期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 59, 期 9, 页码 4644-4648出版社
AMER CHEMICAL SOC
DOI: 10.1021/jf104786t
关键词
Bioavailability; cyclosporine; quercetin; rutin; P-gp; CYP 3A4
资金
- National Science Council, Republic of China (NSC) [NSC 99-2320-B-039-017-MY3, NSC99-2628-B-039-005-MY3]
- Taiwan Department of Health Clinical Trial and Research Center of Excellence [DOH100-TD-B-111-004]
- China Medical University, Taichung, Taiwan, Republic of China [CMU98-S-34, CMU98-S-32]
Quercetin and rutin are popular flavonoids in plant foods, herbs, and dietary supplements. Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). This study investigated the effects of quercetin and rutin on CSP pharmacokinetics from Neoral and relevant mechanisms. Rats were orally administered Neoral with and without quercetin or rutin. The blood CSP concentration was assayed by a specific monoclonal fluorescence polarization immunoassay. The results showed that quercetin and rutin significantly decreased the C-max of CSP by 67.8 and 63.2% and reduced the AUC(0-540) by 43.3 and 57.2%, respectively. The in vitro studies indicated that the quercetin and rutin induced the functions of P-gp and CYP3A4. In conclusion, quercetin and rutin decreased the bioavailability of CSP through activating P-gp and CYP3A. Transplant patients treated with Neoral should avoid concurrent consumption of quercetin or rutin to minimize the risk of allograft rejection.
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