Bioavailability, disposition, and dose-response effects of soy isoflavones when consumed by healthy women at physiologically typical dietary intakes
Bioavailability, disposition, and dose-response effects of soy isoflavones when consumed by healthy women at physiologically typical dietary intakes
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DOI：
10.1093/jn/133.4.1027
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发表时间：
2003-04-01
影响因子：
4.2
通讯作者：
Heubi, JE
中科院分区：
文献类型：
--
作者：
Setchell, KDR;Brown, NM;Heubi, JE
10 名健康女性中异黄酮的药代动力学是通过单次推注摄入 10、20 或 40 g 大豆坚果后的血清出现/消失浓度曲线和尿排泄来确定的，其中提供了越来越多的缀合形式的大豆黄酮（6.6、13.2 和 26.4 mg）和染料木黄酮（9.8、19.6 和 39.2 mg）。 4-8 小时后，血清黄豆苷元和染料木黄酮浓度达到峰值，消除半衰期分别为 8.0 和 10.1 小时。绝经前和绝经后妇女之间大豆黄酮和染料木黄酮的药代动力学没有差异，表明异黄酮的吸收和处置与年龄或绝经状态无关。观察到大豆黄酮和染料木黄酮的生物利用度之间存在曲线关系，从血清浓度-时间曲线的曲线下面积至无穷大(AUC(inf))和摄入的异黄酮的量明显可见。当以给药剂量的百分比表示时，尿液中排泄的异黄酮的平均分数随着摄入量的增加而减少（大豆苷元分别为 63.2 +/- 8.0、54.4 +/- 8.1 和 44.0 +/- 4.3%，相应地，大豆苷元为 25.2 +/- 5.3、13.4 +/- 2.1 和 15.8 +/- 2.7%）金雀异黄素），强调了非线性药代动力学的趋势。雌马酚被确定为 30% 女性的代谢物；它始终存在于同一受试者的尿液和血液中。其延迟出现与结肠合成一致。根据药代动力学，最佳稳态血清异黄酮浓度预计来自每天定期食用的适量大豆食品，而不是来自单一高度浓缩的产品。
The pharmacokinetics of isoflavones in 10 healthy women were determined from serum appearance/disappearance concentration profiles and urinary excretions after single-bolus ingestion of 10, 20 or 40 g of soy nuts delivering increasing amounts of the conjugated forms of daidzein (6.6, 13.2 and 26.4 mg) and genistein (9.8, 19.6 and 39.2 mg). Peak serum daidzein and genistein concentrations were attained after 4-8 h, and elimination half-lives were 8.0 and 10.1 h, respectively. There were no differences in the pharmacokinetics of daidzein and genistein between pre- and postmenopausal women, indicating absorption and disposition of isoflavones to be independent of age or menopausal status. A curvilinear relationship was observed between the bioavailability of daidzein and genistein, apparent from the area under the curve to infinity (AUC(inf)) of the serum concentration-time profiles and the amount of isoflavones ingested. The mean fraction of the isoflavones excreted in urine decreased with increasing intake when expressed as a percentage of the administered dose (63.2 +/- 8.0, 54.4 +/- 8.1 and 44.0 +/- 4.3%, respectively, for daidzein, and correspondingly, 25.2 +/- 5.3, 13.4 +/- 2.1 and 15.8 +/- 2.7% for genistein), underscoring the trend toward nonlinear pharmacokinetics. Equol was identified as a metabolite in 30% of women; it was present consistently in urine and blood from the same subjects. Its delayed appearance was consistent with colonic synthesis. On the basis of the pharmacokinetics, optimum steady-state serum isoflavone concentrations would be expected from modest intakes of soy foods consumed regularly throughout the day rather than from a single highly enriched product.