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) 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 the 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. Garcinol is also known as Camboginol, and 3-(3,4-dihydroxybenzoyl)-4-hydroxy-8,8-dimethyl-1,7-bis(3-methyl-2-buten-1-yl)-5-[(2S)-5-methyl-2-(1-methylethenyl)-4-hexen-1-yl]-bicyclo[3.3.1]non-3-ene-2,9-dione.
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 (CAS 78824-30-3). Click on the entry to view the PubMed entry .
PMID: 35597525 | NCOA2 coordinates with the transcriptional KAT2B-NF-κB partner to trigger inflammation response in acute kidney injury. | Zhou, P. et al. 2022. Gene. 146583.
PMID: 34017833 | FOXC2 Autoregulates Its Expression in the Pulmonary Endothelium After Endotoxin Stimulation in a Histone Acetylation-Dependent Manner. | Xia, S. et al. 2021. Front Cell Dev Biol. 9: 657662.
PMID: 33809417 | Garcinol Attenuates Lipoprotein(a)-Induced Oxidative Stress and Inflammatory Cytokine Production in Ventricular Cardiomyocyte through α7-Nicotinic Acetylcholine Receptor-Mediated Inhibition of the p38 MAPK and NF-κB Signaling Pathways. | Chang, NC. et al. 2021. Antioxidants (Basel). 10:
PMID: 29174768 | Acetylation of TBX5 by KAT2B and KAT2A regulates heart and limb development. | Ghosh, TK. et al. 2018. J. Mol. Cell. Cardiol. 114: 185-198.
PMID: 29414668 | Garcinol inhibits cancer stem cell-like phenotype via suppression of the Wnt/β-catenin/STAT3 axis signalling pathway in human non-small cell lung carcinomas. | Huang, WC. et al. 2018. J. Nutr. Biochem. 54: 140-150.
PMID: 29740418 | Inhibition of Tip60 Reduces Lytic and Latent Gene Expression of Kaposi′s Sarcoma-Associated Herpes Virus (KSHV) and Proliferation of KSHV-Infected Tumor Cells. | Simpson, S. et al. 2018. Front Microbiol. 9: 788.
PMID: 25538147 | Reversal of glucose intolerance in rat offspring exposed to ethanol before birth through reduction of nuclear skeletal muscle HDAC expression by the bile acid TUDCA. | Yao, XH. et al. 2014. Physiological reports. 2:
PMID: 23644046 | Lysosome-dependent p300/FOXP3 degradation and limits Treg cell functions and enhances targeted therapy against cancers. | Du, T. et al. 2013. Experimental and molecular pathology. 95: 38-45.
PMID: 33300026 | | Nucleic Acids Res.
PMID: 30377593 | Evaluation of hematopoietic stem cell expansion in the presence of garcinol. | Habibi, A. et al. Avicenna J Phytomed. 8: 350-357.