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

• Published in: Scientific 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
• Language: English
• Published: London Nature Publishing Group UK 24.10.2016; Nature Publishing Group
• Subjects: 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
• ISSN: 2045-2322; 2045-2322
• DOI: 10.1038/srep35460

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.