Oral bioavailability and pharmacokinetics of esculetin following intravenous and oral administration in rats

Kwak, Jae‐Hwan; Kim, Young-Hwa; Staatz, Christine E.; Baek, In‐hwan

doi:10.1080/00498254.2021.1925774

Cited by 13 publications

(8 citation statements)

References 31 publications

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“…and higher plasma protein binding at about 47 %. The research found that fraxin‘s absolute oral bioavailability may be very low owing to its extended deletion half‐life (t1/2), which was calculated to be 2–3 hours at varied experimental dosages [63] . Multiple studies showed that fraxin is distributed all over the body mostly in the liver, kidneys, and lungs, and has the capacity to pass the blood‐brain barrier [64] .…”

Section: Resultsmentioning

confidence: 99%

“…The research found that fraxin's absolute oral bioavailability may be very low owing to its extended deletion half-life (t1/2), which was calculated to be 2-3 hours at varied experimental dosages. [63] Multiple studies showed that fraxin is distributed all over the body mostly in the liver, kidneys, and lungs, and has the capacity to pass the blood-brain barrier. [64] Fraxin is mainly metabolized in the hepatic tissue of the liver through the operation of the cytochrome P450 enzyme system.…”

Section: Pharmacokineticsmentioning

confidence: 99%

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Pharmacological Activities of Plant‐Derived Fraxin with Molecular Mechanisms: A Comprehensive Review

Ferdous,

Bhuia,

Chowdhury

et al. 2024

Chemistry & Biodiversity

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This study focuses to investigate the pharmacological activities, botanical sources, and biopharmaceutical profile of the phytochemical fraxin based on different preclinical and non‐clinical studies to show the scientific evidence and to evaluate the underlying molecular mechanisms of the therapeutic effects against various ailments. For this, data was searched and collected (as of February 15, 2024) in a variety of credible electronic databases, including PubMed/Medline, Scopus, Springer Link, ScienceDirect, Wiley Online, Web of Science, and Google Scholar. The findings demonstrated favorable outcomes in relation to a range of diseases or medical conditions, including inflammation, neurodegenerative disorders such as cerebral ischemia‐reperfusion (I/R) and depression, viral infection, as well as diabetic nephropathy. The phytochemical also showed protective effects such as osteoprotective, renoprotective, pulmoprotective, hepatoprotective, and gastroprotective effects due to its antioxidant capacity. Fraxin has a great capability to diminish oxidative stress‐related damage in different organs by stimulating the antioxidant enzymes, downregulating nuclear factor kappa B and NLRP3, and triggering the Nrf2/ARE signaling pathways. Fraxin exhibited poor oral bioavailability beacuses of reduced absorption and a wide distribution into tissues of different organs.

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Section: Resultsmentioning

confidence: 99%

Section: Pharmacokineticsmentioning

confidence: 99%

Pharmacological Activities of Plant‐Derived Fraxin with Molecular Mechanisms: A Comprehensive Review

Ferdous,

Bhuia,

Chowdhury

et al. 2024

Chemistry & Biodiversity

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“…It is noteworthy that the halogenation of stilbenes is a quite dangerous way of increasing their bioavailability, since the presence of halogens can cause the appearance of pro-oxidant properties in stilbenes [ 115 ]. The bioavailability of coumarins, for example, of esculetin, is also low and amounts to approximately 19% when taken orally [ 144 , 145 ]. Scopoletin shows even lower bioavailability (approximately 6%) when taken by mouth [ 146 ].…”

Section: Polyphenols As Regulators Of Transcription Factorsmentioning

confidence: 99%

Modulation of redox-sensitive transcription factors with polyphenols as pathogenetically grounded approach in therapy of systemic inflammatory response

Костенко¹,

Akimov²,

Gutnik³

et al. 2023

Heliyon

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“…Moreover, the bioavailability of esculetin in rat plasma was found to be 19% when orally administrated. This research summarizes that there is a need to ameliorate the bioavailability score of esculetin by increasing its absorption [ 121 ]. Likewise, Tsai and colleagues used a microdialysis technique using a microdialysis probe to collect blood from animals receiving esculetin therapy.…”

Section: Detection Pharmacokinetic and Metabolic Studies Of Esculetinmentioning

confidence: 99%

Pharmacological and Therapeutic Applications of Esculetin

Garg

Gupta

Sahu

et al. 2022

IJMS

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Esculetin is a coumarin compound, which belongs to the class of benzopyrone enriched in various plants such as Sonchus grandifolius, Aesculus turbinata, etc. Free radicals lead to the development of oxidative stress causing inflammation, arthritis, cancer, diabetes, fatty liver disease, etc. These further reduce the efficacy of anticancer drugs, activate inflammatory signaling pathways, degrade joints and cartilage, and disrupt the glycemic index and normal function of liver enzymes. For instance, the current treatment modalities used in arthritis such as non-steroidal anti-inflammatory drugs, disease-modifying anti-rheumatoid drugs, and lipoxygenase inhibitors present limited efficacy and adverse effects. Thus, there is a constant need to find newer and safer alternatives. Esculetin has an immense antioxidative potential thereby alleviating arthritis, diabetes, malignancies, and hepatic disorders. Structurally, esculetin contains two hydroxyl groups, which enhance its ability to function as an antioxidant by inhibiting oxidative stress in pathological conditions. Leukotriene B4 synthesis, NF-κB and MPAK pathway activation, and inflammatory cytokine production are the main causes of bone and joint deterioration in arthritis, whereas esculetin treatment reverses these factors and relieves the disease condition. In contrast, lipid peroxidation caused by upregulation of TGF-β-mediated expression and dysfunction of antioxidant enzymes is inhibited by esculetin therapy, thus reducing liver fibrosis by acting on the PI3K/FoxO1 pathway. Therefore, targeting NF-κB, pro-inflammatory cytokines, TGF-β and oxidative stress may be a therapeutic strategy to alleviate arthritis and liver fibrosis.

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Oral bioavailability and pharmacokinetics of esculetin following intravenous and oral administration in rats

Cited by 13 publications

References 31 publications

Pharmacological Activities of Plant‐Derived Fraxin with Molecular Mechanisms: A Comprehensive Review

Pharmacological Activities of Plant‐Derived Fraxin with Molecular Mechanisms: A Comprehensive Review

Modulation of redox-sensitive transcription factors with polyphenols as pathogenetically grounded approach in therapy of systemic inflammatory response

Pharmacological and Therapeutic Applications of Esculetin

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