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Potential Risk of Mulberry-Drug Interaction: Modulation on P-glycoprotein and Cytochrome P450 3A.


J Agric Food Chem. 2013 Apr 16;


Authors: Hsu PW, Shia CS, Lin SP, Chao PD, Juang SH, Hou YC


Abstract

Mulberry is a fruit containing polyphenol antioxidants. Cyclosporine (CSP), a potent immunosuppressant with narrow therapeutic range, is widely used in transplant patients. This study investigated the effect of coadministration of mulberry on the bioavailability of CSP, a probe drug of P-gp/CYP 3A4, in rats and relevant mechanisms. CSP (2.5 mg/kg) was orally administered with and without single dose and the 7th dose of mulberry (2 g/kg) to rats. The results showed that single dose of mulberry significantly decreased the area under the curve of concentration (AUC0-540) and the maximum blood concentration (Cmax) of CSP by 53.2% and 65.8%, respectively. Repeated dosing of mulberry significantly decreased the AUC0-540 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.

PMID: 23590720 [PubMed - as supplied by publisher]