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健康人体中白藜芦醇代谢产物谱在适量饮用红酒和葡萄提取物片后的药代动力学。

Pharmacokinetics of resveratrol metabolic profile in healthy humans after moderate consumption of red wine and grape extract tablets.

机构信息

Nutrition and Food Science Department, XaRTA-INSA, Pharmacy Faculty, University of Barcelona, Av Joan XXIII, s/n, Barcelona, Spain.

出版信息

Pharmacol Res. 2012 Nov;66(5):375-82. doi: 10.1016/j.phrs.2012.08.001. Epub 2012 Aug 10.

DOI:10.1016/j.phrs.2012.08.001
PMID:22906730
Abstract

A pharmacokinetic study of the metabolic profile of resveratrol has been performed in healthy men after moderate red wine (RW) consumption. The bioavailability of resveratrol is highly influenced by several factors such as the food matrix and, therefore, this study has been compared with a pilot study in which men ingested grape extract (GE) tablets as a nutraceutical, containing similar total amounts of resveratrol than RW. Blood and urine samples were taken before and at several time points after intervention and then analyzed by SPE and LC-ESI-MS/MS. Up to 17 resveratrol and piceid derivatives were identified, including those formed by the intestinal microbiota. Resveratrol glucosides were found in plasma as intact forms and reached the lowest maximum concentrations 1h after both interventions. Higher plasma concentrations and longer times (t(max)) were observed for resveratrol glucuronides due to phase II metabolism and even higher values for conjugates derived from microbiota, such as dihydroresveratrol-glucuronides. The same trend was observed for total excreted amounts in urine samples. When both treatments were compared, statistically significant differences for some metabolites were obtained, which may be due to the different composition of resveratrol and piceid in both sources. However, GE formulation seems to delay resveratrol absorption, staying longer in the gut where could be metabolized to a greater degree, since 2.1-3.6-fold higher urinary concentrations of microbial metabolites were observed after GE intervention at 12-24h urinary fraction. Therefore, supplement intake could be also a way to bring resveratrol benefits to human health.

摘要

在健康男性中进行了一项关于白藜芦醇代谢谱的药代动力学研究,这些男性在摄入适量红葡萄酒(RW)后。白藜芦醇的生物利用度受到多种因素的影响,如食物基质,因此,这项研究与一项初步研究进行了比较,该研究中男性摄入了含有与 RW 相似总量白藜芦醇的葡萄提取物(GE)片作为营养补充剂。在干预前后的不同时间点采集血液和尿液样本,然后通过 SPE 和 LC-ESI-MS/MS 进行分析。共鉴定出 17 种白藜芦醇和白皮杉醇衍生物,包括由肠道微生物群形成的衍生物。白藜芦醇糖苷以完整形式存在于血浆中,在两种干预后 1 小时达到最低的最大浓度。由于 II 期代谢,白藜芦醇葡萄糖苷在血浆中的浓度更高,时间更长(t(max)),甚至对于源自微生物群的共轭物,如二氢白藜芦醇葡萄糖苷,其值更高。尿液样本中总排泄量也观察到相同的趋势。当比较两种处理方法时,一些代谢物的浓度存在统计学差异,这可能是由于两种来源中白藜芦醇和白皮杉醇的组成不同。然而,GE 配方似乎会延迟白藜芦醇的吸收,在肠道中停留更长时间,在那里可以被更大程度地代谢,因为在 GE 干预后 12-24 小时的尿液部分,微生物代谢物的尿浓度高出 2.1-3.6 倍。因此,补充剂的摄入也可能是为人类健康带来白藜芦醇益处的一种方式。

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