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食用单剂量开环异落叶松脂醇二葡萄糖苷的健康男性和女性中肠木脂素的药代动力学。

Pharmacokinetics of enterolignans in healthy men and women consuming a single dose of secoisolariciresinol diglucoside.

作者信息

Kuijsten Anneleen, Arts Ilja C W, Vree Tom B, Hollman Peter C H

机构信息

RIKILT-Institute of Food Safety, Wageningen UR, 6700 AE Wageningen, The Netherlands.

出版信息

J Nutr. 2005 Apr;135(4):795-801. doi: 10.1093/jn/135.4.795.

Abstract

High concentrations of enterolignans in plasma are associated with a lower risk of acute coronary events. However, little is known about the absorption and excretion of enterolignans. The pharmacokinetic parameters and urinary excretion of enterodiol and enterolactone were evaluated after consumption of their purified plant precursor, secoisolariciresinol diglucoside (SDG). Twelve healthy volunteers ingested a single dose of purified SDG (1.31 micromol/kg body wt). Enterolignans appeared in plasma 8-10 h after ingestion of the purified SDG. Enterodiol reached its maximum plasma concentration 14.8 +/- 5.1 h (mean +/- SD) after ingestion of SDG, whereas enterolactone reached its maximum 19.7 +/- 6.2 h after ingestion. The mean elimination half-life of enterodiol (4.4 +/- 1.3 h) was shorter than that of enterolactone (12.6 +/- 5.6 h). The mean area under the curve of enterolactone (1762 +/- 1117 nmol/L . h) was twice as large as that of enterodiol (966 +/- 639 nmol/L . h). The mean residence time for enterodiol was 20.6 +/- 5.9 h and that for enterolactone was 35.8 +/- 10.6 h. Within 3 d, up to 40% of the ingested SDG was excreted as enterolignans via urine, with the majority (58%) as enterolactone. In conclusion, a substantial part of enterolignans becomes available in the blood circulation and is subsequently excreted. The measured mean residence times and elimination half-lives indicate that enterolignans accumulate in plasma when consumed 2-3 times a day and reach steady state. Therefore, plasma enterolignan concentrations are expected to be good biomarkers of dietary lignan exposure and can be used to evaluate the effects of lignans.

摘要

血浆中高浓度的肠内酯与较低的急性冠状动脉事件风险相关。然而,关于肠内酯的吸收和排泄情况却知之甚少。在摄入其纯化的植物前体开环异落叶松树脂酚二葡萄糖苷(SDG)后,对肠二醇和肠内酯的药代动力学参数及尿排泄情况进行了评估。12名健康志愿者单次摄入纯化的SDG(1.31微摩尔/千克体重)。摄入纯化的SDG后8 - 10小时,血浆中出现肠内酯。摄入SDG后,肠二醇在14.8±5.1小时(平均值±标准差)达到其最大血浆浓度,而肠内酯在摄入后19.7±6.2小时达到最大值。肠二醇的平均消除半衰期(4.4±1.3小时)短于肠内酯(12.6±5.6小时)。肠内酯的平均曲线下面积(1762±1117纳摩尔/升·小时)是肠二醇(966±639纳摩尔/升·小时)的两倍。肠二醇的平均驻留时间为20.6±5.9小时,肠内酯的平均驻留时间为35.8±10.6小时。在3天内,高达40%摄入的SDG以肠内酯形式通过尿液排泄,其中大部分(58%)为肠内酯。总之,相当一部分肠内酯在血液循环中可用,随后被排泄。所测得的平均驻留时间和消除半衰期表明,当每天摄入2 - 3次时,肠内酯会在血浆中蓄积并达到稳态。因此,可以预期血浆肠内酯浓度将是膳食木脂素暴露的良好生物标志物,并可用于评估木脂素的作用。

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