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大鼠灌注小肠中白藜芦醇生物利用度的评估。

Assessment of resveratrol bioavailability in the perfused small intestine of the rat.

作者信息

Andlauer W, Kolb J, Siebert K, Fürst P

机构信息

Institute for Biological Chemistry and Nutrition, University of Hohenheim, Stuttgart, Germany.

出版信息

Drugs Exp Clin Res. 2000;26(2):47-55.

PMID:10894555
Abstract

Resveratrol, which is present in grapes, wine and peanuts, is believed to possess chemoprotective properties such as anticarcinogenic effects and to provide protection against cardiovascular diseases. Little is known, however, about its intestinal absorption. We investigated the absorption and metabolism of resveratrol by using an isolated preparation of luminally and vascularly perfused rat small intestine. A synthetic perfusate free from blood components was used as vascular medium with a perfluorocarbon as oxygen carrier. Luminal media consisted of a bicarbonate buffered sodium chloride solution spiked with resveratrol in physiological, nutritionally relevant concentrations (28, 34 and 57 micromol/l, respectively). Viability was maintained during the entire perfusion and no significant differences between resveratrol and control perfusions for oxygen consumption, arterial pressure, lactate-pyruvate ratio and acid-base homeostasis were observed. Vascular uptake of luminally administered resveratrol was 20.5%. The majority of the absorbed resveratrol was conjugated to yield resveratrol glucuronide (16.8%), which was also the main luminal metabolite (11.2%). Lesser amounts of resveratrol sulfate, 3.0% and 0.3%, were found on the luminal and vascular side, respectively, while only minute amounts of resveratrol and resveratrol conjugates (1.9%) were found in the intestinal tissue. The structures of the resveratrol conjugates were verified by liquid chromatography coupled with mass spectometry (LC-MS). The results demonstrate an ample uptake and metabolic conversion of resveratrol. The proposed perfusion model serves as a tool to evaluate intestinal absorption and metabolic handling of phytochemicals, a pertinent input to the ongoing discussion about their health benefits.

摘要

白藜芦醇存在于葡萄、葡萄酒和花生中,被认为具有化学保护特性,如抗癌作用,并能预防心血管疾病。然而,人们对其肠道吸收情况知之甚少。我们使用离体的经腔内和血管灌注的大鼠小肠制剂,研究了白藜芦醇的吸收和代谢。一种不含血液成分的合成灌注液被用作血管介质,全氟碳化合物作为氧载体。腔内介质由添加了生理相关营养浓度(分别为28、34和57微摩尔/升)白藜芦醇的碳酸氢盐缓冲氯化钠溶液组成。在整个灌注过程中维持了活力,并且在白藜芦醇灌注和对照灌注之间,未观察到耗氧量、动脉压、乳酸 - 丙酮酸比值和酸碱平衡的显著差异。腔内给予的白藜芦醇的血管摄取率为20.5%。大部分吸收的白藜芦醇被结合生成白藜芦醇葡萄糖醛酸苷(16.8%),这也是主要的腔内代谢产物(11.2%)。分别在腔内和血管侧发现少量的硫酸白藜芦醇,含量为3.0%和0.3%,而在肠组织中仅发现微量的白藜芦醇及其结合物(1.9%)。通过液相色谱 - 质谱联用(LC - MS)验证了白藜芦醇结合物的结构。结果表明白藜芦醇有充足的摄取和代谢转化。所提出的灌注模型可作为评估植物化学物质肠道吸收和代谢处理的工具,为正在进行的关于其健康益处的讨论提供相关依据。

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