gambogic acid

Gambogic acid is a natural caged xanthone compound isolated from the resin of the Garcinia hanburyi tree. It is recognized for its potent **anticancer activity** across a wide range of cancer types—including breast, lung, gastric, colon, prostate, and brain cancers. Gambogic acid modulates multiple molecular pathways, including **inhibition of heat-shock protein 90 (HSP90)** and effects on the **proteasome**, **NF-κB**, **PI3K/AKT**, and **MAPK/ERK** pathways. It induces apoptosis, inhibits tumor proliferation, invasion, metastasis, and angiogenesis, and overcomes chemotherapy resistance in several cancer cell lines. Gambogic acid also activates the JNK signaling pathway and affects proteins such as p53 and Bcl-2, and inhibits vascular endothelial growth factor receptor 2 (VEGFR2) signaling, reducing angiogenesis. It has undergone clinical trials (including phase II in China) for use in solid tumors and hematologic malignancies, demonstrating a favorable safety profile and tumor-selective toxicity due to metabolism by CYP2E1. Poor aqueous solubility and stability are development challenges, and research is ongoing to enhance its clinical utility through formulation and analogs.[1][2][3][4][5][6]

Brand names

THS

Other names

gambogic acidGBAcaged xanthonexanthonoid