Gambogic Acid, a natural product originally isolated from Garcinia hanburyi, is a cell-permeable caspase activator. It has been shown to induce apoptosis in proliferative cells independent of cell cycle. Mechanistic studies suggest that Gambogic acid causes a decrease of Bcl-2 gene and an increase in Bax gene expression, which may result in apoptosis. Additionally, this compound has been noted to bind CD71 (transferrin receptors) and prevent their internalization, which causes induction of cell death. Gambogic Acid is an inhibitor of A1 and Bcl-2 family proteins, including Bcl-xl, Bcl-2, Bcl-w, Bcl-B, Bfl-1, and Mcl-1. Has shown to cause apoptosis in T47D breast cancer cells and MGC-803 human gastric carcinoma cells.
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