Aim Abelmoschi Corolla is a well-known herbal medicine used for the treatment of chronic renal disease . Flavonoids are the major bioactive ingredients of Abelmoschi Corolla, but some non-flavonoid components also exist in this herb. In order to clarify the influences of non-flavonoid components on the pharmacokinetics profile of the flavonoid fraction from Abelmoschi Corolla (FFA), an investigation was carried out to compare the pharmacokinetic parameters of seven flavonoid components after administration of FFA and after administration of FFA combined with different non-flavonoid fractions. Materials and methods A selective and sensitive UPLC–MS/MS method was established to determine the plasma concentrations of the seven compounds. Sprague-Dawley rats were allocated to four groups which orally administered FFA, FFA combined with macromolecular fraction (FFA–MF), FFA combined with small molecule fraction (FFA–SF) and FFA combined with MF–SF (FFA–MF–SF) with approximately the same dose of FFA. At different time points, the concentration of rutin (1), hyperoside (2), isoquercitrin (3), hibifolin (4), myricetin (5), quercetin-3′- O -glucose (6), quercetin (7) in rat plasma were determined and main pharmacokinetic parameters including T 1/2 , T max , AUC and C max were calculated using the DAS 2.0 software package. The statistical analysis was performed using the Student's t -test with P <0.05 as the level of significance. Results Flavonoids almost had similar pharmacokinetics profile that were rapidly absorbed, reached the peak concentration at 30–60 min in group A, but the pharmacokinetic profiles and parameters of these flavonoids changed when co-administered with non-flavonoid components. It was found that AUC of five flavonoids but not hibifolin and quercetin in group FFA–SF and group FFA–MF–SF increased ( P <0.05) in comparison with group FFA while the tendency was not observed in group FFA–MF. Moreover, seven flavonoids had varying degrees of differences in the pharmacokinetics parameters such as C max , T max and T 1/2 ( P <0.05) in group FFA–MF, FFA–SF and FFA–MF–SF by comparison with group FFA. Conclusion These results indicate that non-flavonoid components could improve the bioavailability and delay the elimination of some flavonoids in rat.
The total flavone of Abelmoschi Corolla (TFA) has diverse pharmacological effects, including anti-inflammatory and antioxidant properties, and improving insulin resistance. Clinically, TFA has been utilized for a substantial duration for managing various renal diseases. Phase II metabolites, such as sulfated and glucuronidated conjugates, are the primary in vivo forms of flavonoids and may mediate the pharmacological effects of TFA. However, the direct quantification of conjugated metabolites is limited by the lack of reference standards. To address this, β-glucuronidase/sulfatase hydrolysis can be used to cleave these conjugates, releasing aglycones and enabling the indirect quantification of total flavonoids. In this study, a reliable and sensitive ultra-high-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the quantification of gossypetin, myricetin, quercetin, and isorhamnetin in mouse plasma following enzymatic hydrolysis. Chromatographic separation was performed using a Waters ACQUITY UPLC HSS-T3 column with gradient elution. The mobile phase consisted of acetonitrile and water (both containing 0.1 % formic acid) at a flow rate of 0.35 mL/min. The method was validated for plasma analysis and successfully applied to a pharmacokinetic study in mice following oral administration of TFA. The results showed that the analyzed aglycones rapidly attained maximum plasma concentrations. The area under the curve for each compound demonstrated a positive correlation with the administered dose in the range of 100–400 mg/kg. Moreover, the isorhamnetin concentration increased significantly following 7-day repeated gavage compared to that with a single 200 mg/kg TFA dose. These pharmacokinetic findings may inform future drug development and clinical applications of TFA-derived substances.
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