Open AccessGarcinol Is an HDAC11 Inhibitor
Author(s) -
Se In Son,
Dan Su,
Thanh Tu Ho,
Hening Lin
Publication year - 2020
Publication title -
acs chemical biology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.899
H-Index - 111
eISSN - 1554-8937
pISSN - 1554-8929
DOI - 10.1021/acschembio.0c00719
Subject(s) - hdac11 , histone deacetylase , histone acetyltransferase , histone deacetylase inhibitor , histone deacetylase 5 , chemistry , acetylation , hdac10 , ic50 , natural product , biochemistry , in vitro , hdac4 , histone deacetylase 2 , histone , pharmacology , biology , gene
Garcinol is a natural product from the Garcinia Indica fruit and is well-known as an antioxidant, anti-inflammatory, and anticancer agent. However, the understanding of its mechanism of action is still incomplete. It has been reported to be a histone acetyltransferase (HAT) inhibitor. Here, we surprisingly found that garcinol is a potent histone deacetylase 11 (HDAC11) inhibitor (IC 50 ∼ 5 μM in vitro with the HPLC assay and IC 50 ∼ 10 μM in the cellular SHMT2 fatty acylation assay), which is comparable to previously reported HDAC11 inhibitors. Additionally, among all the HDACs tested, garcinol specifically inhibits HDAC11 over other HDACs. HDAC11 is the only class IV HDAC, and there are very few inhibitors available for it. Therefore, this study provides a new HDAC11 inhibitor lead from natural products and may help explain the various biological activities of garcinol.