Gambogic Acid, a Caged Xanthone: Therapeutic Effects, Pharmacokinetics, Toxicological Properties, and Delivery Platforms

Many herbal and traditional medicines show promise in the treatment of diverse diseases, but their molecular mechanisms in different dynamic pathological contexts remain poorly understood. Several herbally-derived agents have entered pharmaceutical development, and there are ongoing efforts to define the pharmacotherapeutic effects of natural ingredients. Gambogic acid (GA), a caged xanthone from the dry resin of the widely used traditional Chinese medicinal herb Garcinia hanburyi Hook.f., has demonstrated therapeutic potential against chronic inflammation, cancer, cardiovascular disorders, and other conditions. However, its mechanisms of action, pharmacokinetics, and toxicological profile remain unclear. Furthermore, no comprehensive review exists on nanotechnology-based delivery strategies for this compound. In this review, we summarize current knowledge of the molecular targets and signaling pathways of GA, systematically assess the available pharmacokinetic data, safety considerations, and nanoplatform delivery systems, and highlight promising directions for future applications. Despite substantial preclinical evidence, the clinical translation of GA is hindered by poor drug availability. This review provides a critical synthesis of existing evidence and outlines strategies to advance the therapeutic development of this traditional medicine–derived compound.