Conjugated quercetin glucuronides as bioactive metabolites and precursors of aglycone in vivo.
Conjugated quercetin glucuronides as bioactive metabolites and precursors of aglycone in vivo.
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DOI：
10.1039/c0fo00106f
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发表时间：
2011-01
期刊：
影响因子：
6.1
通讯作者：
J. Terao;K. Murota;Y. Kawai
中科院分区：
文献类型：
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作者：
J. Terao;K. Murota;Y. Kawai
槲皮素是一种典型的抗氧化类黄酮，广泛存在于蔬菜中。它可能通过发挥活性氧（ROS）清除活性和/或结合信号转导途径中的特定蛋白质如氧化酶和转录因子而作为生物活性化合物。其吸收和代谢（以及其分子靶点）已从其预防疾病的潜力的角度进行了广泛的探索。已知在摄入含槲皮素的饮食后，具有或不具有O-甲基化的葡糖苷酸和/或硫酸盐结合物仅在人体血流中循环。我们建议，葡糖苷酸结合物的槲皮素功能不仅作为解毒代谢产物，但亲水性生物活性剂的各种ROS生成系统和前体的疏水糖苷配基。假设槲皮素苷元在氧化应激（如炎症）下通过β-葡萄糖醛酸苷酶活性的作用出现在靶位点。心血管系统和中枢神经系统似乎是人体血液中循环的结合槲皮素葡萄糖醛酸苷的主要靶点。
Quercetin is a typical anti-oxidative flavonoid ubiquitously distributed in vegetables. It is likely to act as a bioactive compound by exerting reactive oxygen species (ROS)-scavenging activity and/or binding to specific proteins such as oxidative enzymes and transcriptional factors in signal transduction pathways. Its absorption and metabolism (as well as its molecular targets) have been extensively explored from the viewpoint of its potential for disease prevention. It is known that glucuronide and/or sulfate conjugates with or without O-methylation exclusively circulate in the human bloodstream after intake of a quercetin-containing diet. We propose that glucuronide conjugates of quercetin function not only as detoxified metabolites but hydrophilic bioactive agents to various ROS-generating systems and precursors of hydrophobic aglycone. Quercetin aglycone is assumed to emerge in the target site by the action of β-glucuronidase activity under oxidative stress such as inflammation. The cardiovascular system and central nervous system seem to be the major targets of conjugated quercetin glucuronides circulating in the human bloodstream.