Pharmacokinetic comparison between quercetin and quercetin 3-O-β-glucuronide in rats by UHPLC-MS/MS

Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3- O - β -glucuronide (Q3G) is present in wine and some medicinal plants. Quercetin and Q3G may be metabolized from each other in vivo . While quercetin has been the subject of many studies, the pharmac...

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Published inScientific reports Vol. 6; no. 1; p. 35460
Main Authors Yang, Le-Le, Xiao, Na, Li, Xiao-Wei, Fan, Yong, Alolga, Raphael N., Sun, Xiao-Yue, Wang, Shi-Lei, Li, Ping, Qi, Lian-Wen
Format Journal Article
LanguageEnglish
Published London Nature Publishing Group UK 24.10.2016
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Abstract Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3- O - β -glucuronide (Q3G) is present in wine and some medicinal plants. Quercetin and Q3G may be metabolized from each other in vivo . While quercetin has been the subject of many studies, the pharmacokinetic profiles of quercetin and Q3G (in animals) have not yet been compared. Herein, we prepared a column-based method for rapid isolation of Q3G from Nelumbo nucifera . Then, we developed an UHPLC-MS/MS method to compare the pharmacokinetics of quercetin and Q3G. Our results showed that the plasma concentration-time curves of quercetin and Q3G show two maxima ( T max 1  ≈ 0.75 h, T max 2  ≈ 5 h). After oral administration of 100 mg/kg quercetin or 100 mg/kg Q3G in rats, predominantly Q3G was detected in plasma with AUC at 39529.2 ± 6108.2 mg·h·L −1 or 24625.1 ± 1563.8 mg·h·L −1 , 18-fold higher than quercetin with AUC at 1583.9 ± 583.3 mg·h·L −1 or 1394.6 ± 868.1 mg·h·L −1 , respectively. After intravenous injection of 10 mg/kg in rats, Q3G showed extensive tissue uptake in kidney (409.2 ± 118.4 ng/g), liver (166.1 ± 52.9 ng/g), heart (97.7 ± 22.6 ng/g), and brain (5.8 ± 1.2 ng/g). In conclusion, we have shown that Q3G is a major active component in plasma and tissue for oral administration of quercetin or Q3G.
AbstractList Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3- O - β -glucuronide (Q3G) is present in wine and some medicinal plants. Quercetin and Q3G may be metabolized from each other in vivo . While quercetin has been the subject of many studies, the pharmacokinetic profiles of quercetin and Q3G (in animals) have not yet been compared. Herein, we prepared a column-based method for rapid isolation of Q3G from Nelumbo nucifera . Then, we developed an UHPLC-MS/MS method to compare the pharmacokinetics of quercetin and Q3G. Our results showed that the plasma concentration-time curves of quercetin and Q3G show two maxima ( T max 1  ≈ 0.75 h, T max 2  ≈ 5 h). After oral administration of 100 mg/kg quercetin or 100 mg/kg Q3G in rats, predominantly Q3G was detected in plasma with AUC at 39529.2 ± 6108.2 mg·h·L −1 or 24625.1 ± 1563.8 mg·h·L −1 , 18-fold higher than quercetin with AUC at 1583.9 ± 583.3 mg·h·L −1 or 1394.6 ± 868.1 mg·h·L −1 , respectively. After intravenous injection of 10 mg/kg in rats, Q3G showed extensive tissue uptake in kidney (409.2 ± 118.4 ng/g), liver (166.1 ± 52.9 ng/g), heart (97.7 ± 22.6 ng/g), and brain (5.8 ± 1.2 ng/g). In conclusion, we have shown that Q3G is a major active component in plasma and tissue for oral administration of quercetin or Q3G.
Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3-O-β-glucuronide (Q3G) is present in wine and some medicinal plants. Quercetin and Q3G may be metabolized from each other in vivo. While quercetin has been the subject of many studies, the pharmacokinetic profiles of quercetin and Q3G (in animals) have not yet been compared. Herein, we prepared a column-based method for rapid isolation of Q3G from Nelumbo nucifera. Then, we developed an UHPLC-MS/MS method to compare the pharmacokinetics of quercetin and Q3G. Our results showed that the plasma concentration-time curves of quercetin and Q3G show two maxima (T  ≈ 0.75 h, T  ≈ 5 h). After oral administration of 100 mg/kg quercetin or 100 mg/kg Q3G in rats, predominantly Q3G was detected in plasma with AUC at 39529.2 ± 6108.2 mg·h·L or 24625.1 ± 1563.8 mg·h·L , 18-fold higher than quercetin with AUC at 1583.9 ± 583.3 mg·h·L or 1394.6 ± 868.1 mg·h·L , respectively. After intravenous injection of 10 mg/kg in rats, Q3G showed extensive tissue uptake in kidney (409.2 ± 118.4 ng/g), liver (166.1 ± 52.9 ng/g), heart (97.7 ± 22.6 ng/g), and brain (5.8 ± 1.2 ng/g). In conclusion, we have shown that Q3G is a major active component in plasma and tissue for oral administration of quercetin or Q3G.
ArticleNumber 35460
Author Sun, Xiao-Yue
Li, Ping
Qi, Lian-Wen
Yang, Le-Le
Xiao, Na
Li, Xiao-Wei
Wang, Shi-Lei
Fan, Yong
Alolga, Raphael N.
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  surname: Fan
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– sequence: 5
  givenname: Raphael N.
  surname: Alolga
  fullname: Alolga, Raphael N.
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/27775094$$D View this record in MEDLINE/PubMed
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Snippet Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3- O - β -glucuronide (Q3G) is present in wine and some...
Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3-O-β-glucuronide (Q3G) is present in wine and some medicinal...
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pubmed
crossref
springer
SourceType Open Access Repository
Index Database
Enrichment Source
Publisher
StartPage 35460
SubjectTerms 140/131
631/1647/296
631/92/349
639/638/11
Administration, Oral
Animals
Chromatography, High Pressure Liquid - methods
Humanities and Social Sciences
Injections, Intravenous
Male
multidisciplinary
Quercetin - administration & dosage
Quercetin - analogs & derivatives
Quercetin - blood
Quercetin - chemistry
Quercetin - pharmacokinetics
Rats, Sprague-Dawley
Reproducibility of Results
Science
Tandem Mass Spectrometry - methods
Tissue Distribution
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Title Pharmacokinetic comparison between quercetin and quercetin 3-O-β-glucuronide in rats by UHPLC-MS/MS
URI https://link.springer.com/article/10.1038/srep35460
https://www.ncbi.nlm.nih.gov/pubmed/27775094
https://pubmed.ncbi.nlm.nih.gov/PMC5075792
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