Natural compounds are increasingly recognized for their therapeutic potential in disease treatment, and they make a significant contribution to modern pharmaceutical research. Among these compounds, acteoside (ACT), also known as verbascoside and kusaginin, is a phenylethanoid glycoside derived from sources like Rehmannia glutinosa Libosch. and Cistanche deserticola Ma. This natural compound exhibits a range of therapeutic properties, including neuroprotective, anti-inflammatory, anti-bacterial, and anti-tumor effects, thereby underscoring its potential value in addressing various clinical conditions. However, the unstable physicochemical properties and low bioavailability of ACT have greatly limited its clinical application. This review summarizes the latest advancements in pharmaceutical plant resources, conducts bibliometric analysis and explores the pharmacokinetics, pharmacological effects and molecular mechanisms of ACT, providing a deeper understanding of its medicinal value and current research trends. Furthermore, we utilize network pharmacology strategies and molecular docking techniques to identify additional potential therapeutic targets for ACT. We posit that ACT holds considerable promise as a treatment for atherosclerosis, diabetes with complications, hepatic and respiratory diseases as well as common malignant tumors. This review enhances our understanding of the mechanisms by which ACT treats various diseases and establishes a theoretical foundation for further drug development and research on medicinal plants. Please cite this article as: Zhang FK, Jia KX, Wang H, Liu RP, Xue XY, Huo ZX, Li XJY. Acteoside as a rising star for clinical treatment: Current fundamental research and future outlooks. J Integr Med. 2026; 24(1):7-23.

Key words: Acteoside, Bibliometric analysis, Herbal medicine, Pharmacokinetics, Pharmacology