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09:11
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
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Garcinol Is an HDAC11 Inhibitor.
Se In Son1, Dan Su1, Thanh Tu Ho1
1Department of Chemistry and Chemical Biology, Cornell University, Ithaca, New York 14853, United States.
ACS Chemical Biology
|October 9, 2020
Summary
Garcinol, a natural compound, is identified as a potent inhibitor of histone deacetylase 11 (HDAC11). This discovery offers a new natural product lead for targeting HDAC11, potentially explaining its known biological activities.
Area of Science:
- Natural product chemistry
- Biochemistry
- Epigenetics
Background:
- Garcinol, derived from *Garcinia Indica*, possesses known antioxidant, anti-inflammatory, and anticancer properties.
- Its precise mechanism of action remains incompletely understood, though it has been identified as a histone acetyltransferase (HAT) inhibitor.
Purpose of the Study:
- To investigate garcinol's inhibitory effects on histone deacetylases (HDACs).
- To identify garcinol as a novel inhibitor of Histone Deacetylase 11 (HDAC11).
Main Methods:
- In vitro inhibition assays using High-Performance Liquid Chromatography (HPLC).
- Cellular assays measuring SHMT2 fatty acylation to assess HDAC11 activity.
Main Results:
- Garcinol demonstrated potent inhibition of HDAC11 with IC50 values around 5 μM (in vitro) and 10 μM (cellular assay).
- Garcinol exhibited specificity, inhibiting HDAC11 more effectively than other tested HDACs.
- HDAC11 is the sole member of the Class IV HDACs, with limited existing inhibitors.
Conclusions:
- Garcinol emerges as a significant natural product-derived inhibitor of HDAC11.
- This finding provides a new lead compound for developing HDAC11-targeted therapeutics.
- The inhibition of HDAC11 by garcinol may contribute to its observed biological effects.
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