Garcinol (78824-30-3) is a HAT (histone acetyltransferase) inhibitor (p300 IC50=7 μM and PCAF IC50=5 μM) both in vitro and in vivo.1 It potentiates TRAIL-induced apoptosis of cancer cells. In cancer cells garcinol, independent of the cell type, induces both of the TRAIL receptors, death receptor 4 (DR4) and DR5. Garcinol neither induces the receptors of normal cells nor sensitizes them to TRAIL.2
1) Balasubramanyam, et al.; (2004) Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression; J. Biol. Chem. 279 33716
2) Prasad, et al. (2010) Garcinol potentiates TRAIL-induced apoptosis through modulation of death receptors and antiapoptotic proteins; Mol. Cancer Ther. 9 856
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