Part of quercetin absorbed in the small intestine is conjugated and further secreted in the intestinal lumen
Part of quercetin absorbed in the small intestine is conjugated and further secreted in the intestinal lumen
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DOI：
10.1152/ajpgi.1999.277.1.g120
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发表时间：
1999-07-01
影响因子：
4.5
通讯作者：
Remesy, C
中科院分区：
文献类型：
--
作者：
Crespy, V;Morand, C;Remesy, C
采用大鼠空肠+回肠原位灌流（15 nmol/min），观察大黄素和槲皮素的吸收和代谢。与芦丁相反，高比例的槲皮素（三分之二）在灌注过程中消失，反映了广泛的转移到肠壁。净槲皮素吸收不完全（2.1 nmol/min），因为52%在管腔中以共轭衍生物形式再排泄（7.7 nmol/min）。通过灌注前胆管插管排除类黄酮的肝肠循环贡献。在30分钟的灌注期后，在血浆中检测到0.71 μ M的槲皮素当量，反映了小肠的显著吸收。通过葡萄糖醛酸酶和/或硫酸酯酶对流出物样品的差异水解表明，在管腔中释放的缀合形式是1）槲皮素及其甲氧基化形式的葡萄糖醛酸化衍生物（64%）和2）槲皮素的硫酸化形式（36%）。在体外槲皮素葡萄糖醛酸苷合成使用空肠和回肠微粒体馏分中回收的灌注流出物中的相似。这些数据表明，葡萄糖醛酸化和硫代硫酸盐发生在肠细胞，而没有葡萄糖醛酸-磺基共轭物可以检测到的流出物。目前的工作表明，槲皮素在小肠中的快速吸收与其在肠细胞中的活性结合一起是非常有效的。
Rutin and quercetin absorption and metabolism were investigated in rats after in situ perfusion of jejunum plus ileum (15 nmol/min). In contrast to rutin, a high proportion of quercetin (two-thirds) disappeared during perfusion, reflecting extensive transfer into the intestinal wall. Net quercetin absorption was not complete (2.1 nmol/min), inasmuch as 52% were reexcreted in the lumen as conjugated derivatives (7.7 nmol/min). Enterohepatic recycling contribution of flavonoids was excluded by catheterization of the biliary duct before perfusion. After a 30-min perfusion period, 0.71 mu M of quercetin equivalents were detected in plasma, reflecting a significant; absorption from the small intestine. The differential hydrolysis of effluent samples by glucuronidase and/or sulfatase indicates that the conjugated forms released in the lumen were 1) glucuronidated derivatives of quercetin and of its methoxylated forms (64%) and 2) sulfated form of quercetin (36%). In vitro quercetin glucuronides synthetized using jejunal and ileal microsomal fractions were similar to those recovered in the effluent of perfusion. These data suggest that glucuronidation and sulfatation take place in intestinal cells, whereas no glucurono-sulfoconjugates could be detected in the effluent. The present work shows that a rapid quercetin absorption in the small intestine is very effective together with its active conjugation in intestinal cells.