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Metabolite profiling and quantification of phytochemicals of Tianma-Gouteng granule in human and rat urine using ultra-performance liquid chromatography coupled with tandem mass spectrometry.

Tianma-Gouteng granule has been used for the treatment of hypertension, headache and stroke in China. However, the metabolism of Tianma-Gouteng granule has not been clear. In the present study, an ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry method has developed for rapid identification of 35 prototypes and 43 metabolites in human and rat urines after single oral administration of Tianma-Gouteng granule. The results showed that glucuronidation and sulfation were the main metabolic pathways for flavonoids, alkaloids, iridoidic glycosides, anthraquinones, phenols and stilbenes that were found in Tianma-Gouteng granule. Moreover, a validated ultra-performance liquid chromatography coupled with tandem mass spectrometry method was applied for the quantification of 14 compounds in rat urine after an oral administration of Tianma-Gouteng granule (2.5g/kg). During 0-48 h after dosing, the cumulative excretion rates of nine prototype components were 53% for gastrodin, 0.07∼1.6% for geniposide, baicalin and baicalein, wogonoside, rhynchophylline and isorhynchophylline, leonurine, and emodin, respectively, indicating that urinary excretion is the major way for gastrodin to eliminate from the body. This study provides a comprehensive understanding of metabolism and excretive kinetics of Tianma-Gouteng granule in human and/or rat, and helpful information for screening of its active components in vivo and clinical application. This article is protected by copyright. All rights reserved.