2-Acetamidoacrylic acid or methyl 2-acetamidoacrylate is reacted with solution of sodium of methylselenol to give N-acetyl-Se-methylselenocysteine.The L(and D)-Se-methylselenocysteine have been prepared in high optica...2-Acetamidoacrylic acid or methyl 2-acetamidoacrylate is reacted with solution of sodium of methylselenol to give N-acetyl-Se-methylselenocysteine.The L(and D)-Se-methylselenocysteine have been prepared in high optical purity by treating N-acetyl-Se-methylselenocysteine in water using acylase I from porcine kidney as a catalyst.The influencing factors on the resolution reaction are discussed by orthogonal experiment,including pH value,reaction temperature,concentration of Co2+ and amount of acylase I.Under the optimizing resolution conditions,L(and D)-Se-methylselenocysteine are obtained with>96 % optical purity in about 40% yield.展开更多
本文以L-硒代胱氨酸为原料合成了L-硒-甲基硒代半胱氨酸(L-MSC),结构经1H NMR、13 C NMR、HRMS和单晶X射线衍射(XRD)表征。L-MSC与甲硫氨酸氨肽酶2(MetAP2)5D6E蛋白的分子对接结果显示,两者具有较好的氢键作用,且两个氢键与ASP251残基...本文以L-硒代胱氨酸为原料合成了L-硒-甲基硒代半胱氨酸(L-MSC),结构经1H NMR、13 C NMR、HRMS和单晶X射线衍射(XRD)表征。L-MSC与甲硫氨酸氨肽酶2(MetAP2)5D6E蛋白的分子对接结果显示,两者具有较好的氢键作用,且两个氢键与ASP251残基形成键角为72.71°的六元刚性船式构象,L-MSC对HEPG2,SGC790和MCF7细胞的体外增殖抑制活性呈剂量依赖关系,在100μM浓度时的抑制率%分别为72.80±1.21、29.32±1.36和39.54±1.62(CCDC:1870311)。展开更多
文摘2-Acetamidoacrylic acid or methyl 2-acetamidoacrylate is reacted with solution of sodium of methylselenol to give N-acetyl-Se-methylselenocysteine.The L(and D)-Se-methylselenocysteine have been prepared in high optical purity by treating N-acetyl-Se-methylselenocysteine in water using acylase I from porcine kidney as a catalyst.The influencing factors on the resolution reaction are discussed by orthogonal experiment,including pH value,reaction temperature,concentration of Co2+ and amount of acylase I.Under the optimizing resolution conditions,L(and D)-Se-methylselenocysteine are obtained with>96 % optical purity in about 40% yield.
文摘为了对Se CPHs的抗氧化活性进行研究,通过老龄小鼠模型以及Hep G2细胞模型考察了普通玉米肽(CPs)、富硒玉米肽(Se CPs)以及甲基硒代半胱氨酸(Me Se Cys)的抗氧化活性。结果表明,采用Se CPs(400 mg/kg)连续灌胃30 d后,老龄小鼠血清中SOD、MDA、GSH-Px、T-AOC以及胸腺指数等指标均有显著改善,总抗氧化能力比CPs高13.38%,说明硒对抗氧化活性有重要贡献;当硒含量相等时,玉米肽比氨基酸的总抗氧化能力高15.79%。在Hep G2细胞模型中,高含硒量的Me Se Cys能极显著提高细胞增殖率。在改善细胞培养液中的ALT、AST和细胞中的SOD、GSH指标方面,Me Se Cys组(硒含量0.5μg/m L)和Se CPs+Me Se Cys组(硒含量0.25μg/m L)均有极显著效果,且水平相当,说明高含硒量化合物与玉米肽间具有协同抗氧化作用。
文摘本文以L-硒代胱氨酸为原料合成了L-硒-甲基硒代半胱氨酸(L-MSC),结构经1H NMR、13 C NMR、HRMS和单晶X射线衍射(XRD)表征。L-MSC与甲硫氨酸氨肽酶2(MetAP2)5D6E蛋白的分子对接结果显示,两者具有较好的氢键作用,且两个氢键与ASP251残基形成键角为72.71°的六元刚性船式构象,L-MSC对HEPG2,SGC790和MCF7细胞的体外增殖抑制活性呈剂量依赖关系,在100μM浓度时的抑制率%分别为72.80±1.21、29.32±1.36和39.54±1.62(CCDC:1870311)。
