Maslinic acid has a variety of biological activities, such as anti‐tumor, hypoglycemic, anti‐inflammatory, and anti‐parasitic. In order to enhance the biological activity of maslinic acid, scholars have carried out a lot of structural modifications, and found some more valuable maslinic acid derivatives. In this paper, the structural modification, biological activity, and structure‐activity relationship of maslinic acid were reviewed, providing references for the development of maslinic acid.