Absorption of kaempferol from endive, a source of kaempferol-3-glucuronide, in humans
Absorption of kaempferol from endive, a source of kaempferol-3-glucuronide, in humans
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DOI：
10.1038/sj.ejcn.1601916
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发表时间：
2004-06-01
影响因子：
4.7
通讯作者：
Kroon, PA
中科院分区：
文献类型：
--
作者：
DuPont, MS;Day, AJ;Kroon, PA
目的：研究山奈酚在人体内的吸收、排泄和代谢。设计：健康男性和健康女性各4名。结果：山奈酚的吸收剂量较低(9 Mg)，平均最大血药浓度为0.1um，平均血药浓度为5.8h，表明山奈酚在小肠和/或结肠远端吸收。虽然观察到最高血药浓度和最低血药浓度之间的个体间差异是7.5倍，但大多数个体表现出非常一致的药动学特征。这与其他主要从大肠吸收的黄酮类化合物(如芦丁)的分布形成了鲜明对比。山奈酚在24小时内的平均排泄量为1.9%。大多数受试者还出现了一个早期吸收峰，可能与山奈酚-3-葡萄糖苷相对应，在菊苣中的水平为14%。血浆和尿液中检出的主要成分为山奈酚-3-葡萄糖醛酸苷。在血浆和尿液中均未检测到槲皮素，说明山奈酚缺乏I相羟基化。结论：山奈酚在人体内的吸收效率高于槲皮素，即使在低剂量口服时也是如此。血浆中的主要形式是3-葡萄糖醛酸偶联物，吸收和排泄的个体间差异很小，这表明尿山奈酚可以作为暴露的生物标志物。
Objective: To determine the absorption, excretion and metabolism of kaempferol in humans.Design: A pharmacokinetic study of kaempferol from endive over 24 h. Subjects: Four healthy males and four healthy females.Results: Kaempferol, from a relatively low dose ( 9 mg), was absorbed from endive with a mean maximum plasma concentration of 0.1 muM, at a time of 5.8 h, indicating absorption from the distal section of the small intestine and/or the colon. Although a 7.5-fold interindividual variation between the highest and lowest maximum plasma concentration was observed, most individuals showed remarkably consistent pharmacokinetic profiles. This contrasts with profiles for other flavonoids that are absorbed predominantly from the large intestine (eg rutin). An average of 1.9% of the kaempferol dose was excreted in 24 h. Most subjects also showed an early absorption peak, probably corresponding to kaempferol-3-glucoside, present at a level of 14% in the endive. Kaempferol-3-glucuronide was the major compound detected in plasma and urine. Quercetin was not detected in plasma or urine indicating a lack of phase I hydroxylation of kaempferol.Conclusions: Kaempferol is absorbed more efficiently than quercetin in humans even at low oral doses. The predominant form in plasma is a 3-glucuronide conjugate, and interindividual variation in absorption and excretion is low, suggesting that urinary kaempferol could be used as a biomarker for exposure.Sponsorship: Biotechnology and Biological Sciences Research council for core strategic funding and the University of Leeds for a departmental fellowship (AJD).