brucine and indole

Brucine is a widely prescribed glycine antagonist, but a complete understanding of its metabolic pathway is still lacking. The present work represents the first investigation of in vivo metabolism of brucine in rats using LC-ESI-ion trap-TOF-MS.. A total of 12 Phase I and five Phase II metabolites were tentatively identified. Brucine can be metabolized by hydrolysis, demethylation and methoxylation, in addition to diverse oxidations in a Phase I manner followed by glucuronidation in Phase II metabolism. Both the renal and biliary routes were observed for the excretion of brucine and its metabolites.. Our results update the metabolism and disposition data on brucine, which provides basic information for better understanding of the pharmacological and toxicological activities of brucine-containing medicines.

Topics: Alkaloids; Animals; Bile; Biotransformation; Chromatography, High Pressure Liquid; Glucuronidase; Hydrolysis; Hydroxylation; Indoles; Metabolic Networks and Pathways; Oxidation-Reduction; Rats; Spectrometry, Mass, Electrospray Ionization; Strychnine