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首页> 外文期刊>Life sciences >Quercetin significantly decreased cyclosporin oral bioavailability in pigs and rats.
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Quercetin significantly decreased cyclosporin oral bioavailability in pigs and rats.

机译：槲皮素显着降低猪和大鼠中环孢菌素的口服生物利用度。

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Cyclosporin, an immunosuppressant with a narrow therapeutic window, is a substrate for both CYP3A4 and P-glycoprotein (Pgp). Quercetin is an inhibitor of CYP3A4 and a modulator of Pgp. This study aimed to measure the effect of quercetin on the absorption and disposition of cyclosporin in pigs and rats. Cyclosporin (Sandimmune(R), 10 mg/kg) was orally administered with and without a concomitant dose of quercetin (50 mg/kg) to pigs and rats. Cyclosporin concentrations in blood samples were determined by a specific monoclonal fluorescence polarization immunoassay. The pharmacokinetic parameters were calculated by noncompartmental analysis using WINNONLIN. A paired Student's t-test was conducted for statistical comparison. A study using the everted intestinal sac was carried out to evaluate the effect of quercetin on the function of intestinal Pgp. The coadministration of quercetin significantly decreased cyclosporin AUC(0-3) (area under the concentration-time curve from time zero to 3 h) by 56% and AUC(0-t) (area under the concentration-time curve from time zero to the last point) by 43% in pigs and rats, respectively, indicating that the coadministration of quercetin significantly decreased cyclosporin oral bioavailability. However, the inverted sac study showed that quercetin significantly inhibited the function of intestinal Pgp. It is suggested that concurrent use of quercetin or quercetin-containing dietary supplement or herbs with cyclosporin or other medications whose absorption and metabolism are mediated by Pgp and/or CYP3A4 should require close monitoring.
机译：环孢霉素是一种治疗窗口狭窄的免疫抑制剂，是CYP3A4和P-糖蛋白（Pgp）的底物。槲皮素是CYP3A4的抑制剂和Pgp的调节剂。这项研究旨在测量槲皮素对猪和大鼠中环孢菌素的吸收和处置的影响。向猪和大鼠口服环孢菌素（10mg / kg，口服和不伴槲皮素（50mg / kg））。血样中环孢菌素的浓度通过特定的单克隆荧光偏振免疫分析法测定。使用WINNONLIN通过非房室分析来计算药代动力学参数。进行配对的学生t检验以进行统计比较。进行了一项使用外翻小肠囊的研究，以评估槲皮素对肠道Pgp功能的影响。槲皮素的共同给药使环孢菌素AUC（0-3）（从时间零到3小时的浓度-时间曲线下的面积）和AUC（0-t）（从时间零到3h的浓度-时间曲线下的面积）降低了56％。最后一点）在猪和大鼠中分别降低了43％，这表明槲皮素的共同给药显着降低了环孢菌素的口服生物利用度。但是，倒囊研究表明槲皮素显着抑制肠道Pgp的功能。建议同时使用槲皮素或含槲皮素的膳食补充剂或草药与环孢菌素或其他吸收和代谢由Pgp和/或CYP3A4介导的药物时，应密切监测。

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