Previous　studies　revealed　the　hepatotoxic　effect　of　aurantio-obtusin　on　rats.　The　aim　of　this　study　was　to　identify　potential　biomarkers　of　urine　caused　by　aurantio-obtusin.　Sprague-Dawley　(SD)　rats　with　body　weight　of　0,　4,　40,　and　200　mg/kg　were　orally　given　aurantio-obtusin　for　28　days,　and　urine　was　collected　for　24　h　after　the　last　administration.　The　urine　metabolites　in　the　aurantio-obtusin　group　and　the　control　group　were　analyzed　by　ultraperformance　liquid　chromatography　quadrupole　time-of-flight　mass　spectrometry　(UPLC-QTOF/MS).　Twenty-three　metabolites　were　identified　as　potential　biomarkers,　and　10　of　them　were　up-regulated,　including　xanthosine,　hippuric　acid,　5-L-glutamyl-taurine,　etc.　The　other　13　biomarkers　were　down-regulated,　including　thymidine,　3-methyldioxyindole,　cholic　acid,　etc.　The　significant　changes　of　these　biomarkers　indicated　that　purine　metabolism,　taurine　and　hypotaurine　metabolism,　primary　bile　acid　biosynthesis,　pyrimidine　metabolism,　and　tryptophan　metabolism　played　an　important　role　in　the　hepatotoxicity　of　aurantio-obtusin　in　rats.　In　this　paper,　the　safety　and　potential　risk　of　aurantio-obtusin　were　studied　for　the　first　time　by　combining　the　toxicity　of　aurantio-obtusin　with　the　results　of　urine　metabolomics,　which　provided　information　for　the　mechanism　of　liver　injury　induced　by　aurantio-obtusin.