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

摘要: 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 on activities cytochrome P450 (CYP) enzymes were with human liver microsomes recombinant CYP isozymes. 6-Paradol showed concentration-dependent CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19 isozymes, IC50 values ranging from 3.8 21.4µM However, inhibition was not potentiated following pre-incubation, indicating that is mechanism-based inhibitor. These results suggest pharmacokinetic drug-drug interactions might occur 6-paradol, which must be considered process development.