Wu Ming-Jiang, Wu Xiao-Lei, Zhang De-Qin, Qiu Feng, Ding Li-Qin, Ma Hao-Ling, Chen Xin-Ze
Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Department of Pharmacy, Zunyi Medical and Pharmaceutical College, Guizhou Province, Zunyi, China.
Biomed Chromatogr. 2017 Dec;31(12). doi: 10.1002/bmc.4016. Epub 2017 Jul 4.
Quercetin, a kind of major flavonoid found in many traditional chinese medicines, is an effective substance for treatments such as lowering blood lipids. However, the studies on quercetin have been mainly focused on its pharmacological effect; the treatment of diseases on a material basis, particularly the metabolites derived from quercetin in vivo, has not been evaluated. In this study, we determined the levels, distributions and types of quercetin's metabolites in plasma, urine, feces and bile of rats after a single oral administration of quercetin at a dose of 80 mg/kg, using ultra-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF/MS). A total of 36 metabolites of quercetin were identified, including 11 metabolites in plasma, 34 metabolites in urine, 12 metabolites in feces and 21 metabolites in bile. The results showed that phase I metabolites were reduction metabolites and phase II metabolites mainly included glucuronidation, sulfation and methylation metabolites. These results provide important information on the metabolism of quercetin, which will be helpful for its further development and utilization.
槲皮素是许多传统中药中发现的一种主要黄酮类化合物，是一种有效的降血脂等治疗物质。然而，对槲皮素的研究主要集中在其药理作用上；基于物质基础的疾病治疗，特别是槲皮素在体内的代谢产物，尚未得到评估。在本研究中，我们使用超高效液相色谱/四极杆-飞行时间质谱（UPLC-Q-TOF/MS），在大鼠单次口服80mg/kg剂量的槲皮素后，测定了其在血浆、尿液、粪便和胆汁中的代谢产物水平、分布和类型。共鉴定出36种槲皮素代谢产物，包括血浆中的11种代谢产物、尿液中的34种代谢产物、粪便中的12种代谢产物和胆汁中的21种代谢产物。结果表明，I相代谢产物为还原代谢产物，II相代谢产物主要包括葡萄糖醛酸化、硫酸化和甲基化代谢产物。这些结果为槲皮素的代谢提供了重要信息，将有助于其进一步开发和利用。
