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.