Pharmacokinetics, tissue distribution and excretion study of resveratrol and its prodrug 3,5,4′-tri-O-acetylresveratrol in rats

被引：79

作者：

Liang, Li ^{[1
]}

Liu, Xueying ^{[1
]}

Wang, Qingwei ^{[2
]}

Cheng, Sikun ^{[1
]}

Zhang, Shengyong ^{[1
]}

Zhang, Meng ^{[3
]}

机构：

[1] Fourth Mil Med Univ, Sch Pharm, Dept Med Chem & Pharmaceut Anal, Xian 710032, Peoples R China

[2] Fourth Mil Med Univ, Affiliated Hosp 2, Dept Pharm, Xian 710032, Peoples R China

[3] Fourth Mil Med Univ, Inst Mat Med, Sch Pharm, Xian 710032, Peoples R China

来源：

PHYTOMEDICINE | 2013年 / 20卷 / 06期

基金：

中国国家自然科学基金;

关键词：

3,5,4 '-Tri-O-acetylresveratrol; Resveratrol; Pharmacokinetics; Tissue distribution; Excretion; HPLC; TRANS-RESVERATROL; METABOLISM;

D O I：

10.1016/j.phymed.2012.12.012

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

3,5,4'-Tri-O-acetylresveratrol (TARES) synthesized by acetylating three hydroxyl groups of resveratrol (RES) is a prodrug of RES. The aim of this study was to investigate and compare the pharmacokinetics, tissue distribution and excretion of TARES and RES in rats following a single intragastric gavage (i.g.) administration. After RES is transformed into TARES, its pharmacokinetic properties are improved, such as the t(1/2) has been prolonged and the AUC has been enhanced. And TARES follows linear plasma pharmacokinetics across the investigated dosage range in rats (77.5-310 mg/kg). The major distribution tissues of TARES or RES in rats were liver, spleen, heart and lung. TARES can increase the content of RES in lung significantly. There was no long-term accumulation of RES in rat tissues. Whether we administrated to rats of equimolar TARES or RES, total recoveries of RES in urine and feces within 36 h were low (0.99% or 0.07% in urine and 1.69% or 0.15% in feces). (C) 2012 Elsevier GmbH. All rights reserved.

引用

页码：558 / 563

页数：6

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