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In this study, an ultra\u2010performance liquid chromatography coupled with quadrupole time\u2010of\u2010flight mass spectrometry was used for profiling the chemical components and related metabolites of Periplocae Cortex. A total of 98 constituents were identified or tentatively characterized in Periplocae Cortex: 42 C21 steroidal glycosides, 10 cardiac glycosides, 23 organic acids, 4 aldehydes, 7 triterpenes, and 12 other types. Among them, 18 components were unambiguously identified by comparison with reference standards. In addition, 176 related xenobiotics (34 prototypes and 142 metabolites) were screened out and characterized in rats\u2019 biosamples (plasma, urine, bile, and feces) after the oral administration of Periplocae Cortex. Moreover, the metabolic fate of periplocoside S\u20104a, a C21 steroidal glycoside, was proposed for the first time. In summary, phase II reactions (methylation, glucuronidation, and sulfation), phase I reactions (hydrolysis reactions, oxygenation, and reduction), and their combinations were the predominant metabolic reactions of Periplocae Cortex in rat. It is the first report to reveal the <jats:italic>in<\/jats:italic> <jats:italic>vivo<\/jats:italic> substances and metabolism feature of Periplocae Cortex. This study also provided meaningful information for further pharmacodynamics study of Periplocae Cortex, as well as its quality control research.<\/jats:p>","DOI":"10.1002\/bmc.4807","type":"journal-article","created":{"date-parts":[[2020,2,5]],"date-time":"2020-02-05T01:22:22Z","timestamp":1580865742000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":16,"title":["Characterization of chemical components of Periplocae Cortex and their metabolites in rats using ultra\u2010performance liquid chromatography coupled with quadrupole time\u2010of\u2010flight mass spectrometry"],"prefix":"10.1002","volume":"34","author":[{"given":"Zi\u2010ting","family":"Li","sequence":"first","affiliation":[{"name":"Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, and International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education 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