Pharmacokinetic comparison of quercetin, isoquercitrin, and quercetin-3-O-β-D-glucuronide in rats by HPLC-MS

Abstract

Background Quercetin (Qr), isoquercitrin (IQ), and quercetin-3-O-β-D-glucuronide (QG) are powerful phytochemicals that have been shown to exhibit disease prevention and health promotion properties. However, there may exist transformations between Qr, IQ, and QG in vivo. And the pharmacokinetic profiles of Qr, IQ, and QG have not been systematically compared. The pharmacokinetics study would be helpful to better understand the pharmacological actions of them. Methods Herein, we developed a reliable HPLC-MS method to compare the pharmacokinetics of Qr, IQ, and QG after separate (50 mg/kg) oral administration of them in rats, using puerarin as internal standard. The detection was performed using negative selected ion monitoring. This method was validated in terms of selectivity, linearity, precision, accuracy, extraction recovery, matrix effect, and stability; and shows reliabilities in monitoring the pharmacokinetic behaviors of these three compounds. Results Our results showed that after separate oral administration of Qr, IQ, and QG, all of the compounds could be detected in plasma. In addition, QG could be detected in the Qr group; Qr and QG could be measured in the IQ group; and Qr could be found in rat plasma after 1.5 h of QG administration. Moreover, the AUC0−t of Qr in the; Qr group (2,590.5 ± 987.9 mg/L*min), IQ group (2,212.7 ± 914.1 mg/L*min), and QG group (3,505.7 ± 1,565.0 mg/L*min) was larger than the AUC0−t of QG in the; Qr group (1,550.0 ± 454.2 mg/L*min), IQ group (669.3 ± 188.3 mg/L*min), and QG group (962.7 ± 602.3 mg/L*min). The AUC0−t of IQ was the lowest among all groups. Discussion Quercetin, IQ, and QG can all be absorbed into plasma. A mutual transformation exists between Qr and QG, and IQ can be metabolized into Qr and QG in SD rats. These results would provide a meaningful basis for understanding the pharmacological actions of these three compounds.

The Anti-Cancer Effect of Quercetin: Molecular Implications in Cancer Metabolism

“…Quercetin in foods is bound to sugars, mainly as β-glycosides, whose bioavailability is affected by their sugar moiety. Isoquercitrin’s bioavailability is only 5% of that observed with QUE, and in the gut, it is rapidly metabolized to QUE by β-glucosidases [102]. This suggests that the systemic and local (in the gut) effects of QUE (glucoside)-rich food are predominantly anti-carcinogenic by targeting glycolysis.…”

Systemic elucidation on the potential bioactive compounds and hypoglycemic mechanism of Polygonum multiflorum based on network pharmacology

“…Quercetin is a natural avonoid, quercetin (Qr), isoquercitrin (IQ), and quercetin-3-O-β-D-glucuronide (QG) were also mutual transform in vivo. The t1/2 of quercetin is about 437min [65]. And studies have shown that QG is a major active component in plasma and tissue for oral administration of Qr or QG [66].…”

Systemic elucidation on the potential bioactive compounds and hypoglycemic mechanism of Polygonum multiflorum based on network pharmacology

“…Quercetin is a natural flavonoid, quercetin (Qr), isoquercitrin (IQ), and quercetin-3-O-β- d -glucuronide (QG) were also mutual transform in vivo. The t1/2 of quercetin is about 437 min [ 65 ]. And studies have shown that QG is a major active component in plasma and tissue for oral administration of Qr or QG [ 66 ].…”