ArticlePharmaceutics2021
Investigation of the Factors Responsible for the Poor Oral Bioavailability of Acacetin in Rats: Physicochemical and Biopharmaceutical Aspects.
Article in Pharmaceutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 30 citations in OpenAlex.
- Enhancement of the Anti-Hepatoma Activity of Acacetin Through Salt Formation of Sodium Acacetin.Chemistry & biodiversity · 2026Article
- Effect and Mechanism of Acacetin Against Stress-Induced Gastric Mucosal Damage: Network Pharmacology, Molecular Docking and Experimental Verification.Food science & nutrition · 2026Article
- Influence of Diet on the Bioaccessibility of Active Substances fromMolecules (Basel, Switzerland) · 2025Article
- 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, 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
- Advancing therapeutic efficacy: nanovesicular delivery systems for medicinal plant-based therapeutics.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Metabolomic Profiling and In Vivo Antiepileptic Effect ofMetabolites · 2024Article
- Advances in Flavonoid Research: Sources, Biological Activities, and Developmental Prospectives.Current issues in molecular biology · 2024Review
- Diabetes cardiomyopathy: targeted regulation of mitochondrial dysfunction and therapeutic potential of plant secondary metabolites.Frontiers in pharmacology · 2024Review
- Factors determining the oral absorption and systemic disposition of zeaxanthin in rats:Pharmaceutical biology · 2022Article
- Synthesis and anti-diabetic activity of novel biphenylsulfonamides as glucagon receptor antagonists.Chemical biology & drug design · 2021Article
- TNBC: Potential Targeting of Multiple Receptors for a Therapeutic Breakthrough, Nanomedicine, and Immunotherapy.Biomedicines · 2021Review
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
Abstract
Acacetin, an important ingredient of acacia honey and a component of several medicinal plants, exhibits therapeutic effects such as antioxidative, anticancer, anti-inflammatory, and anti-plasmodial activities. However, to date, studies reporting a systematic investigation of the in vivo fate of orally administered acacetin are limited. Moreover, the in vitro physicochemical and biopharmaceutical properties of acacetin in the gastrointestinal (GI) tract and their pharmacokinetic impacts remain unclear. Therefore, in this study, we aimed to systematically investigate the oral absorption and disposition of acacetin using relevant rat models. Acacetin exhibited poor solubility (≤119 ng/mL) and relatively low stability (27.5-62.0% remaining after 24 h) in pH 7 phosphate buffer and simulated GI fluids. A major portion (97.1%) of the initially injected acacetin dose remained unabsorbed in the jejunal segments, and the oral bioavailability of acacetin was very low at 2.34%. The systemic metabolism of acacetin occurred ubiquitously in various tissues (particularly in the liver, where it occurred most extensively), resulting in very high total plasma clearance of 199 ± 36 mL/min/kg. Collectively, the poor oral bioavailability of acacetin could be attributed mainly to its poor solubility and low GI luminal stability.
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Registered trials
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