TY - JOUR AU - 유혜현 DA - 2017/04 PY - 2017 UR - https://www.sciencedirect.com/science/article/pii/S0960894X17301798 UR - https://repository.hanyang.ac.kr/handle/20.500.11754/71966 AB - 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. PB - PERGAMON-ELSEVIER SCIENCE LTD KW - 6-Paradol KW - Unsaturated ketone KW - Ginger KW - CYP inhibition KW - Drug-drug interaction KW - ENZYMES TI - Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism IS - 8 VL - 27 DO - 10.1016/j.bmcl.2017.02.047 T2 - BIOORGANIC & MEDICINAL CHEMISTRY LETTERS ER -