Rapid and sensitive LC-MS/MS method for the determination of auraptene in rat plasma and its application in a pharmacokinetic and bioavailability study in rats

Ye, X D; Ouyang, Hui; Zhong, Lei; Li, T E; Rao, Xiao-Yong; Feng, Yi; Yang, Wuliang

doi:10.4238/gmr.15028786

Cited by 7 publications

(5 citation statements)

References 4 publications

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“…After auraptene (100 mg/kg, p.o.) administration to rats, the maximum plasma concentration was previously reported to be 1.72 ± 0.38 µg/mL [ 26 ]. As the content of auraptene in CHEP was 80%, its maximum plasma concentration after administration of 300 mg/kg/day p.o., was supposed to be 5.16 µg/mL in our in vivo study.…”

Section: Discussionmentioning

confidence: 99%

Citrus hassaku Extract Powder Increases Mitochondrial Content and Oxidative Muscle Fibers by Upregulation of PGC-1α in Skeletal Muscle

et al. 2021

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Peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) is expressed in skeletal muscles and regulates systemic metabolism. Thus, nutraceuticals targeting skeletal muscle PGC-1α have attracted attention to modulate systemic metabolism. As auraptene contained in citrus fruits promotes lipid metabolism and improves mitochondrial respiration, it could increase mitochondrial function through PGC-1α. Therefore, we hypothesized that PGC-1α is activated by auraptene and investigated its effect using Citrus hassaku extract powder (CHEP) containing >80% of auraptene. C2C12 myotubes were incubated with vehicle or CHEP for 24 h; C57BL/6J mice were fed a control diet or a 0.25% (w/w) CHEP-containing diet for 5 weeks. PGC-1α protein level and mitochondrial content increased following CHEP treatment in cultured myotubes and skeletal muscles. In addition, the number of oxidative fibers increased in CHEP-fed mice. These findings suggest that CHEP-mediated PGC-1α upregulation induced mitochondrial biogenesis and fiber transformation to oxidative fibers. Furthermore, as CHEP increased the expression of the protein sirtuin 3 and of phosphorylated AMP-activated protein kinase (AMPK) and the transcriptional activity of PGC-1α, these molecules might be involved in CHEP-induced effects in skeletal muscles. Collectively, our findings indicate that CHEP mediates PGC-1α expression in skeletal muscles and may serve as a dietary supplement to prevent metabolic disorders.

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Section: Discussionmentioning

confidence: 99%

Citrus hassaku Extract Powder Increases Mitochondrial Content and Oxidative Muscle Fibers by Upregulation of PGC-1α in Skeletal Muscle

et al. 2021

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“…Thus, oral administration of osthenol to ICR mice at a dose of 5 mg/kg and 20 mg/kg resulted in the following PK parameters: C max of 66.1 ± 3.2 and 56.0 ± 29.1 ng/mL, respectively, and T max of 36.3 ± 13.8 and 6.3 ± 1.3 min, respectively, indicating the very low bioavailability of the compound as well as its non-linear pharmacokinetics [22]. Oral administration of auraptene to rats at a dose of 100 mg/kg provided the maximum concentration of the compound in blood plasma of 1719 ± 384.3 ng/mL and T max of 108.0 ± 25.3 min, and the bioavailability of auraptene was determined to be 8.5% [23]. Taking into account the data mentioned above, we suppose that the agent K-142 can be metabolized rapidly after administration to animals and metabolized in the first pass, and the search for metabolites of K-142 will be the objective of our next studies.…”

Section: Pharmacokinetics Study Of K-142 After Oral Administration To...mentioning

confidence: 99%

Stability Study, Quantification Method and Pharmacokinetics Investigation of a Coumarin–Monoterpene Conjugate Possessing Antiviral Properties against Respiratory Syncytial Virus

et al. 2022

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The stability of a new coumarin derivative, agent K-142, bearing α-pinene residue and possessing antiviral activity against respiratory syncytial virus (RSV) was studied in whole mice blood in vitro, and a method for its quantification in this matrix was developed and validated. The sample preparation method was precipitation of whole blood with a mixture of 0.2 M ZnSO4 with MeOH (2:8 v/v) containing 2-adamantylamine hydrochloride as an internal standard (IS). Analysis was carried out by HPLC-MS/MS using reversed phase chromatography and a triple quadrupole mass spectrometer 6500 QTRAP (SCIEX) in multiple reaction monitoring (MRM) mode. The transitions 351.2 → 217.1 Da and 152.2 → 93.1/107.2 Da were monitored for K-142 and the IS, respectively. The method was validated in terms of selectivity, calibration curve, LLOQ, accuracy and precision, stability, recovery and carry over. The developed method was used for a pharmacokinetics study of the compound after its oral administration to mice at a dose of 20 mg/kg.

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“…Ye et al determined the pharmacokinetics of auraptene in rat plasma using LC-MS/MS method. Data showed that a dose range of 0.5–200 ng/ml of auraptene was safe and bioavailability of oral administration of auraptene was merely 8.5% in rats ( Ye et al, 2016 ). In another study, the absorption and metabolism of auraptene in rodent models was examined.…”

Section: Pharmacokinetics Of Auraptenementioning

confidence: 99%

A Review of Auraptene as an Anticancer Agent

2021

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Auraptene is a bioactive monoterpene coumarin isolated from Citrus aurantium and Aegle marmelos that belong to the Rutaceae family. Auraptene can modulate intracellular signaling pathways that control cell growth, inflammation and apoptosis and can exert pharmacological properties such as anti-bacterial, anti-fungal, antileishmania and anti-oxidant activity. Auraptene had inhibitory and chemo-preventive effects on the proliferation, tumorigenesis and growth of several cancer cell lines through increase in the activity of glutathione S-transferase, formation of DNA adducts and reduction of the number of aberrant crypt foci. Auraptene exhibits anticancer effects via targeting different cell signaling pathways such as cytokines, genes modulating cellular proliferation, growth factors, transcription factors and apoptosis. The present review is a detailed survey of scientific researches on the cytotoxicity and anticancer activity of Auraptene on cancer cells and tumor bearing animals.

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Rapid and sensitive LC-MS/MS method for the determination of auraptene in rat plasma and its application in a pharmacokinetic and bioavailability study in rats

Cited by 7 publications

References 4 publications

Citrus hassaku Extract Powder Increases Mitochondrial Content and Oxidative Muscle Fibers by Upregulation of PGC-1α in Skeletal Muscle

Citrus hassaku Extract Powder Increases Mitochondrial Content and Oxidative Muscle Fibers by Upregulation of PGC-1α in Skeletal Muscle

Stability Study, Quantification Method and Pharmacokinetics Investigation of a Coumarin–Monoterpene Conjugate Possessing Antiviral Properties against Respiratory Syncytial Virus

A Review of Auraptene as an Anticancer Agent

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