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

机译:适量食用红酒和葡萄提取物片剂后,白藜芦醇代谢特性在健康人体内的药代动力学

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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 1 h 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 12-24 h urinary fraction. Therefore, supplement intake could be also a way to bring resveratrol benefits to human health.
机译:食用适量的红酒(RW)后,在健康男性中进行了白藜芦醇代谢特性的药代动力学研究。白藜芦醇的生物利用度受多种因素的影响,例如食物基质,因此,该研究已与一项初步研究进行了比较,在该研究中,男性摄取了葡萄提取物(GE)片剂作为营养食品,其中白藜芦醇的总量与RW 。在干预之前和之后的几个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。最多鉴定出17种白藜芦醇和piceid衍生物,包括由肠道菌群形成的衍生物。在血浆中发现了完整形式的白藜芦醇葡萄糖苷,两种干预后1小时均达到最低的最高浓度。由于II期代谢,白藜芦醇葡糖醛酸苷的血浆浓度更高,时间更长(t max),而源自微生物群的结合物(如二氢白藜芦醇-葡糖醛酸苷)的血浆浓度更高,时间更长(t max)。尿液样本中总排泄量的趋势相同。比较两种治疗方法后,某些代谢物在统计学上有显着差异,这可能是由于两种来源中白藜芦醇和木虱的成分不同。但是,GE制剂似乎延迟了白藜芦醇的吸收,在肠道中的代谢时间更长,因为在GE干预12-24小时后,尿液中微生物代谢产物的尿液浓度升高了2.1-3.6倍。因此,补充摄入也可能是白藜芦醇有益于人体健康的一种方式。

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