Modification of flavonoids: methods and influences on biological activities

Abstract

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–activity relationship
• structure modification
• synthesis method

Disclosure statement

The authors are not aware of any affiliations, memberships, funding, or financial holdings that might be perceived as affecting the objectivity of this review.

Additional information

Funding

This study was supported financially by the National Natural Science Foundation of China (No. 32160572, 32101948), the first batch of high-end talents (Youth) projects of science and technology innovation in Jiangxi Province [No. jxsq2019201076], Natural Science Foundation of Jiangxi Province (No. 20202BAB215014), and the Research Project of State Key Laboratory of Food Science and Technology, Nanchang University (No. SKLF-ZZA-201908).