槲皮素化学修饰与体内转运过程研究进展  

Research Progress in Chemical Modification and in Vivo Transit Process of Quercetin

作　　者：彭游[1,2,3] 付小兰[1,3] 陶春元[1,3] 邓泽元[2] 

机构地区：[1]九江学院化学化工学院,九江332005 [2]南昌大学食品科学与技术国家重点实验室,南昌330047 [3]江西省鄱阳湖生态经济研究中心,江西九江332005

出　　处：《天然产物研究与开发》2012年第3期398-405,共8页Natural Product Research and Development

基　　金：江西省教育厅科技课题(GJJ11626);江西省自然科学基金(2010GZN0106);国家自然科学基金(81160412)

摘　　要：本文综述了槲皮素的化学修饰和药代动力学等方面的研究进展,为槲皮素的前药分子设计、寻找活性化合物提供科学依据。文献合成的目标产物主要包括槲皮素糖苷等水溶性产物和槲皮素磺酸酯等脂溶性产物,迄今仍未找到药理作用明显,能临床运用的槲皮素修饰物。文献表明槲皮素生物活性低是由于其低的生物利用度,溶解性差与首过效应是影响其生物利用度的主要因素。The recent advance of quereetin in the chemical modification and pharmacokinetic are reviewed in order to provide scientific envidences for searching for bioactive compounds and designing prodrug. Target products synthesised include water-soluble products such as quereetin glycosides and other oil-soluble anlfonate products in literature, but the quereetin modifier that can be clin/eally applied haven＇ t been found. Documents show that the low biological activity of quereetin is due to its low bioavailability. Poor solubility and first-pass effect are the main factors that affect its bioavail- ability.

关 键 词：槲皮素 化学修饰 前药 生物利用度 

分 类 号：O629.9[理学—有机化学]