Abstract
Histone deacetylases (HDACs) are key enzymes for post-translational modification and influence on various cellular activities. Thus, HDACs are associated with many diseases and their inhibitors have clinical significance. Here, 4-Hexylresorcinol (4HR) was studied as an inhibitor for class I HDACs using the HDAC inhibitor (HDACi) Trichostatin-A as a positive control. The 4HR was administered 1–100 μM to human umbilical endothelial cells (HUVECs) and the HDAC expression and activity were examined. The 4HR decreased the expression level of HDAC1, 3, 4, and 5 in a time and dose-dependent manner. The 4HR also increased acetylated lysine and decreased HDAC activity significantly (p < 0.05). Collectively, 4HR was a new class I HDAC inhibitor that reduced the expression and activity of HDAC in HUVECs.
Highlights
Histone deacetylase (HDAC) is an enzyme for removing the acetyl group from lysine in the protein [1]
During investigation of the mechanism of Transforming growth factor-β1 (TGF-β1) expression by 4HR administration, we found that the broad function of 4HR might be similar to that of HDAC inhibitor (HDACi)
trichostatin A (TSA) is known as broad-spectrum HDACi [30]
Summary
Histone deacetylase (HDAC) is an enzyme for removing the acetyl group from lysine in the protein [1]. Except for histone, the function of the other proteins is influenced by HDAC as a post-translational modification process [2]. There are several types of HDACs in 4 classes (Table 1) Their intracellular localizations are various according to their functional demands. The 4HR suppresses the nuclear factor-κB (NF-κB) pathway by inhibiting transglutaminase-2 (TG-2) in oral cancer cells [19,21]. TSA was treated and the expression levels of HDAC1, 3, 4, and 5 and Ac-lys were investigated. The enzymatic activity of Class I HDAC was investigated after 4HR administration
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