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Biological Activity:
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator. Triggers CD95- and p53-independent apoptosis via activation of caspases. It induces mitochondrial permeability pore opening and the release of cytochrome c and apoptosis-inducing factor. Displays anti-HIV activity. EC50 for inhibion of HIV-1 replicaton in H9 lymphocytes: 1.4µM
References:
1.Fulda S, Scaffidi C, Susin SA et al. Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid. J Biol Chem. 1998 Dec 18;273(51):33942-8.
2. Chowdhury AR, Mandal S, Mittra B, et al. Betulinic acid, a potent inhibitor of eukaryotic topoisomerase I: identification of the inhibitory step, the major functional group responsible and development of more potent derivatives. Med Sci Monit. 2002 Jul;8(7):BR254-65.