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Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism

Title
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism
Author
유혜현
Keywords
6-Paradol; Unsaturated ketone; Ginger; CYP inhibition; Drug-drug interaction; ENZYMES
Issue Date
2017-04
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v. 27, No. 8, Page. 1826-1830
Abstract
Paradols are unsaturated ketones produced by biotransformation of shogaols in gingers. Among them, 6-paradol has been investigated as a new drug candidate due to its anti-inflammatory, apoptotic, and neuroprotective activities. In this study, the inhibitory effects of 6-paradol on the activities of cytochrome P450 (CYP) enzymes were investigated with human liver microsomes and recombinant CYP isozymes. 6-Paradol showed concentration-dependent inhibitory effects on CYP1A2, CYP2B6, CYP2C8, CYP2C9, and CYP2C19 isozymes, with IC50, values ranging from 3.8 to 21.4 mu M in recombinant CYP isozymes. However, the inhibition was not potentiated following pre-incubation, indicating that 6-paradol is not a mechanism-based inhibitor. These results suggest that pharmacokinetic drug-drug interactions might occur with 6-paradol, which must be considered in the process of new drug development. (C) 2017 Elsevier Ltd. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S0960894X17301798http://repository.hanyang.ac.kr/handle/20.500.11754/71966
ISSN
0960-894X; 1464-3405
DOI
10.1016/j.bmcl.2017.02.047
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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