Absolute bioavailability of isoflavones from soy protein isolate-containing food in female BALB/c mice.
Absolute bioavailability of isoflavones from soy protein isolate-containing food in female BALB/c mice.
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DOI：
10.1021/jf9039843
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发表时间：
2010-04-14
影响因子：
6.1
通讯作者：
Doerge DR
中科院分区：
文献类型：
--
作者：
Andrade JE;Twaddle NC;Helferich WG;Doerge DR
大豆异黄酮、染料木黄酮和大豆苷元因其公认的健康益处而被广泛用于大豆食品和膳食补充剂中;然而，从实验动物研究中获得了潜在不良影响的证据。了解马槟榔酮药效学的一个重要前提是更好地了解药代动力学和生物利用度。本研究通过比较相同剂量给药后染料木黄酮和大豆苷元苷元及其结合形式的血浆药代动力学，确定了染料木黄酮和大豆苷元在小鼠模型中的生物利用度（1.2mg/kg染料木黄酮和0.55mg/kg大豆苷元）通过静脉内注射（IV）或管饲90%的水溶液相对于在使用商业大豆蛋白分离物（SPI）作为淀粉来源制备的食物颗粒中递送的等摩尔剂量的推注给药。染料木黄酮和大豆苷元的生物利用度是相当于管饲和饮食途径的管理，尽管使用的苷元在前者和SPI衍生的糖苷在后者。虽然两种口服途径对总黄酮的吸收几乎是定量的（IV AUC>84%），但系统前和全身II期偶联大大减弱了对受体活性苷元黄酮的内部暴露（基于IV AUC，染料木素为9-14%，大豆苷元为29-34%）。这些结果表明，SPI是一种有效的药物递送载体，能够以活性糖苷配基形式将总剂量的显著比例提供到循环中，以分布到携带受体的组织中，并随后产生确定可能的健康益处和/或风险的药理学作用。
Soy isoflavones, genistein and daidzein, are widely consumed in soy-based foods and dietary supplements for their putative health benefits; however, evidence for potential adverse effects has been obtained from experimental animal studies. An important prerequisite for understanding the pharmacodynamics of isoflavones is better information about pharmacokinetics and bioavailability. This study determined the bioavailability of genistein and daidzein in a mouse model by comparing plasma pharmacokinetics of their aglycone and conjugated forms following administration of identical doses (1.2 mg/kg genistein and 0.55 mg/kg daidzein) by either an intravenous injection (IV) or gavage of the aglycones in 90% aqueous solution vs. a bolus administration of equimolar doses delivered in a food pellet prepared using commercial soy protein isolate (SPI) as the isoflavone source. The bioavailability of genistein and daidzein were equivalent for the gavage and dietary routes of administration despite the use of isoflavone aglycones in the former and SPI-derived glucosides in the latter. While absorption of total isoflavones was nearly quantitative from both oral routes (>84% of AUCs for IV), presystemic and systemic Phase II conjugation greatly attenuated internal exposures to the receptor-active aglycone isoflavones (9–14% for genistein and 29–34% for daidzein based on AUCs for IV). These results show that SPI is an efficient isoflavone delivery vehicle capable of providing significant proportions of the total dose into the circulation in the active aglycone form for distribution to receptor-bearing tissues and subsequent pharmacological effects that determine possible health benefits and/or risks.
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影响因子：
4.3
作者：
Fukutake, M;Takahashi, M;Wakabayashi, K
通讯作者：
Wakabayashi, K
影响因子：
10.4
作者：
Jefferson, Wendy N.;Doerge, Daniel;Newbold, Retha
通讯作者：
Newbold, Retha
影响因子：
3.5
作者：
Muthyala, RS;Ju, YH;Katzenellenbogen, JA
通讯作者：
Katzenellenbogen, JA
影响因子：
4.3
作者：
McClain, RM;Wolz, E;Bausch, J
通讯作者：
Bausch, J
影响因子：
2
作者：
Lin, J;Krishnan, PG;Wang, CY
通讯作者：
Wang, CY