芦丁的结构修饰及生物活性研究进展  

Research progress on structural modification and biological activity of rutin

作　　者：李珂 冯亚莉 曹瑞梅 陈虹 翟广玉 LI Ke;FENG Ya-li;CAO Rui-mei;CHEN Hong;ZHAI Guang-yu(School of Pharmacy and Chemical Engineering,Zhengzhou University of Industrial Technology,Zhengzhou 451100,China)

机构地区：[1]郑州工业应用技术学院药学与化学工程学院,河南郑州451100

出　　处：《中草药》2021年第20期6413-6424,共12页Chinese Traditional and Herbal Drugs

基　　金：河南省高等学校重点科研项目(21B350003);郑州市高等学校名师技术技能工作室(郑教高[2015]70号)。

摘　　要：芦丁是一个典型的类黄酮,主要存在于日常食用的各种中草药、水果和蔬菜中。芦丁是天然的抗氧化剂,具有广泛的药理活性,如抗炎、抗病毒、抗肿瘤、预防和治疗心脑血管疾病等作用。由于生物利用度低、水溶性差,限制了其在临床上的应用。通过对芦丁的羟基、羰基、槲皮素A、B环等优化修饰,获得了溶解性好、生物利用度高、代谢稳定和毒副作用小的醚类、酯类、配合物等芦丁衍生物。综述了近年来对芦丁结构修饰后,获得的性能优良、生物活性显著的芦丁衍生物。Rutin is a typical flavonoid, which is mainly found in various Chinese herbal medicines, fruits and vegetables. Rutin is a natural antioxidant with a wide range of pharmacological activities, such as anti-inflammatory, anti-virus, antitumor, prevention and treatment of cardiovascular and cerebrovascular diseases. Due to low bioavailability and poor water solubility, clinical application of rutin is limited. The hydroxyl, carbonyl, quercetins A and B ring of rutin were optimized and modified by to obtain rutin derivatives such as ether, ester, and complex with good solubility, high bioavailability, stable metabolism and small toxic side effects. The structural modification of rutin in recent years was reviewed in this paper, and derivatives were obtained with excellent properties and significant biological activity.

关 键 词：芦丁 结构修饰 衍生物 配合物 生物活性 

分 类 号：R282.710.5[医药卫生—中药学]