ArticlePloS one2013
Properties and molecular determinants of the natural flavone acacetin for blocking hKv4.3 channels.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 30 citations in OpenAlex.
- Acacetin Attenuates Lysophosphatidylcholine-Induced Vascular Smooth Muscle Cell Injury via Sirt1-Nrf2/p62 Signaling Axis.Biomedicines · 2026Article
- Ionic Disorders in Persistent Atrial Fibrillation: Therapeutic Targeting by Plant-Derived Bioactive Compounds.Cardiology research and practice · 2026Review
- Molecular Mechanism Discovery of Acacetin Against Cancers: Insights from Network Pharmacology and Molecular Docking.International journal of molecular sciences · 2025Review
- Acacetin as a natural cardiovascular therapeutic: mechanisms and preclinical evidence.Frontiers in pharmacology · 2025Review
- Acacetin-loaded microemulsion for transdermal delivery: preparation, optimization and evaluation.Pharmaceutical biology · 2023Article
- Acacetin, a Potent Transient Outward Current Blocker, May Be a Novel Therapeutic forCirculation. Genomic and precision medicine · 2022Article
- Acacetin as a Potential Protective Compound against Cardiovascular Diseases.Evidence-based complementary and alternative medicine : eCAM · 2022Review
- Acacetin suppresses the electrocardiographic and arrhythmic manifestations of the J wave syndromes.PloS one · 2020Article
- Recent advances in the treatment of Brugada syndrome.Expert review of cardiovascular therapy · 2018Review
- The Natural Flavone Acacetin Confers Cardiomyocyte Protection Against Hypoxia/Reoxygenation Injury via AMPK-Mediated Activation of Nrf2 Signaling Pathway.Frontiers in pharmacology · 2018Article
- The Natural Flavone Acacetin Blocks Small Conductance CaFrontiers in pharmacology · 2017Article
- Water-soluble acacetin prodrug confers significant cardioprotection against ischemia/reperfusion injury.Scientific reports · 2016Article
- Synthesis of a highly water-soluble acacetin prodrug for treating experimental atrial fibrillation in beagle dogs.Scientific reports · 2016Article
- Acacetin inhibits glutamate release and prevents kainic acid-induced neurotoxicity in rats.PloS one · 2014Article
- Acacetin and chrysin, two polyphenolic compounds, alleviate telomeric position effect in human cells.Molecular therapy. Nucleic acids · 2013Article
Corrections and comments
- Erratum issued
Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The natural flavone acacetin has been demonstrated to inhibit transient outward potassium current (Ito) in human atrial myocytes. However, the molecular determinants of acacetin for blocking Ito are unknown. The present study was designed to investigate the properties and molecular determinants of this compound for blocking hKv4.3 channels (coding Ito) stably expressed in HEK 293 cells using the approaches of whole-cell patch voltage-clamp technique and mutagenesis. It was found that acacetin inhibited hKv4.3 current by binding to both the closed and open channels, and decreased the recovery from inactivation. The blockade of hKv4.3 channels by acacetin was use- and frequency-dependent, and IC50s of acacetin for inhibiting hKv4.3 were 7.9, 6.1, 3.9, and 3.2 µM, respectively, at 0.2, 0.5, 1, and 3.3 Hz. The mutagenesis study revealed that the hKv4.3 mutants T366A and T367A in the P-loop helix, and V392A, I395A and V399A in the S6-segment had a reduced channel blocking efficacy of acacetin (IC50, 44.5 µM for T366A, 25.8 µM for T367A, 17.6 µM for V392A, 16.2 µM for I395A, and 19.1 µM for V399A). These results demonstrate the novel information that acacetin may inhibit the closed channels and block the open state of the channels by binding to their P-loop filter helix and S6 domain. The use- and rate-dependent blocking of hKv4.3 by acacetin is likely beneficial for managing atrial fibrillation.
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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.