Dihydromyricetin is a kind of flavanonol,which possesses a variety of biological activities such as antibacterial,anti-inflammatory,anti-tumor and liver protection.The six hydroxyl groups in structure lead to its poor lipid solubility and low bioavailability,and it is expected to improve its bioavailability and biological activity by structural modification.In this paper,we reviewed studies on the structural modification of dihydromyricetin and the biological activities of corresponding derivatives.The chemical modification methods involve etherification reactions,esterification reactions and metal complexe formation,and the derivatives of dihydromyricetin have antiviral,antibacterial,antioxidant,neuroprotection and antitumor activities.Then the challenges arising from the structural modification of dihydromyricetin and the development directions are presented.Further efforts on more thoughtful structural modification are necessary to improve both biological activity and druggability.