Flavonoids are important active ingredients in plant-based food, which have many beneficial effects on health. But the low solubility, poor oral bioavailability, and inferior stability of many flavonoids may limit their applications in the food, cosmetics, and pharmaceutical industries. Structural modification can overcome these shortcomings to improve and extend the application of flavonoids. The study of how to modify flavonoids and the influence of various modifications on biological activity have drawn great interest in the current literature. In this review, the working principles and operating conditions of modification methods were summarized along with their potential and limitations in terms of operational safety, cost, and productivity. The influence of various modifications on biological activities and the structure-activity relationships of flavonoids derivatives were discussed and highlighted, which may give guidance for the synthesis of highly effective active agents. In addition, the safety of flavonoids derivatives is reviewed, and future research directions of flavonoid modification research are discussed.
Keywords: Biological activity; flavonoids; structure modification; structure–activity relationship; synthesis method.