熊果酸的结构修饰与生物活性研究进展

Advances in the Study of Structural Modification and Biological Activities of Ursolic Acid

熊果酸是从药用植物、水果和蔬菜中提取的具有多种药理活性的五环三萜类化合物.近年来,熊果酸的药理作用得到了广泛的研究,大量研究表明熊果酸具有多种药理活性,包括抗癌、抗炎、抗氧化、抗菌、抗糖尿病等.熊果酸虽然具有广泛的生物学活性,但其水溶性差、生物利用度低等限制了在临床上的应用.为了克服这些缺点,国内外研究人员通过对熊果酸母体骨架进行化学修饰,设计并开发了大量结构新颖、活性强的熊果酸衍生物.对近年来合成的有进一步研究价值的熊果酸衍生物及其生物活性研究进展进行总结,为以熊果酸为先导化合物的药物研究提供参考.

Ursolic acid(UA)belongs to a group of pentacyclic triterpenoids extracted from medicinal plants,fruits and vegetables.In recent years,the pharmacological action of ursolic acid has been widely studied.It has been reported that UA has a variety of pharmacological activities,including anti-cancer,anti-inflammation,anti-oxidation,anti-bacterial,anti-diabetes and so on.In spite of that UA shows the extensive therapeutic potential as a drug candidate,the poor water solubility and low bioavailability of UA limit its clinical application.To address these issue,large numbers of UA-based derivatives with enhanced activities and better physicochemical character have been developed by structural modification of its parent skeleton.In this paper,the research progress of the synthesized UA derivatives with therapeutic potential along with their biological activities is reviewed,which provides reference for further drug development using UA as a lead compound.