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Characterization of human liver cytochrome P450 enzymes involved in the metabolism of rutaecarpine

Title
Characterization of human liver cytochrome P450 enzymes involved in the metabolism of rutaecarpine
Author
유혜현
Keywords
rutaecarpine; human liver microsomes; LC-ESI/MS
Issue Date
2006-04
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, v. 41, No. 1, Page. 304-309
Abstract
Rutaecarpine has recently been characterized to have an anti-inflammatory activity through cyclooxygenase-2 inhibition. The incubation of rutaecarpine with human liver microsomes in the presence of NADPH generated six isobaric mono-hydroxylated metabolites. The specific cytochrome P450 (CYP) isozymes responsible for rutaecarpine metabolites were identified using the combination of chemical inhibition, immuno-inhibition and metabolism by cDNA expressed CYP enzymes. The results suggested that CYP3A4 might play major roles in the metabolism of rutaecarpine in human liver microsomes. The production of M1, M2, M3, M4 and M6 formed in human liver microsomes was inhibited by ketoconazole, a selective CYP3A4 inhibitor, and anti-CYP3A4 antibody. CYP1A2 and CYP2C9 played minor roles in the metabolism of rutaecarpine. These results were confirmed in microsomes derived from cDNA expressed lymphoblastoid cells. CYP3A4 microsome clearly formed M 1, M2, M3 and M6. CYP1A2 and CYP2C9 microsomes comparably formed M5. (c) 2005 Elsevier B.V. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S073170850500693Xhttp://repository.hanyang.ac.kr/handle/20.500.11754/107876
ISSN
0731-7085; 1873-264X
DOI
10.1016/j.jpba.2005.10.039
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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