garcinol

Product Namegarcinol
CAS78824-30-3
MFC38H50O6
MW602.8
EINECS200-258-5
MOL File78824-30-3.mol

Chemical Properties

Melting point	132 °C
Boiling point	710.8±60.0 °C(Predicted)
Density	1.114±0.06 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 25 mg/ml).
pka	4.50±1.00(Predicted)
form	Yellow solid.
color	Yellow
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. Garcinol is prone to oxidation. Protect from exposure to air.
LogP	11.546 (est)

Usage And Synthesis

Description

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

Uses

Garcinol is an inhibitor of the histone acetyltransferases (HATs) p300 and PCAF (IC50 = 7 and 5 μM, respectively). It also inhibits the HAT GCN5 in Cryptococcus neoformans, inducing temperature sensitivity and impairing growth. A polyisoprenylated benzophenone isolated from Garcinia indica, garcinol promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells. Moreover, it induces apoptosis in several types of cancer cells and has anti-inflammatory actions.

Uses

Garcinol is a small molecule inhibitor of histone acetyltransferases. Used in cancer therapy. Garcinol, harvested from Garcinia indica.

Definition

ChEBI: Garcinol is a monoterpenoid.

in vivo

Garcinol (i.p.; 1 and 2 mg/kg; five times/week for 4 consecutive weeks) induces significant inhibition of tumor growth^[3].

Animal Model:	Five-week-old athymic nu/nu male mice bearing subcutaneous CAL27 tumors^[3]
Dosage:	1 and 2 mg/kg
Administration:	I.p.; five times/week for 4 consecutive weeks
Result:	Induced significant inhibition of tumor growth.

IC 50

AChE; BChE; GCN5/PCAF; Human Endogenous Metabolite

References

[1] KARANAM BALASUBRAMANYAM. Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression.[J]. The Journal of Biological Chemistry, 2004, 279 32: 33716-33726. DOI:10.1074/jbc.m402839200
[2] SAHDEO PRASAD. Garcinol potentiates TRAIL-induced apoptosis through modulation of death receptors and antiapoptotic proteins.[J]. Molecular Cancer Therapeutics, 2010, 9 4: 856-868. DOI:10.1158/1535-7163.mct-09-1113

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