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Licochalcone A (LCA) is an important secondary metabolite in licorice that has attracted extensive attention due to its unique species-specific distribution characteristics and various pharmacodynamic activities, particularly its anti-inflammatory and anti-cancer effects. LCA was originally considered exclusive to Glycyrrhiza inflata Batal. However, further analyses have shown its distribution in different licorice species, extending its known distribution among licorice species and suggesting a broader role in secondary metabolism. Nevertheless, the complex chemical synthesis of LCA presents challenges in regioselectivity control. The oral bioavailability of LCA is limited due to the intestinal first-pass effect, and its metabolic mechanism has not yet been fully elucidated. These issues restrict the therapeutic effects and practical applications of LCA in vivo. In recent years, advancements in optimizing synthetic pathways and developing new delivery systems have significantly improved the efficacy of LCA while also achieving notable breakthroughs in its safety. This review examines the distribution patterns, synthesis methods, in vivo metabolic processes, pharmacological activities, and current application status of LCA, while also exploring future research directions. However, its metabolic mechanisms and prospects for clinical application still require further investigation in the future. A multi-source database search related literature employed “Licochalcone A”as the anchor term, synergized with species taxonomy (Glycyrrhiza), biogeographic patterns, and phytochemical dynamics (biosynthesis/metabolism).
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