Aurantio-obtusin,　an　anthraquinone　isolated　from　cassiae　semen,　possesses　diverse　pharmacological　activities,　including　hypotensive,　hypolipidemic　and　anti-inflammatory　effects.　However,　our　previous　studies　demonstrated　that　exposure　to　aurantio-obtusin　induced　hepatotoxicity,　but　the　mechanisms　of　the　toxic　effects　remain　unknown.　The　purpose　of　the　present　study　is　to　establish　a　strategy　for　the　metabolite　profiling　of　aurantio-obtusin　in　normal　and　liver-injured　rats.　This　study　aimed　at　identifying　the　in　vivo　metabolites　and　the　metabolic　profiling　in　rats　after　oral　administration　at　a　dose　of　aurantio-obtusin　(4　and　200　mg/kg)　by　using　an　ultra　performance　liquid　chromatography　coupled　with　quadrupole　time-of-flight　mass　spectrometry　(UPLC-QTOF-MS)　and　metabolynx™　software.　A　total　of　39　metabolites　were　detected　and　3　of　them　were　compared　with　standard　substances.　The　results　indicated　that　the　principal　metabolism　pathways　of　aurantio-obtusin　in　normal　rats　were　glucuronidation　and　sulfation,　while　in　rats　with　liver　injury,　demethylation,　dehydroxylation　and　reduction　were　also　observed　and　regarded　as　new　metabolic　patterns　of　aurantio-obtusin.　These　findings　helped　us　to　understand　the　pharmacological　and　toxicological　mechanisms　of　aurantio-obtusin.　Moreover,　this　study　could　help　to　elucidate　the　metabolic　profiling　of　other　anthraquinones.