Gambogin is primarily studied for its potent anticancer properties. It has shown significant activity against various cancer cell lines, including breast, lung, and liver cancers, by inducing apoptosis and inhibiting cell proliferation. Research indicates it can suppress tumor growth by targeting mitochondrial function and generating reactive oxygen species (ROS), leading to cancer cell death. It also exhibits anti-inflammatory effects, making it a candidate for development in treating chronic inflammatory diseases. Additionally, gambogin has demonstrated antibacterial and antifungal activities, suggesting potential use in managing microbial infections. Due to its ability to cross the blood-brain barrier, gambogin is being explored for neuroprotective applications, particularly in neurodegenerative conditions. However, most of the current data come from in vitro and animal studies, and further clinical research is needed to validate its therapeutic uses.