Related Experiment Videos
Potential risk of mulberry-drug interaction: modulation on P-glycoprotein and cytochrome P450 3A
Pei-Wen Hsu1, Chi-Sheng Shia, Shiuan-Pey Lin
1School of Pharmacy, China Medical University, Taichung 404, Taiwan, Republic of China.
Abstract:
Mulberry is a fruit containing polyphenol antioxidants. Cyclosporine (CSP), a potent immunosuppressant with a narrow therapeutic range, is widely used in transplant patients. This study investigated the effect of co-administration of mulberry on the bioavailability of CSP, a probe drug of P-glycoprotein (P-gp)/cytochrome P450 3A4 (CYP 3A4), in rats and relevant mechanisms. CSP (2.5 mg/kg) was orally administered with and without a single dose or the seventh dose of mulberry (2 g/kg) to rats. The results showed that a single dose of mulberry significantly decreased the area under the curve of concentration (AUC(0-540)) and the maximum blood concentration (Cmax) of CSP by 53.2 and 65.8%, respectively. Repeated dosing of mulberry significantly decreased the AUC(0-540) and Cmax of CSP by 23.7 and 39.7%, respectively. Mechanism studies indicated that mulberry significantly increased the activities of P-gp and CYP 3A. In conclusion, mulberry significantly reduced the bioavailability of CSP through activating the functions of P-gp and CYP 3A.
Related Concept Videos
Pharmacokinetics: Drug–Drug Interactions
Drug toxicity: Drug–Drug Interaction
Pharmacokinetics: Drug–Food and Drug–Viral Interactions
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu
Drug toxicity: Idiosyncratic Reactions
Effect of Hepatic Disease on Pharmacokinetics: Dose Adjustments Due to Hepatic Impairment