A polyisoprenylated benzophenone with diverse biological activities
Garcinol is an inhibitor of the histone acetyltransferases (HATs) p300 and PCAF (IC50 = 7 and 5 μM, respectively).[1] It also inhibits the HAT GCN5 in Cryptococcus neoformans, inducing temperature sensitivity and impairing growth.[2] A polyisoprenylated benzophenone isolated from Garcinia indica, garcinol promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells.[3],[4] Moreover, it induces apoptosis in several types of cancer cells and has anti-inflammatory actions.[5],[6]
Reference:
[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(6), 33716-33726 (2004).
[2]. 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).
[3]. 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. Journal of Agricultural and Food Chemistry 59, 1031-1040 (2011).
[4]. Nishino, T., Wang, C., Mochizuki-Kashio, M., et al. Ex vivo expansion of human hematopoietic stem cells by garcinol, a potent inhibitor of histone acetyltransferase. PLoS One 6(9), 1-9 (2011).
[5]. Prasad, S., Ravindran, J., Sung, B., et al. Garcinol potentiates TRAIL-induced apoptosis through modulation of death receptors and antiapoptotic proteins. Molecular Cancer Therapeutics 9(4), 856-868 (2010).
[6]. 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. Biochemical Pharmacology 77(9), 1513-1521 (2009).
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