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 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
Escherichia coli BL21 (DE3) cells
Function assay
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
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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