Garcinol

Epigenetic modifier; Inhibits histone acetyltransferases (HATs) p300 and pCAF

Garcinol

Epigenetic modifier; Inhibits histone acetyltransferases (HATs) p300 and pCAF

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Epigenetic modifier; Inhibits histone acetyltransferases (HATs) p300 and pCAF
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Overview

Garcinol is an inhibitor of histone acetyltransferases (HATs) p300 and pCAF (IC₅₀ = 7 and 5 μM, respectively) (Balasubramanyam et al.). It also inhibits the HAT GCN5 in Cryptococcus neoformans, inducing temperature sensitivity and impairing growth (O’Meara et al.).

MAINTENANCE AND SELF-RENEWAL
· Promotes ex vivo expansion of human hematopoietic stem cells (Nishino et al.).

DIFFERENTIATION
· Promotes neurogenesis in rat cortical progenitor cells (Weng et al.).

CANCER
· Induces apoptosis in several types of cancer cells and has anti-inflammatory actions (Koeberle et al.; Prasad et al.).
Cell Type
Cancer Cells and Cell Lines, Hematopoietic Stem and Progenitor Cells, Neural Stem and Progenitor Cells, Neurons
Species
Human, Mouse, Non-Human Primate, Other, Rat
Application
Differentiation, Expansion
Area of Interest
Cancer, Neuroscience, Stem Cell Biology
CAS Number
78824-30-3
Chemical Formula
C₃₈H₅₀O₆
Purity
≥ 95%
Pathway
Epigenetic
Target
HAT

Protocols and Documentation

Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.

Document Type
Product Name
Catalog #
Lot #
Language
Product Name
Garcinol
Catalog #
72452
Lot #
All
Language
English
Document Type
Safety Data Sheet
Product Name
Garcinol
Catalog #
72452
Lot #
All
Language
English

Applications

This product is designed for use in the following research area(s) as part of the highlighted workflow stage(s). Explore these workflows to learn more about the other products we offer to support each research area.

Resources and Publications

Educational Materials (2)

Publications (6)

Garcinol promotes neurogenesis in rat cortical progenitor cells through the duration of extracellular signal-regulated kinase signaling. Weng M-S et al. Journal of agricultural and food chemistry 2011 MAR

Abstract

Garcinol is a polyisoprenylated benzophenone derivative found in Garcinia indica fruit rind and other species. The potential antioxidative and neuroprotective effects of garcinol in rat cortical astrocyte were demonstrated in our laboratory recently. Here, the effects of garcinol on the neuritogenesis process in cultured cortical progenitor cells were investigated to understand the roles of garcinol in neuronal survival and differentiation. These cells, derived from embryonic day 17 rats, differentiated into EGF-responsive neural precursor cells, would further form neurospheres. Our data exhibited garcinol induced neurite outgrowth in early developing EGF-treated neurospheres and significantly enhanced the expression of neuronal proteins, microtubule-associated protein 2 (MAP-2), and glial fibrillary acidic protein (GFAP). Furthermore, the neuronal marker, high-molecular-weight subunit of neurofilaments (NFH), was highly expressed after 5 μM garcinol treatment in neural precursor cells for 20 days. To identify the extracellular mechanism, rat cortical progenitor cells were treated garcinol and accordingly mediated the sustained activation of extracellular signal-regulated kinase (ERK) for different periods up to 20 h. In this regard, NMDA receptor-mediated calcium influx led to excitotoxic death and activated tyrosine phosphatase which limited the duration of ERK in cultured neurons. MK801, the NMDA receptor antagonist, treatment also induced the sustained phosphorylation of ERK and therefore enhanced neuronal survival. In our observation, garcinol treatment reduced growth factor deprivation-mediated cell death and nuclear import of C/EBPβ levels. Noteworthy, garcinol could promote neurite outgrowth in EGF-responsive neural precursor cells and modulate the ERK pathway in the enhancement of neuronal survival.
Ex vivo expansion of human hematopoietic stem cells by garcinol, a potent inhibitor of histone acetyltransferase. Nishino T et al. PloS one 2011 JAN

Abstract

BACKGROUND: Human cord blood (hCB) is the main source of hematopoietic stem and progenitor cells (HSCs/PCs) for transplantation. Efforts to overcome relative shortages of HSCs/PCs have led to technologies to expand HSCs/PCs ex vivo. However, methods suitable for clinical practice have yet to be fully established. METHODOLOGY/PRINCIPAL FINDINGS: In this study, we screened biologically active natural products for activity to promote expansion of hCB HSCs/PCs ex vivo, and identified Garcinol, a plant-derived histone acetyltransferase (HAT) inhibitor, as a novel stimulator of hCB HSC/PC expansion. During a 7-day culture of CD34(+)CD38(-) HSCs supplemented with stem cell factor and thrombopoietin, Garcinol increased numbers of CD34(+)CD38(-) HSCs/PCs more than 4.5-fold and Isogarcinol, a derivative of Garcinol, 7.4-fold. Furthermore, during a 7-day culture of CD34(+) HSCs/PCs, Garcinol expanded the number of SCID-repopulating cells (SRCs) 2.5-fold. We also demonstrated that the capacity of Garcinol and its derivatives to expand HSCs/PCs was closely correlated with their inhibitory effect on HAT. The Garcinol derivatives which expanded HSCs/PCs inhibited the HAT activity and acetylation of histones, while inactive derivatives did not. CONCLUSIONS/SIGNIFICANCE: Our findings identify Garcinol as the first natural product acting on HSCs/PCs and suggest the inhibition of HAT to be an alternative approach for manipulating HSCs/PCs.
Cryptococcus neoformans histone acetyltransferase Gcn5 regulates fungal adaptation to the host. O'Meara TR et al. Eukaryotic cell 2010 AUG

Abstract

Cryptococcus neoformans is an environmental fungus and an opportunistic human pathogen. Previous studies have demonstrated major alterations in its transcriptional profile as this microorganism enters the hostile environment of the human host. To assess the role of chromatin remodeling in host-induced transcriptional responses, we identified the C. neoformans Gcn5 histone acetyltransferase and demonstrated its function by complementation studies of Saccharomyces cerevisiae. The C. neoformans gcn5Delta mutant strain has defects in high-temperature growth and capsule attachment to the cell surface, in addition to increased sensitivity to FK506 and oxidative stress. Treatment of wild-type cells with the histone acetyltransferase inhibitor garcinol mimics cellular effects of the gcn5Delta mutation. Gcn5 regulates the expression of many genes that are important in responding to the specific environmental conditions encountered by C. neoformans inside the host. Accordingly, the gcn5Delta mutant is avirulent in animal models of cryptococcosis. Our study demonstrates the importance of chromatin remodeling by the conserved histone acetyltransferase Gcn5 in regulating the expression of specific genes that allow C. neoformans to respond appropriately to the human host.