Identification of absolute conversion to geraldol from fisetin and pharmacokinetics in mouse

Jo, Jun Hyeon; Jo, Jung Jae; Lee, Jae-Mok; Lee, Sangkyu

doi:10.1016/j.jchromb.2016.10.034

Cited by 18 publications

(9 citation statements)

References 13 publications

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“…and 100 and 200 mg/kg (p.o.) in mice ( Jo et al, 2016 ). The oral bioavailability of fisetin was reported 7.8 and 31.7% for oral doses of 100 and 200 mg/kg, respectively.…”

Section: Fisetinmentioning

confidence: 99%

“…The oral bioavailability of fisetin was reported 7.8 and 31.7% for oral doses of 100 and 200 mg/kg, respectively. It was also shown that the Cmax and AUC values for geraldol were more than those of fisetin ( Jo et al, 2016 ). Fisetin and its phase II conjugated forms have been reported to be partly excreted in biliary excretion through P-glycoprotein in rats ( Huang et al, 2018 ) which was assumed due to its 3-OH group and a 2,3-double bond, resulting in high binding affinity to P- glycoprotein ( Huang et al, 2018 ).…”

Section: Fisetinmentioning

confidence: 99%

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The neuroprotective effects of fisetin, a natural flavonoid in neurodegenerative diseases: Focus on the role of oxidative stress

et al. 2022

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Oxidative stress (OS) disrupts the chemical integrity of macromolecules and increases the risk of neurodegenerative diseases. Fisetin is a flavonoid that exhibits potent antioxidant properties and protects the cells against OS. We have viewed the NCBI database, PubMed, Science Direct (Elsevier), Springer-Nature, ResearchGate, and Google Scholar databases to search and collect relevant articles during the preparation of this review. The search keywords are OS, neurodegenerative diseases, fisetin, etc. High level of ROS in the brain tissue decreases ATP levels, and mitochondrial membrane potential and induces lipid peroxidation, chronic inflammation, DNA damage, and apoptosis. The subsequent results are various neuronal diseases. Fisetin is a polyphenolic compound, commonly present in dietary ingredients. The antioxidant properties of this flavonoid diminish oxidative stress, ROS production, neurotoxicity, neuro-inflammation, and neurological disorders. Moreover, it maintains the redox profiles, and mitochondrial functions and inhibits NO production. At the molecular level, fisetin regulates the activity of PI3K/Akt, Nrf2, NF-κB, protein kinase C, and MAPK pathways to prevent OS, inflammatory response, and cytotoxicity. The antioxidant properties of fisetin protect the neural cells from inflammation and apoptotic degeneration. Thus, it can be used in the prevention of neurodegenerative disorders.

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“…and 100 and 200 mg/kg (p.o.) in mice ( Jo et al, 2016 ). The oral bioavailability of fisetin was reported 7.8 and 31.7% for oral doses of 100 and 200 mg/kg, respectively.…”

Section: Fisetinmentioning

confidence: 99%

Section: Fisetinmentioning

confidence: 99%

The neuroprotective effects of fisetin, a natural flavonoid in neurodegenerative diseases: Focus on the role of oxidative stress

et al. 2022

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“…Plasma samples collection: After gavage, blood was obtained from the eye canthus in rats at 0.083, 0.17, 0.5, 1, 2, 4, 6, 9, 12, and 24 h . All plasma samples were combined.…”

Section: Methodsmentioning

confidence: 99%

UHPLC-Q-TOF-MS/MS Method Based on Four-Step Strategy for Metabolism Study of Fisetin in Vitro and in Vivo

Zhang

Yin

Liang

et al. 2017

J. Agric. Food Chem.

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Fisetin has been identified as an anticancer agent with antiangiogenic properties in mice. However, its metabolism in vitro (rat liver microsomes) and in vivo (rats) is presently not characterized. In this study, ultra-high-performance liquid chromatography coupled with hybrid triple quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS) was employed for data acquiring, and a four-step analytical strategy was developed to screen and identify metabolites. First, full-scan was applied, which was dependent on a multiple mass defect filter (MMDF) combined with dynamic background subtraction (DBS). Then PeakView 1.2 and Metabolitepilot 1.5 software were used to load data to seek possible metabolites. Finally, metabolites were identified according to mass measurement and retention time. Moreover, isomers were distinguished based on Clog P parameter. Based on the proposed method, 53 metabolites in vivo and 14 metabolites in vitro were characterized. Moreover, metabolic pathways mainly included oxidation, reduction, hydrogenation, methylation, sulfation, and glucuronidation.

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“…It is important to note that in our studies geraldol appears to be just as effective as fisetin in impacting rRNA biogenesis. Other reports from the literature indicate that geraldol exhibits low cytotoxicity, with no effect on primary cell types [ 14 , 76 ]. Geraldol has been advocated to also be of potential therapeutic value for NMO (Neuromyelitis optica) drug development and may usher a new class of antitumor drugs [ 14 , 77 ].…”

Section: Discussionmentioning

confidence: 99%

Novel role of the dietary flavonoid fisetin in suppressing rRNA biogenesis

Kammerud

Metge

Elhamamsy

et al. 2021

Laboratory Investigation

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The nucleolus of a cell is a critical cellular compartment that is responsible for ribosome biogenesis and plays a central role in tumor progression. Fisetin, a nutraceutical, is a naturally occurring flavonol from the flavonoid group of polyphenols that has anti-cancer effects. Fisetin negatively impacts several signaling pathways that support tumor progression. However, effect of fisetin on the nucleolus and its functions were unknown. We observed that fisetin is able to physically enter the nucleolus. In the nucleolus, RNA polymerase I (RNA Pol I) mediates the biogenesis of ribosomal RNA. Thus, we investigated the impacts of fisetin on the nucleolus. We observed that breast tumor cells treated with fisetin show a 20–30% decreased nucleolar abundance per cell and a 30–60% downregulation of RNA Pol I transcription activity, as well as a 50–70% reduction in nascent rRNA synthesis, depending on the cell line. Our studies show that fisetin negatively influences MAPK/ERK pathway to impair RNA Pol I activity and rRNA biogenesis. Functionally, we demonstrate that fisetin acts synergistically (CI = 0.4) with RNA Pol I inhibitor, BMH-21 and shows a noteworthy negative impact (60% decrease) on lung colonization of breast cancer cells. Overall, our findings highlight the potential of ribosomal RNA (rRNA) biogenesis as a target for secondary prevention and possible treatment of metastatic disease.

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Identification of absolute conversion to geraldol from fisetin and pharmacokinetics in mouse

Cited by 18 publications

References 13 publications

The neuroprotective effects of fisetin, a natural flavonoid in neurodegenerative diseases: Focus on the role of oxidative stress

The neuroprotective effects of fisetin, a natural flavonoid in neurodegenerative diseases: Focus on the role of oxidative stress

UHPLC-Q-TOF-MS/MS Method Based on Four-Step Strategy for Metabolism Study of Fisetin in Vitro and in Vivo

Novel role of the dietary flavonoid fisetin in suppressing rRNA biogenesis

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