Nicotinamide(烟酰胺,又称Vitamin B3),是sirtuins的非竞争性抑制剂,该抑制作用影响体内外多种重要的调控机制。Nicotinamide强烈抑制酵母SIR2介导的转录沉默,增加rDNA重组,并缩短复制寿命。酵母酶PNC1可将nicotinamide转化为烟酸(nicotinic acid),用于激活Sir2,阻止nicotinamide对端粒的抑制作用和rDNA沉默。Nicotinamide抑制p53的去乙酰化反应,并抑制组蛋白H3和H4的去乙酰化反应。Nicotinamide诱导多种肿瘤细胞凋亡,并伴随caspase级联活化反应。
Nicotinamide已用于临床前实验,用于治疗癌症和I型糖尿病。
参考文献
[1] Bitterman KJ, et al. Inhibition of Silencing and Accelerated Aging by Nicotinamide, a Putative Negative Regulator of Yeast Sir2 and Human SIRT1. J Biol Chem, 277(47): 45099-45107 (2002).
[2] Avalos JL, et al. Mechanism of Sirtuin Inhibition by Nicotinamide: Altering the NAD+ Cosubstrate Specificity of a Sir2 Enzyme. 17(6): 855–868 (2005).
[3] Wang T, et al. Nicotinamide-mediated inhibition of SIRT1 deacetylase is associated with the viability of cancer cells exposed to antitumor agents and apoptosis. Oncol Lett. 6(2): 600–604 (2013).
[4] Audrito V, et al. Nicotinamide Blocks Proliferation and Induces Apoptosis of Chronic Lymphocytic Leukemia Cells through Activation of the p53/miR-34a/SIRT1 Tumor Suppressor Network. Cancer Res. 71(13): 4473–4483 (2011).
粉末直接保存于-25~-15℃,有效期2年。建议避光干燥保存,避免反复冻融。