Pharmacokinetics and Modeling of Quercetin and Metabolites

Chen, Xiao; Yin, Ophelia; Zuo, Zhong; Chow, Moses S.S.

doi:10.1007/s11095-005-4584-1

Cited by 189 publications

(109 citation statements)

References 28 publications

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“…Of critical importance is an understanding of quercetin bioavailability and metabolism within a biological organism. The current hypothesis would suggest that both the liver and small intestine participate in the metabolism of quercetin (8,14,26,33). KO animals are characterized by an ϳ90% reduction in bile acid synthesis and secretion (12).…”

Section: Discussionmentioning

confidence: 94%

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Hepatic cytochrome P-450 reductase-null mice show reduced transcriptional response to quercetin and reveal physiological homeostasis between jejunum and liver

Mutch¹,

Crespy²,

Clough³

et al. 2006

American Journal of Physiology-Gastrointestinal and Liver Physi

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P-450reductase-null mice show reduced transcriptional response to quercetin and reveal physiological homeostasis between jejunum and liver. Am J Physiol Gastrointest Liver Physiol 290: G63-G72, 2006. First published February 2, 2006 doi:10.1152/ajpgi.00565.2005.-Using mice deficient in hepatic cytochrome P-450 oxidoreductase (POR), which disables the liver cytochrome P-450 system, we examined the metabolism and biological response of the anticarcinogenic flavonoid, quercetin. Profiling circulating metabolites revealed similar profiles over 72 h in wild-type (WT) and POR-null (KO) mice, showing that hepatic P450 and reduced biliary secretion do not affect quercetin metabolism. Transcriptional profiling at 24 h revealed that two-to threefold more genes responded significantly to quercetin in WT compared with KO in the jejunum, ileum, colon, and liver, suggesting that hepatic P450s mediate many of the biological effects of quercetin, such as immune function, estrogen receptor signaling, and lipid, glutathione, purine, and amino acid metabolism, even though quercetin metabolism is not modified. The functional interpretation of expression data in response to quercetin (single dose of 7 mg/animal) revealed a molecular relationship between the liver and jejunum. In WT animals, amino acid and sterol metabolism was predominantly modulated in the liver, fatty acid metabolism response was shared between the liver and jejunum, and glutathione metabolism was modulated in the small intestine. In contrast, KO animals do not regulate amino acid metabolism in the liver or small intestine, they share the control of fatty acid metabolism between the liver and jejunum, and regulation of sterol metabolism is shifted from the liver to the jejunum and that of glutathione metabolism from the jejunum to the liver. This demonstrates that the quercetin-mediated regulation of these biological functions in extrahepatic tissues is dependent on the functionality of the liver POR. In conclusion, using a systems biology approach to explore the contribution of hepatic phase 1 detoxification on quercetin metabolism demonstrated the resiliency and adaptive capacity of a biological organism in dealing with a bioactive nutrient when faced with a tissue-specific molecular dysfunction.

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Section: Discussionmentioning

confidence: 94%

“…Findings from the present study would support this notion. Both rat and human intestinal and hepatic cell models are capable of differentially metabolizing quercetin (33), and intestinal metabolism of quercetin is extensive (8,29). Taken together, the functional elimination of all hepatic Table S1.…”

Section: Discussionmentioning

confidence: 99%

Hepatic cytochrome P-450 reductase-null mice show reduced transcriptional response to quercetin and reveal physiological homeostasis between jejunum and liver

Mutch¹,

Crespy²,

Clough³

et al. 2006

American Journal of Physiology-Gastrointestinal and Liver Physi

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show abstract

“…Quercetin is believed to be the most effective orally active antioxidant and the present observations of quercetin activity are consistent with the proposal that hydroxyl groups of flavones at positions 3Ј, 4Ј, 5 and 7 are associated with TNF-a inhibition. [32][33][34] IL-10 is known to inhibit the activation of macrophages and T cells and to decrease proinflammatory cytokine production in acute pancreatitis. 35,36) Administration of exogenous IL-10 protects the pancreas against acute damage.…”

Section: Discussionmentioning

confidence: 99%

The Natural Flavonoid Quercetin Ameliorates Cerulein-Induced Acute Pancreatitis in Mice

Carvalho

Morais

Melo

et al. 2010

Biological & Pharmaceutical Bulletin

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“…Additionally, in vitro penetration test and bioavailability study in rats were performed. The previous QC bioavailability studies were only done through the oral, intravenous or other parenteral routes [31][32][33][34][35][36][37] . Davies and Yaniez [32] , stated that until 2013, no one had tested the pharmacokinetics of QC from a transdermal dosage form, either in animals or humans.…”

Section: In Vitro Penetration and Bioavailability Of Novel Transdermamentioning

confidence: 99%

In vitro Penetration and Bioavailability of Novel Transdermal Quercetin-loaded Ethosomal Gel

Ramadon¹,

Anwar²,

Harahap³

2017

pharmaceutical-sciences

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Quercetin has been widely used to treat many diseases because of its high antioxidant activity. However, it has low oral bioavailability and penetration through the skin. The aim of this research was to enhance penetration and bioavailability of quercetin using transdermal ethosomal gel. Three ethosomal formulae, E1 (1 %), E2 (1.5 %) and E3 (2 %) with different concentration of quercetin were prepared using thin-film hydration method. Their physical properties were characterized, and then a selected ethosomal formula was incorporated into a gel dosage form. Two gels, one ethosomal and the other non-ethosomal were prepared. In vitro penetration using Franz diffusion cells and bioavailability study in Sprague Dawley male rats were carried out. Results showed that E2 was the chosen formula to be incorporated into the gel dosage form. According to the in vitro penetration study, the diffusion flux of quercetin from the ethosomal and non-ethosomal gels were 343.35±17.69 ng/cm 2 /h and 120.68±11.92 ng/cm 2 /h, respectively (P<0.05). In the bioavailability study, ethosomal gel showed higher maximum concentration (C max ) and area under curve (AUC 0-t ) when compared to non-ethosomal gel and oral suspension. C max from the ethosomal gel, nonethosomal gel, and oral suspension were 413.49±28.64, 189.46±49.68, and 61.92±14.31 ng/ml, respectively (P<0.05). AUC 0-t from the ethosomal gel, non-ethosomal gel, and oral suspension were 4035.15±560.60, 584.87±265.46, and 431.21±239.85, respectively (P<0.05). In conclusion, ethosomal gel could increase penetration and bioavailability of quercetin compared to non-ethosomal gel.

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Pharmacokinetics and Modeling of Quercetin and Metabolites

Cited by 189 publications

References 28 publications

Hepatic cytochrome P-450 reductase-null mice show reduced transcriptional response to quercetin and reveal physiological homeostasis between jejunum and liver

Hepatic cytochrome P-450 reductase-null mice show reduced transcriptional response to quercetin and reveal physiological homeostasis between jejunum and liver

The Natural Flavonoid Quercetin Ameliorates Cerulein-Induced Acute Pancreatitis in Mice

In vitro Penetration and Bioavailability of Novel Transdermal Quercetin-loaded Ethosomal Gel

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