There are two types of enzymes that affect the acetylationstate of histones: histone acetyltransferases and the opposinghistone deacetylases (HDACs). Yeast silent information regulator 2 (Sir2) is the founding member of Class III HDACs. Nonredox enzyme, sirtuin 1 (Sirt1) is an important member of the mammalian sirtuin family of proteins that commonly have dual activities as a nicotinamide adenine dinucleotide (NAD+)- dependent deacetylase and as a mono-ADP ribosyltransferase. Nicotinamide (NAM), a form of vitamin B3, is an inhibitor of yeast Sir2 and human Sirt1 with IC50 < 50 μM. Treatment of the fetal cells with 10 mM NIC resulted in a twofold increase in DNA content and a threefold increase in insulin content and induced differentiation and maturation of human fetal pancreatic islet cells[3]. Nicotinamide incubation (5 mM) 2h prior to hypoxia significantly increased total nicotinamide adenine dinucleotide (NADH) content, improved neuronal recovery, enhanced ATP content, and prevented NADH hyperoxidation in hippocampal slices[4]. It was found that nicotinamide (200 mg/kg/day) treatment in Alzheimer’s disease transgenic mice-drinking water from birth until 4 months of age improved both the short- and long term memory[5].
作用机制
Nicotinamide inhibits deacetylation by binding to a conserved pocket adjacent to NAD+.
Nicotinamide/烟酰胺 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Yeast Pichia pastoris
0.5 g/L
96 hours
Evaluate the expression effects of different Nampt enzymes in yeast, the Nampt-CP expression strain achieved the highest NMN production of 13.3 mg/L.
Inhibition of catalytically active human SIRT3 (102 to 399 amino acids) expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=6.2 μM
25275824
human SK-MEL-28 cells
100 μM
Function assay
24 h
Reduction in ATP level in human SK-MEL-28 cells at 100 uM maintained in Locke's solution after 24 hrs by luciferase-based assay in absence of GF and glucose
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