Obacunone, a natural product isolated and purified from the barks of Phellodendron chinense, has cytotoxicity in androgen-dependent human prostate cancer cells. Obacunone may have the potential to prevent estrogen-responsive breast cancer through inhibition of thearomatase enzyme and inflammatory pathways, as well as activation of apoptosis.
Obacunone belongs to a class of unique triterpenoids called limonoids, present in Citrus species. Obacunone possesses antivirulence activity and demonstrates inhibition of cell-cell signaling in Vibrio harveyi and Escherichia coli O157:H7[3]. Obacunone inhibited SW480 cell proliferation with IC50 values of 97 μM at 24h. Sequence of events such as decreased ratio of bcl2/bax gene transcription, activation of caspase-3, fragmentation of DNA in cells treated with obacunone demonstrated induction of apoptosis by limonoids[4]. Obacunone stimulated the transcriptional activity of the bile acids-specific G protein-coupled receptor, TGR5, in a dose-dependent manner. In addition, obacunone inhibited adipocyte differentiation in 3T3-L1 cells and antagonized ligand-stimulated peroxisome proliferator-activated receptor γ (PPARγ) transcriptional activity[5].
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