Different Profiles of Quercetin Metabolites in Rat Plasma: Comparison of Two Administration Methods
Different Profiles of Quercetin Metabolites in Rat Plasma: Comparison of Two Administration Methods
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DOI：
10.1271/bbb.80516
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发表时间：
2009-03-01
影响因子：
1.6
通讯作者：
Terao, Junji
中科院分区：
文献类型：
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作者：
Kawai, Yoshichika;Saito, Satomi;Terao, Junji
多酚类化合物在人体和啮齿类动物中的生物利用度已就其生物活性进行了讨论。我们发现不同的代谢产物谱槲皮素在大鼠血浆之间的两个给药程序。单次胃内给药（50 mg/kg）导致血浆中出现多种代谢物，而通过自由进入仅检测到大部分代谢物（1%槲皮素）。自由使用组的甲基化/非甲基化代谢物比率要高得多。质谱分析表明，从自由获取的馏分中含有高度共轭的槲皮素代谢产物，如槲皮素和甲基槲皮素的磺基葡萄糖醛酸苷。摄入洋葱后人体血浆中的代谢产物谱与大鼠灌胃给药后的代谢产物谱相似。人低密度脂蛋白体外氧化实验表明，槲皮素儿茶酚部分的甲基化显著减弱了其抗氧化活性。这些结果可为槲皮素的生物利用度研究提供参考。
The bioavailability of polyphenols in human and rodents has been discussed regarding their biological activity. We found different metabolite profiles of quercetin in rat plasma between two administration procedures. A single intragastric administration (50 mg/kg) resulted in the appearance of a variety of metabolites in the plasma, whereas only a major fraction was detected by free access (1% quercetin). The methylated/non-methylated metabolites ratio was much higher in the free access group. Mass spectrometric analyses showed that the fraction from free access contained highly conjugated quercetin metabolites such as sulfo-glucuronides of quercetin and methylquercetin. The metabolite profile of human plasma after an intake of onion was similar to that with intragastric administration in rats. In vitro oxidation of human low-density lipoprotein showed that methylation of the catechol moiety of quercetin significantly attenuated the antioxidative activity. These results might provide information about the bioavailability of quercetin when conducting animal experiments.