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 in | Scientific reports Vol. 6; no. 1; p. 35460 |
---|---|
Main Authors | , , , , , , , , |
Format | Journal Article |
Language | English |
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London
Nature Publishing Group UK
24.10.2016
Nature Publishing Group |
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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. |
Author_xml | – sequence: 1 givenname: Le-Le surname: Yang fullname: Yang, Le-Le organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 2 givenname: Na surname: Xiao fullname: Xiao, Na organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 3 givenname: Xiao-Wei surname: Li fullname: Li, Xiao-Wei organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 4 givenname: Yong surname: Fan fullname: Fan, Yong organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 5 givenname: Raphael N. surname: Alolga fullname: Alolga, Raphael N. organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 6 givenname: Xiao-Yue surname: Sun fullname: Sun, Xiao-Yue organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 7 givenname: Shi-Lei surname: Wang fullname: Wang, Shi-Lei organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 8 givenname: Ping surname: Li fullname: Li, Ping organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University – sequence: 9 givenname: Lian-Wen surname: Qi fullname: Qi, Lian-Wen organization: State Key Laboratory of Natural Medicines, China Pharmaceutical University |
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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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 |
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