天然黄酮类化合物及其衍生物的构效关系研究进展

Advances in the structure-activity relationship study of natural flavonoids and its derivatives

天然黄酮类化合物是广泛分布于自然界的一大类化合物,已有文献报道其具有抗癌、抗氧化、抗炎、保肝、抗血栓形成、舒张血管、抗病毒、抗菌和抗过敏等多种药理活性。但该类化合物因溶解度差、生物利用度不高等自身缺点而限制了临床上的广泛应用。目前国内外许多课题组选择以天然黄酮为研究对象,通过结构改造研究其针对不同生理活性的构效关系,力求克服其自身缺点,开发出一批具有新颖结构的黄酮类药物的先导化合物。本文总结分析了近几年该类化合物构效关系的研究进展,期望为黄酮类衍生物的设计合成提供参考。

Flavonoids are a large class of compounds widely distributed in nature.Many pharmacological activities of flavonoids have been reported such as anti-cancer,antioxidant,anti-inflammatory,hepatoprotective,antithrombotic,vasodilator,antiviral,antibacterial,antiallergic,and so on.In recent years,domestic and foreign research groups choose natural flavonoids and optimize their chemical structures in order to develop a number of new derivatives with stronger pharmacological activities.As part of the mechanisms are not clear,we need to strengthen in-depth research in the SAR（structure-activity relationship） study for targeted and efficient structure optimization.This paper systematically summarize current researches in the SAR studies of flavonoids and their derivatives,which can serve as a reference for synthesizing new flavonoid derivatives.