槲皮素衍生物的生物活性研究进展

Progress in Research on Biological Activity of Quercetin Derivatives

槲皮素属于黄酮类化合物,广泛存在于人们日常食用的各种蔬菜、水果和中草药中。槲皮素是天然的抗氧化剂,具有广泛的药理活性,可调节与众多疾病进展有关的细胞内和细胞外信号通路,抗炎、抗病毒、抗癌、预防和治疗心脑血管疾病。由于槲皮素的结构特征,生物利用度低,限制了其在临床上的应用。人们经过结构优化对槲皮素进行修饰,合成出了性能优良、溶解性能好、生物利用度高、代谢稳定、毒副作用小、生物活性显著的槲皮素衍生物。笔者综述了近十年来以槲皮素为先导化合物合成的槲皮素衍生物,重点介绍了这些衍生物的药理作用,如抗炎、降糖、抗癌、抗阿尔茨海默病、抗疟疾等,为天然化合物的开发和利用奠定基础。

Quercetin is a flavonoid compound,which is widely present in various vegetables,fruits and Chinese herbal medicines that people eat daily.Quercetin is a natural antioxidant and has a wide range of pharmacological activities.It can regulate the intracellular and extracellular signaling pathways related to the progression of many diseases,possessing anti-inflammatory,anti-viral,anti-cancer activities,thus can be used to prevent and treat cardiovascular and cerebrovascular diseases.Its structural characteristics and low bioavailability has limited its clinical application.Quercetin has been modified into derivatives through structural optimization with excellent performance,good solubility,high bioavailability,stable metabolism,low toxic and side effects,and significant biological activity.This article reviews the quercetin derivatives synthesized using quercetin as the lead compound in the past decade,and highlights the pharmacological effects of these derivatives,such as anti-inflammatory,effect hypoglycemic,anti-cancer,anti-Alzheimer′s disease,anti-malaria,etc.,to lay the foundation for the development and utilization of natural compounds.