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Betulinic Acid is a cytotoxic agent isolated from Platanus acerifolia (plane) tree bark. Studies have shown Betulinic Acid, a pentacyclic lupane-type triterpene, to be cytotoxic to leukemia K562 cells. In vitro experiments have shown up-regulation of pro-apoptotic proteins Bax and caspase-3 in mixtures of Betulinic Acid and K562 cells, as well as an increase in NF-κB and reactive oxygen species (ROS). It has been noted that Bax induces cell death by acting on mitochondria via binding of the permeability transition pore complex (PTPC). PTPC is a channel that is involved in permeability regulation of the mitochondrial membrane and this induction of PTPC alone is sufficient to trigger the full apoptosis program of the cell. Additional research has shown that Betulinic Acid acts as a potent inhibitor of Hh/Gli signaling pathway. Betulinic Acid is an activator of Caspase and TGR5.
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