ArticleScientific reports2016
Synthesis of a highly water-soluble acacetin prodrug for treating experimental atrial fibrillation in beagle dogs.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 49 citations in OpenAlex.
- A Review of the Effects of Herbal Medicines on the Conductance of Ion Channels.Physiological research · 2026Review
- Enhancement of the Anti-Hepatoma Activity of Acacetin Through Salt Formation of Sodium Acacetin.Chemistry & biodiversity · 2026Article
- Acacetin Attenuates Lysophosphatidylcholine-Induced Vascular Smooth Muscle Cell Injury via Sirt1-Nrf2/p62 Signaling Axis.Biomedicines · 2026Article
- Acacetin as a natural cardiovascular therapeutic: mechanisms and preclinical evidence.Frontiers in pharmacology · 2025Review
- Acacetin, a Natural Flavone with Potential in Improving Liver Disease Based on Its Anti-Inflammation, Anti-Cancer, Anti-Infection and Other Effects.Molecules (Basel, Switzerland) · 2024Review
- Protective Effect of Water-Soluble Acacetin Prodrug on APAP-Induced Acute Liver Injury Is Associated with Upregulation of PPARγ and Alleviation of ER Stress.International journal of molecular sciences · 2023Article
- Advances in basic and translational research in atrial fibrillation.Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 2023Review
- Acacetin inhibits invasion, migration and TGF-β1-induced EMT of gastric cancer cells through the PI3K/Akt/Snail pathway.BMC complementary medicine and therapies · 2022Article
- Acacetin as a Potential Protective Compound against Cardiovascular Diseases.Evidence-based complementary and alternative medicine : eCAM · 2022Review
- Research Progress on Natural Products' Therapeutic Effects on Atrial Fibrillation by Regulating Ion Channels.Cardiovascular therapeutics · 2022Review
- Cardiac senescence is alleviated by the natural flavone acacetin via enhancing mitophagy.Aging · 2021Article
- Doxorubicin cardiomyopathy is ameliorated by acacetin via Sirt1-mediated activation of AMPK/Nrf2 signal molecules.Journal of cellular and molecular medicine · 2020Article
- Article
- Acacetin Protects Against High Glucose-Induced Endothelial Cells Injury by Preserving Mitochondrial Function via Activating Sirt1/Sirt3/AMPK Signals.Frontiers in pharmacology · 2020Article
- The Natural Flavone Acacetin Confers Cardiomyocyte Protection Against Hypoxia/Reoxygenation Injury via AMPK-Mediated Activation of Nrf2 Signaling Pathway.Frontiers in pharmacology · 2018Article
- Breast Cancer Resistance Protein and Multidrug Resistance Protein 2 Regulate the Disposition of Acacetin Glucuronides.Pharmaceutical research · 2017Article
- 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
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We previously reported that duodenal administration of the natural flavone acacetin can effectively prevent the induction of experimental atrial fibrillation (AF) in canines; however, it may not be used intravenously to terminate AF due to its poor water-solubility. The present study was to design a water-soluble prodrug of acacetin and investigate its anti-AF effect in beagle dogs. Acacetin prodrug was synthesized by a three-step procedure. Aqueous solubility, bioconversion and anti-AF efficacy of acacetin prodrug were determined with different methodologies. Our results demonstrated that the synthesized phosphate sodium salt of acacetin prodrug had a remarkable increase of aqueous solubility in H2O and clinically acceptable solution (5% glucose or 0.9% NaCl). The acacetin prodrug was effectively converted into acacetin in ex vivo rat plasma and liver microsome, and in vivo beagle dogs. Intravenous infusion of acacetin prodrug (3, 6 and 12 mg/kg) terminated experimental AF without increasing ECG QTc interval in beagle dogs. The intravenous LD50 of acacetin prodrug was 721 mg/kg in mice. Our preclinical study indicates that the synthesized acacetin prodrug is highly water-soluble and safe; it effectively terminates experimental AF in beagle dogs and therefore may be a promising drug candidate for clinical trial to treat patients with acute AF.
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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.