Garcinol (camboginol) is a polyisoprenylated benzophenone derivative from the rind of Garcinia indica fruit and is a potent inhibitor of histone acetyltransferases p300 (IC50 ~ 7 μM) and PCAF (IC50 ~ 5 μM) in vitro. P300, also known as E1A binding protein p300, regulates cell growth and division via interactions 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 and promotes apoptosis through caspase-3 activation. Additionally, this compound 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 antiiinflammatory properties through selective suppression of prostaglandin E2 synthesis and 5-lipoxygenase product formation.
1. Matsumoto, Kenji., et al., 2003. Cytotoxic benzophenone derivatives from Garcinia species display a strong apoptosis-inducing effect against human leukemia cell lines. Biological & pharmaceutical bulletin. 26(4): 569-71. PMID: 12673047
2. Balasubramanyam, Karanam., et al., 2004. Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression. The Journal of biological chemistry. 279(32): 33716-26. PMID: 15155757
3. Mantelingu, K., et al., 2007. Specific inhibition of p300-HAT alters global gene expression and represses HIV replication. Chemistry & biology. 14(6): 645-57. PMID: 17584612
4. Koeberle, Andreas., et al., 2009. Identification of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol. Biochemical pharmacology. 77(9): 1513-21. PMID: 19426689
5. Ahmad, Aamir., et al., 2010. Apoptosis-inducing effect of garcinol is mediated by NF-kappaB signaling in breast cancer cells. Journal of cellular biochemistry. 109(6): 1134-41. PMID: 20108249
6. Chen, Ching-Shyang., et al., 2011. Nicotine-induced human breast cancer cell proliferation attenuated by garcinol through down-regulation of the nicotinic receptor and cyclin D3 proteins. Breast cancer research and treatment. 125(1): 73-87. PMID: 20229177
See how others have used Garcinol. Click on the entry to view the PubMed entry .
PMID: # 25538147 Yao, XH. et al. 2014. Physiological reports. 2:
PMID: # 23644046 Du, T. et al. 2013. Experimental and molecular pathology. 95: 38-45.
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