Involvement of Breast Cancer Resistance Protein (BCRP1/ABCG2) in the Bioavailability and Tissue Distribution of trans-Resveratrol in Knockout Mice

被引：43

作者：

Alfaras, Irene ^{[2
,3
]}

Perez, Miriam ^{[1
]}

Emilia Juan, Maria ^{[2
,3
]}

Merino, Gracia ^{[4
]}

Gabriel Prieto, Julio ^{[1
]}

Maria Planas, Joana ^{[2
,3
]}

Alvarez, Isabel ^{[1
]}

机构：

[1] Univ Leon, Area Fisiol, Dept Ciencias Biomed, E-24071 Leon, Spain

[2] Univ Barcelona, Grp Fisiol & Nutr Expt, Dept Fisiol Farm, E-08028 Barcelona, Spain

[3] Univ Barcelona, Inst Recerca Nutr & Seguretat Alimentaria INSA, E-08028 Barcelona, Spain

[4] Univ Leon, Inst Sanidad Anim & Desarrollo Ganadero, E-24071 Leon, Spain

来源：

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY | 2010年 / 58卷 / 07期

关键词：

Bioavailability; Bcrp1(-/-) mice; distribution; HPLC-DAD; trans-resveratrol; GLUCURONIDE METABOLITES; DIETARY RESVERATROL; BILIARY-EXCRETION; RAT MODEL; BCRP/ABCG2; SULFATE; ABCG2; PHARMACOKINETICS; MITOXANTRONE; DISPOSITION;

D O I：

10.1021/jf9042858

中图分类号：

S [农业科学];

学科分类号：

09 ;

摘要：

trans-Resveratrol undergoes extensive metabolism in the intestinal cells, which leads to the formation of glucuronide and sulfate conjugates. Given the important role of the breast cancer resistance protein (ABCG2/BCRP) in the efflux of conjugated forms, the present study investigates the bioavailability and tissue distribution of trans-resveratrol and its metabolites after the oral administration of 60 mg/kg in Bcrp1(-/-) mice. trans-Resveratrol and its metabolites were measured in intestinal content, plasma and tissues by HPLC. At 30 min after administration, intestinal content showed decreases of 71% and 97% of resveratrol glucuronide and sulfate, respectively, in Bcrp1(-/-), indicating a lower efflux from the enterocytes. Furthermore, the area under plasma concentration curves (AUC) of these metabolites increased by 34% and 392%, respectively, whereas a decrease in the AUC of trans-resveratrol was found. In conclusion, Bcrp1 plays an important role in the efflux of resveratrol conjugates, contributing to their bioavailability, tissue distribution and elimination.

引用

页码：4523 / 4528

页数：6

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