Phase I and phase II metabolite identification of rutaecarpine in freshly isolated hepatocytes from male Sprague–Dawley rats

• Published in: Archives of pharmacal research Vol. 40; no. 8; pp. 972 - 979
• Main Authors: Lee, Dong Wook, Kang, Youra, Kang, Mi Jeong, Noh, Keumhan, Kim, Ju Hyun, Nepal, Mahesh R., Shakya, Rajina, Lee, Yu-Jeong, Jahng, Yurngdong, Lee, Sangkyu, Kim, Jung-Ae, Jeong, Tae Cheon
• Format: Journal Article
• Language: English
• Published: Seoul Pharmaceutical Society of Korea 01.08.2017; 대한약학회
• Subjects: alkaloids; Asia; digestive system diseases; drugs; Euodia; hepatocytes; laboratory animals; liquid chromatography; males; Medicine; metabolites; Pharmacology/Toxicology; Pharmacy; rats; Research Article; sulfates; tandem mass spectrometry; 약학; Asia; Phase II; Phase I; Hepatocytes; Metabolism; Rutaecarpine
• ISSN: 0253-6269; 1976-3786; 1976-3786
• DOI: 10.1007/s12272-017-0937-7

Rutaecarpine, an alkaloid originally isolated from Evodia rutaecarpa , has been used for the treatment of gastrointestinal disorders in Asia. In the present study, the phase I and phase II metabolites of rutaecarpine were investigated in freshly isolated hepatocytes from male Sprague–Dawley rats. The individual metabolites were characterized via liquid chromatography-tandem mass spectrometry. The incubation of rutaecarpine with freshly isolated hepatocytes for 2 h yielded five major phase I metabolites. In addition, three glucuronide conjugates and four sulfate conjugates were observed. Because the majority of metabolites observed in vivo were identified, freshly isolated hepatocytes might be useful for the identification of certain metabolites formed from drug candidates from a reduced number of experimental animals.