-expressing TRPV4 and in native endothelial cells. In rat small mesenteric arteries, apigenin acts on TRPV4 in endothelial cells to induce EDHF-mediated vascular dilatation.
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Registered trials
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.