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/S0960894X17301798https://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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