槲皮素衍生物的合成及生物活性研究进展

综述了槲皮素衍生物的合成及生物活性研究进展,介绍了国内外槲皮素氨基酸类、糖苷类、酯类、醚类衍生物及金属配合物的合成方法及其生物活性研究现状.指出槲皮素是一种从天然植物中提取的黄酮醇类化合物,具有抗氧化,抗菌,扩张血管,抗肿瘤及抗突变等多种生物学活性.然而,槲皮素具有水溶性差、生物利用度较低等缺点,临床应用受到限制.为此,国内外学者对其结构进行修饰改造,开发出了一系列具有新颖结构的槲皮素先导化合物,可望为新型槲皮素衍生物的设计合成提供参考.

Research progress of synthesis and biological activity of quercetin derivatives

A review is provided of the progress of research on the synthesis and biological activity of quercetin derivatives.The methods for preparing quercetin amino acids,glycosides,esters,ethers derivatives and metal complexes as well as the current status of study on the biological activities of those derivatives are briefed.It is pointed out that,as a kind of flavonol compound extracted from natural plants,quercetin has many biological activities such as antioxidant,antibacterial,antihyper-tensive,anti-tumor and anti-mutation.However,the poor water solubility and low bioavailability of quercetin limit its clinical application.Therefore,domestic and foreign scholars have made efforts to modify the structure of quercetin and developed a series of novel lead compounds of quercetin,which,hopefully,is to provide references for the design and synthesis of novel quercetin derivatives.