An enzyme-linked immunosorbent assay for the measurement of plasma flavonoids in mice fed apigenin-<i>C</i>
-glycoside

Ninfali, Paolino; Dominici, Sabrina; Angelino, Donato; Gennari, Lorenzo; Buondelmonte, Costantina; Giorgi, Luca

doi:10.1002/jsfa.6143

Cited by 7 publications

(6 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Another study using 5.4mg/kg IV apigenin in rats showed a comparatively lower Vd at 2.07 ± 0.14L/kg, and a Vd of its metabolite luteolin at 0.868 ± 0.1L/kg-however both values are still above the TBW of rodents, indicating distribution and accumulation into tissue (Chen et al, 2012;Ninfali et al, 2013). Lipinski's "Rule of Five" points to whether the physical properties of chemical compounds increase their propensity of being orally active drug candidates.…”

Section: Tissue Distribution Of Apigenin After Systemic Uptakementioning

confidence: 95%

“…Following IV administration of 20mg/kg of apigenin in rats, the Vd of apigenin was 15.75 ± 11.73L/kg–much larger than the Total Body Water (TBW) of rodents, at 0.67L/kg ( Wan et al, 2007 ). Another study using 5.4mg/kg IV apigenin in rats showed a comparatively lower Vd at 2.07 ± 0.14L/kg, and a Vd of its metabolite luteolin at 0.868 ± 0.1L/kg–however both values are still above the TBW of rodents, indicating distribution and accumulation into tissue ( Chen et al, 2012 ; Ninfali et al, 2013 ).…”

Section: Current Knowledge and Analysismentioning

confidence: 97%

“…There are differences in rates of clearance between apigenin and its primary metabolite luteolin. Following 5.4mg/kg IV administration of apigenin in rats, the clearance of luteolin was 0.450 ± 0.03L/h/kg ( Chen et al, 2012 ; Ninfali et al, 2013 ). Apigenin clearance was 0.065 ± 0.005L/h/kg ( Chen et al, 2012 ; Ninfali et al, 2013 ).…”

Section: Current Knowledge and Analysismentioning

confidence: 99%

“…Following 5.4mg/kg IV administration of apigenin in rats, the clearance of luteolin was 0.450 ± 0.03L/h/kg ( Chen et al, 2012 ; Ninfali et al, 2013 ). Apigenin clearance was 0.065 ± 0.005L/h/kg ( Chen et al, 2012 ; Ninfali et al, 2013 ). Studies using primary rat hepatocytes suggest this faster rate of elimination for luteolin is likely due to rapid metabolism by phase I metabolism, in addition to phase II metabolism by UGTs, SULTs, and COMT–whereas apigenin is mostly metabolized via UGT and SULTs ( Chen et al, 2012 ; Ninfali et al, 2013 ).…”

Section: Current Knowledge and Analysismentioning

confidence: 99%

See 3 more Smart Citations

Does Oral Apigenin Have Real Potential for a Therapeutic Effect in the Context of Human Gastrointestinal and Other Cancers?

DeRango-Adem

Blay

2021

Front. Pharmacol.

View full text Add to dashboard Cite

Apigenin (4′, 5, 7-trihydroxyflavone) is a plant flavone that has been found to have various actions against cancer cells. We evaluated available evidence to determine whether it is feasible for apigenin to have such effects in human patients.Apigenin taken orally is systemically absorbed and recirculated by enterohepatic and local intestinal pathways. Its bioavailability is in the region of 30%. Once absorbed from the oral route it reaches maximal circulating concentration (Cmax) after a time (Tmax) of 0.5–2.5h, with an elimination half-life (T1/2) averaging 2.52 ± 0.56h.Using a circulating concentration for efficacy of 1–5μmol/L as the target, we evaluated data from both human and rodent pharmacokinetic studies to determine if a therapeutic concentration would be feasible. We find that oral intake of dietary materials would require heroic ingestion amounts and is not feasible. However, use of supplements of semi-purified apigenin in capsule form could reach target blood levels using amounts that are within the range currently acceptable for other supplements and medications. Modified formulations or parenteral injection are suitable but may not be necessary.Further work with direct studies of pharmacokinetics and clinical outcomes are necessary to fully evaluate whether apigenin will contribute to a useful clinical strategy, but given emerging evidence that it may interact beneficially with chemotherapeutic drugs, this is worthy of emphasis. In addition, more effective access to intestinal tissues from the oral route raises the possibility that apigenin may be of particular relevance to gastrointestinal disorders including colorectal cancer.

show abstract

Section: Tissue Distribution Of Apigenin After Systemic Uptakementioning

confidence: 95%

Section: Current Knowledge and Analysismentioning

confidence: 97%

Section: Current Knowledge and Analysismentioning

confidence: 99%

Section: Current Knowledge and Analysismentioning

confidence: 99%

See 2 more Smart Citations

Does Oral Apigenin Have Real Potential for a Therapeutic Effect in the Context of Human Gastrointestinal and Other Cancers?

DeRango-Adem

Blay

2021

Front. Pharmacol.

View full text Add to dashboard Cite

show abstract

“…However, none of these methods is suitable for biological analysis and pharmacokinetic studies. The only reported approach to determine hinokiflavone in plasma is through enzyme‐linked immunosorbent assay (Ninfali et al, ), and no other methods are available to analyze hinokiflavone in a biological matrix because of poor selectivity and low sensitivity. Therefore, in this study, we developed a simple and highly sensitive LC–MS/MS method to determine hinokiflavone in rat plasma.…”

Section: Introductionmentioning

confidence: 99%

Development and validation of an LC–MS/MS method for the determination of hinokiflavone in rat plasma and its application to a pharmacokinetic study

Ruo-Feng

Xiong

Wen

et al. 2016

Biomedical Chromatography

View full text Add to dashboard Cite

Hinokiflavone has drawn a lot of attention for its multiple biological activities. In this study, a sensitive and selective method for determination of hinokiflavone in rat plasma was developed for the first time, using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Amentoflavone was used as an internal standard. Separation was achieved on a Hypersil Gold C column with isocratic elution using methanol-water (65:35, v/v) as mobile phase at a flow rate of 0.3 mL/min. A triple quadrupole mass spectrometer operating in the negative electrospray mode with selected reaction monitoring was used to detect the transitions of m/z 537 → 284 for hinokiflavone and m/z 537 → 375 for IS. The LOQ was 0.9 ng/mL with a linear range of 0.9-1000 ng/mL. The intra- and inter-day accuracy (RE%) ranged from -3.75 to 6.91% and from -9.20 to 2.51% and the intra- and inter-day precision (RSD) was between 0.32-14.11 and 2.85-10.04%. The validated assay was successfully applied to a pharmacokinetic study of hinokiflavone in rats. The half-life of drug elimination at the terminal phase was 6.10 ± 1.86 h, and the area under the plasma concentration-time curve from time zero to the time of last measurable concentration and to infinity values obtained were 2394.42 ± 466.86 and 2541.93 ± 529.85 h ng/mL, respectively.

show abstract

Regulation of gut microbiota and alleviation of DSS-induced colitis by vitexin

Li,

Luo,

Wang

et al. 2023

Eur J Nutr

View full text Add to dashboard Cite

An enzyme-linked immunosorbent assay for the measurement of plasma flavonoids in mice fed apigenin-C -glycoside

Abstract: By using the ELISA, the concentration of apigenin flavonoids and their metabolites can be detected in VOX- or VOR-supplemented animals. The assay represents a useful tool for rapid screening to compare bioavailability of apigenin flavonoids in respect to control animals.

Cited by 7 publications

References 21 publications

Does Oral Apigenin Have Real Potential for a Therapeutic Effect in the Context of Human Gastrointestinal and Other Cancers?

Does Oral Apigenin Have Real Potential for a Therapeutic Effect in the Context of Human Gastrointestinal and Other Cancers?

Development and validation of an LC–MS/MS method for the determination of hinokiflavone in rat plasma and its application to a pharmacokinetic study

Regulation of gut microbiota and alleviation of DSS-induced colitis by vitexin

Contact Info

Product

Resources

About