荞麦碱 TQ0298

Product Introduction
Bioactivity


英文名: Fagomine

描述: Fagomine (D-Fagomine) 是一种温和的糖苷酶 (glycosidase) 抑制剂，是1-脱氧野尻霉素 （DNJ） 的类似物，具有降血糖活性，Fagomine 降低了细胞内活性氧（ROS）的产生和丙二醛（MDA）水平。

细胞实验: Human skin fibroblasts from a healthy and three Gaucher disease patients (with N188S/G183W, V230G/R296X, and L444P/L444P mutations) are maintained in DMEM supplemented with 10% FBS as the culture medium. For enzyme activity enhancement assay, cells are cultured in the presence of different concentrations of Fagomine or DMSO alone (as a control) for 5 days and harvested by scraping. Cytotoxicity of Fagomine is monitored by measuring the lactate dehydrogenase activities in the cultured supernatants [1].

激酶实验: Lysosomal enzyme activities in cell lysates are determined. Briefly, cells are scraped in ice-cold 0.1% Triton X-100 in water. After centrifugation (6000 rpm for 15 min at 4°C) to remove insoluble materials, protein concentrations are determined using Protein Assay Rapid Kit. The lysates are incubated at 37°C with the corresponding 4-methylumbelliferyl β-D-glycopyranoside solution in 0.1 M citrate buffer (pH 4). The liberated 4-methylumbelliferone is measured with a fluorescence plate reader (excitation 340 nm; emission 460 nm). For enzyme inhibition assay, cell lysates from normal skin fibroblasts are mixed with the 4-methylumbelliferyl β-D-glycopyranoside substrates in the absence or presence of increasing concentrations of Fagomine [1].

动物实验: Sprague-Dawley rats (male, 22 weeks old) are randomly assigned to one of the three dietary groups: the control group fed a standard diet (STD); a group fed HFHS (modified high-fat high-sucrose diet); a group fed HFHS supplemented with 0.065% Fagomine (HFHS+FG). The percentage of Fagomine is adjusted so that its ratio to sucrose is 2 mg/g, as defined before from the results of post-prandial tests. The modified diets are processed. Feed consumption is monitored every day throughout the experiment and body weight is measured before and at the end of the nutritional intervention. All animal manipulations are carried out in the morning to minimize the effects of circadian rhythms [3].

体外活性: Fagomine (D-fagomine)，一种次氨基糖，在体外展现出对大肠杆菌的选择性凝集作用。D-fagomine选择性地聚集有鞭毛的大肠杆菌，阻止它们附着于肠道黏膜。这种效果可能归因于其与结合到凝集素（如甘露糖）的糖基团结构相似性。D-fagomine能够改变高脂高糖饮食（HFHS）对肠道内肠杆菌科和拟杆菌属比例的影响[3]。

体内活性: Fagomine（D-fagomine），一种天然的亚氨基糖，能够抵消高能量密度饮食对体重、空腹血糖水平及肠道肠杆菌属[3]短期影响。与标准组相比，同时摄入D-fagomine的高脂高蔗糖饮食（HFHS）大鼠体重增加显著较低（15.3%），而仅摄入HFHS的大鼠体重增加为20.9%[2]。

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 30 mg/mL (203.85 mM)


关键字: Fagomine

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