Garcinol is a polyisoprenylated benzophenone derivative from the rind of Garcinia indica fruit and is a potent inhibitor of histone acetyltransferases p300 （IC50= ~7 um） and PCAF （IC50= ~5 um） both in vitro and in vivo. p300， also known as E1A binding protein p300， regulates cell growth and division through interacting with numerous transcription factors， and the p53 associated trancriptional coactivator PCAF （P300/CBP-associated factor） plays a direct role in transcriptional regulation. Reports show that Garcinol represses the p300-mediated acetylation of p53 in vivo， promotes apoptosis through caspase-3 activation and predominantly down-regulates global gene expression in HeLa cells. Researchers found that Garcinol exhibits dose-dependent cancer cell-specific growth inhibition in ER-positive MCF-7 and ER-negative MDA-MB-231 breast cancer cells. Additional research shows that Garcinol exhibits anti-carcinogenic and anti-inflammatory properties through selectively suppressing Prostaglandin E2 synthesis and 5-lipoxygenase product formation.
