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

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.