Garcinol

Garcinol is a polyisoprenylated benzophenone that has been found in G. indica and has diverse biological activities.^1,2,3,4,5 It inhibits the histone acetyltransferases (HATs) p300 and p300/CREB-binding protein-associated factor (PCAF; IC₅₀s = ~7 and ~5 µM, respectively), as well as COX-1, microsomal prostaglandin E₂ (PGE₂) synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO; IC₅₀s = 12, 0.1, and 0.3 µM, respectively).^1,2 Garcinol (0.8 µM) is active against the fungus C. neoformans in vitro.³ It scavenges hydroxyl radicals and superoxide anions in cell-free assays.⁴ Garcinol (5 µM) induces neurite outgrowth of primary embryonic rat neural progenitor cells.⁵ It reduces ulcer area in rat models of gastric ulcers induced by water immersion stress or indomethacin (Item No. 70270) when administered at a dose of 200 mg/kg.⁴

WARNING This product is not for human or veterinary use.

1. Balasubramanyam, K., Altaf, M., Varier, R.A., et al. Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression. The Journal of Biological Chemisty 279(32), 33716-33726 (2004).

2. Koeberle, A., Northoff, H., and Werz, O. Identification of 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol. Biochem. Pharmacol. 77(9), 1513-1521 (2009).

3. O'Meara, T.R., Hay, C., Price, M.S., et al. Cryptococcus neoformans histone acetyltransferase Gcn5 regulates fungal adaptation to the host. Eukaryot. Cell 9(8), 1193-1202 (2010).

4. Yamaguchi, F., Saito, M., Ariga, T., et al. Free radical scavenging activity and antiulcer activity of garcinol from Garcinia indica fruit rind. J. Agric. Food Chem. 48(6), 2320-2325 (2000).

5. Weng, M.-S., Liao, C.-H., Yu, S.-Y., et al. Garcinol promotes neurogenesis in rat cortical progenitor cells through the duration of extracellular signal-regulated kinase signaling. J. Agric. Food Chem. 59(3), 1031-1040 (2011).