The metabolites of Ambinine, a benzo[c]phenanthridine alkaloid, in rats identified by ultra-performance liquid chromatography–quadrupoletime-of-flight mass spectrometry (UPLC/Q-TOF-MS/MS)

• A powerful UPLC/Q-TOF-MS/MS method was employed to screen and identify the in vivo metabolites of ambinine, a hexahydrobenzo[c] phenanthridine alkaloids, in rat urine, feces, plasma and bile and the metabolic pathway of AM also was proposed for the first time.
• The 44 metabolites of AM in rat were studied by UPLC/Q-TOF-MS/MS and 41 metabolites of them were reported for the first time.
• The major metabolic pathway of AM was demethylation, sulfation and glucuronidation.

Ambinine (AM), one of the major hexahydrobenzo[c]phenanthridine alkaloids from Corydalis ambigua Cham. et Schlecht. var. amurensis Maxim, is considered to be an important compound because of its special content and activity. However, there are few published studies on AM metabolism. In this research, the metabolism of AM in vivo was comprehensively studied for the first time. A total 44 metabolites (including 13 phase I and 31 phase II metabolites) as well as its parent drug in plasma, bile, urine and feces of rats were identified and 41 of them were reported for the first time. The results obtained indicated that demethylation, sulfation and glucuronidation were the major metabolic pathways of AM in vivo. Furthermore, this study provides valuable and new information about the metabolism of AM, which will be very helpful for understanding the safety and efficacy of AM, as well as its analogues.