Abstract: Catechins not only have antitumor, antioxidant, antibacterial and antiviral functions, but also can protect the heart and brain and execute other pharmacological effects. These pharmacological effects are principally dependent on the polyhydroxyl structure of catechins, which, however, makes catechins unstable under neutral and alkaline conditions. Catechins are rapidly methylated or glycosylated by enzymes when ingested into the human body. Researchers have found that introducing new chemical groups into the structure of catechins can significantly improve their stability and bioavailability and specifically enhance their pharmacological effects. Notably, methylated catechins can suppress allergic reaction and tumor cell resistance; glycosylation can increase the water solubility of catechins and effectively prevent browning, while acylated catechins show significantly improved antioxidant and antitumor activity due to their high fat solubility. Moreover, the effects of substitution at different locations are different. Studying the synthesis routes and pharmacological effects of catechin derivatives will help discover new pharmacological effects of catechins and promote the clinical application of catechins. The aim of this article is to outline the the biosynthesis and chemical synthesis pathways of catechins with focus on the synthesis pathways and pharmacological effects of catechin derivatives.

Key words: biosynthesis, chemical synthesis, structural modification, pharmacological effects, research prospect