Ursolic acid (UA) is a widely distributed triterpenoid in nature. Due to its easy availability and multiple pharmacological activities, ursolic acid has attracted much attention in the field of medicine and pharmacology. To overcome the disadvantages of bioavailability and poor water solubility during the ursolic acid application, we focused on the synthetic and medicinal properties of UA derivatives modified at C-3 and C-28 sites. This review presents the synthesis of UA derivatives with modification at C-3 and C-28 sites and their pharmacological activity, which may provide some important in...