Anti-Inflammation Activity of Flavones and Their Structure–Activity Relationship

• Published in: Journal of agricultural and food chemistry 2021-07, Vol.69 (26), p.7285-7302
• Main Authors: Wang, Xiang, Cao, Yujia, Chen, Siyu, Lin, Jiachen, Bian, Jinsong, Huang, Dejian
• Format: Article
• Language: English
• ISSN: 0021-8561; 1520-5118
• DOI: 10.1021/acs.jafc.1c02015

Flavones are an important class of bioactive constituents in foods, and their structural diversity enables them to interact with different targets. In particular, flavones are known for their anti-inflammatory activity. Herein, we summarized commonly applied in vitro, in vivo, and clinical models in testing anti-inflammatory activity of flavones. The anti-inflammatory structure–activity relationship of flavones was systematically mapped and supported with cross comparisons of that with flavanones, flavanols, and isoflavones. Hydroxyl groups (−OH) are indispensable for the anti-inflammatory function of flavones, and −OH at the C-5 and C-4′ positions enhance while −OH at the C-6, C-7, C-8, and C-3′ positions attenuate their activity. Moreover, the C2–C3 single bond, −OH at the C-3 and B-ring positions undermine flavone aglycones’ activity. Most of the flavone aglycones function through NF-κB, MAPK, and JNK-STAT pathways, and their possible cell binding targets are kinase, aryl hydrocarbon receptor (AhR), G-protein coupled receptors, and estrogen receptors. However, the structure and anti-inflammatory activity relationship of flavones were unclear, and further research shall be conducted to close the gap in order to guide development of evidence-based functional foods.