Vitrac Xavier, Desmoulière Alexis, Brouillaud Brigitte, Krisa Stéphanie, Deffieux Gérard, Barthe Nicole, Rosenbaum Jean, Mérillon Jean Michel
Laboratoire de Mycologie et Biotechnologie Végétale, EA 491, Université de Bordeaux 2, 146, rue Léo Saignat, 33076 Bordeaux Cedex, France.
Life Sci. 2003 Apr 4;72(20):2219-33. doi: 10.1016/s0024-3205(03)00096-1.
Trans-resveratrol, a phenolic compound present in wine, has been reported to be a potential cancer chemopreventive agent. However, although it has numerous biological activities in vitro, there are few data about its bioavailability and tissue distribution in vivo. The objectives of this study were to investigate the absorption and tissue distribution of 14C-trans-resveratrol following oral administration to mice. Male Balb/c mice were given a single oral dose of 14C-trans-resveratrol and were sacrificed at 1.5, 3 or 6 h postdose. The distribution of radioactivity in tissues was evaluated using whole-body autoradiography, quantitative organ-level determination and microautoradiography. In addition, identification of radioactive compounds in kidney and liver was done with high-performance liquid chromatography. Autoradiographic survey of mice sections as well as radioactivity quantification in various organs revealed a preferential fixation of 14C-trans-resveratrol in the organs and biological liquids of absorption and elimination (stomach, liver, kidney, intestine, bile, urine). Moreover, we show that 14C-trans-resveratrol derived radioactivity is able to penetrate the tissues of liver and kidney, a finding supported by microautoradiography. The presence of intact 14C-trans-resveratrol together with glucurono- and/or sulfoconjugates in these tissues was also shown. This study demonstrates that trans-resveratrol is bioavailable following oral administration and remains mostly in intact form. The results also suggest a wide range of target organs for cancer chemoprevention by wine polyphenols in humans.
反式白藜芦醇是一种存在于葡萄酒中的酚类化合物,据报道它是一种潜在的癌症化学预防剂。然而,尽管它在体外具有多种生物活性,但关于其体内生物利用度和组织分布的数据却很少。本研究的目的是调查口服给予小鼠14C-反式白藜芦醇后的吸收和组织分布情况。给雄性Balb/c小鼠单次口服一剂14C-反式白藜芦醇,并在给药后1.5、3或6小时处死。使用全身放射自显影、定量器官水平测定和显微放射自显影来评估组织中的放射性分布。此外,用高效液相色谱法对肾脏和肝脏中的放射性化合物进行鉴定。对小鼠切片的放射自显影检查以及各器官中的放射性定量分析表明,14C-反式白藜芦醇优先在吸收和排泄的器官及生物液体(胃、肝脏、肾脏、肠道、胆汁、尿液)中固定。此外,我们发现14C-反式白藜芦醇衍生的放射性能够穿透肝脏和肾脏组织,这一发现得到了显微放射自显影的支持。这些组织中还显示存在完整的14C-反式白藜芦醇以及葡糖醛酸和/或硫酸酯共轭物。本研究表明,反式白藜芦醇口服后具有生物利用度,且大多保持完整形式。研究结果还表明,葡萄酒多酚在人体内对癌症化学预防具有广泛的靶器官。