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Isovitexin, a bioactive flavonoid constituent isolated from Desmodii Styracifolii, is considered an adjuvant for antiurolithiasis diseases. In this study, an ultra‐high‐performance liquid chromatography coupled with hybrid triple quadruple time‐of‐flight mass spectrometry method was developed to characterize and compare the metabolic profiling of isovitexin experimented on normal and kidney stone model rats. The comparative research indicated that 28 metabolites (18 phase I and 10 phase II) in normal rats and 33 metabolites (20 phase I and 13 phase II) in kidney stone model rats were initially identified. The results of relative quantitative determination reflected that the contents of metabolites produced by deglycosylation, reduction, and isomerization in kidney stone model rats were greater than those in healthy rats. Instead, the levels of oxidative and dehydrogenated metabolites in normal groups were higher than those in kidney stone model groups. The results of this study are valuable and important for understanding the metabolic process of isovitexin in clinical application, and especially the metabolism study in kidney stone model rats could provide a beneficial reference for the further search of effective substances associated with the treatment of kidney stones. [ABSTRACT FROM AUTHOR]

Schaftoside is a flavone-C-glycoside isolated from Herba Desmodii Styracifolii with valuable anti-kidney stones efficacies. In this study, a six-step strategy was first developed to detect and identify the metabolites in plasma, urine, bile, feces and rat intestinal bacteria samples of healthy and model rats administrated with schaftoside using ultra-high-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS). The number and the relative peak area of metabolites in healthy rats and model rats were compared, and it was noticed that metabolites in bio-samples of healthy and model rats both had obvious differences. A total of 28 metabolites of schaftoside in healthy rats and 30 metabolites in model rats were initially indentified. The relative peak area of the parent drug and every metabolite in model rat plasma samples were larger than those in healthy rat plasma. Those metabolites with high blood concentrations might be beneficial for the treatment of calcium oxalate stones in the kidney. The results are valuable and important for understanding the metabolic process of schaftoside in clinical application, and especially the metabolism study in calcium oxalate kidney stone model rats could provide a beneficial reference for the further search of effective substances associated with the treatment of kidney stones. Image 1 • A practical method by UHPLC-Q-TOF-MS/MS for comparing the metabolites of schaftoside in healthy and model rats was developed. • A six-step strategy was developed to screen and identify metabolites. • 28 metabolites of schaftoside in healthy rats and 30 metabolites in model rats were initially indentified. • Proposed metabolic pathways of schaftoside in healthy and model rats were inferred. [ABSTRACT FROM AUTHOR]