Abstract: Ginsenosides exhibit a range of biological activities, including antitumor, anti-inflammatory, anti-aging, and antioxidant effects. They have been extensively investigated across various fields such as biology, chemistry, food science, and medicine. However, the limited water solubility and short half-life of ginsenosides pose significant challenges to their application. Optimizing the bioactivity and pharmacokinetic attributes of ginsenosides through the modification of their aglycone structures and sugar chains has emerged as a prominent focus in contemporary ginsenoside research. The primary methods for modifying ginsenoside structures include esterification, oxidation, heterocyclization, and complex modification strategies. This article reviews recent advancements in the structural modification and activities of ginsenosides. It aims to provide valuable references for the design, synthesis, and application of ginsenoside derivatives.