蕎麥堿作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetFagomineCat. No.: HY-13005CAS No.: 53185-12-9分式: CHNO分量: 147.17作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 36 mg/mL (244.62 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 6.

2、7949 mL 33.9743 mL 67.9486 mL5 mM 1.3590 mL 6.7949 mL 13.5897 mL10 mM 0.6795 mL 3.3974 mL 6.7949 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。BIOLOGICAL ACTIVITY物活性 Fagomine 種溫和的糖苷酶 (glycosidase) 抑制劑，F(xiàn)agomine 作于

3、Amyloglucosidase (A.niger)，-Glucosidase (bovine) 和 Isomaltase (yeast)，Ki 分別為 4.8 M，39 M 和 70 M。IC & Target Glycosidase1體外研究 Fagomine (D-fagomine) is an iminosugar that has been shown to selectively agglutinate Enterobacteriales in vitro.Fagomine selectively agglutinates fimbriated enterobacteria (e.

4、g., E.coli) and inhibits their adhesion to the intestinalmucosa; the reason for this is probably related to its structural similarity with lectin-binding saccharides (e.g.,mannose). Fagomine is capable of altering this effect of high-fat high-sucrose diet (HFHS) on the proportion ofEnterobacteriales

5、 and E.coli2.Page 1 of 2 www.MedChemE體內(nèi)研究 Fagomine (D-fagomine) is a natural iminosugar that counteracts the short-term effects of a high-energy-dense dieton body weight, fasting blood glucose levels and the proportion of gut Enterobacteriales3. Compare to the standard group, rats fed high-fat high-

6、sucrose diet (HFHS) with Fagomine (D-fagomine) gain significantly less weight (15.3%)than those fed HFHS (20.9%)2.PROTOCOLKinase Assay 1 Lysosomal enzyme activities in cell lysates are determined. Briefly, cells are scraped in ice-cold 0.1% Triton X-100 inwater. After centrifugation (6000 rpm for 15

7、 min at 4C) to remove insoluble materials, protein concentrations aredetermined using Protein Assay Rapid Kit. The lysates are incubated at 37C with the corresponding 4-methylumbelliferyl -D-glycopyranoside solution in 0.1 M citrate buffer (pH 4). The liberated 4-methylumbelliferoneis measured with

8、a fluorescence plate reader (excitation 340 nm; emission 460 nm). For enzyme inhibition assay, celllysates from normal skin fibroblasts are mixed with the 4-methylumbelliferyl -D-glycopyranoside substrates in theabsence or presence of increasing concentrations of Fagomine1.MCE has not independently

9、confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Human skin fibroblasts from a healthy and three Gaucher disease patients (with N188S/G183W, V230G/R296X andL444P/L444P mutations) are maintained in our laboratory with DMEM supplemented with 10% FBS as the culturemediu

10、m. For enzyme activity enhancement assay, cells are cultured in the presence of different concentrations ofFagomine or DMSO alone (as a control) for 5 days and harvested by scraping. Cytotoxicity of Fagomine is monitoredby measuring the lactate dehydrogenase activities in the cultured supernatants1.

11、MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats3Administration 3 Sprague-Dawley rats (male, 22 weeks old) are randomly assigned to one of the three dietary groups: the controlgroup, fed a standard diet (STD); a group fed HFHS (modified high-

12、fat high-sucrose diet); and a group fed HFHSsupplemented with 0.065% Fagomine (HFHS+FG). The percentage of Fagomine is adjusted so that its ratio to sucroseis 2 mg/g, as defined before from the results of post-prandial tests.The modified diets are processed. Feedconsumption is monitored every day th

13、roughout the experiment and body weight is measured before and at the endof the nutritional intervention. All animal manipulations are carried out in the morning to minimize the effects ofcircadian rhythms.MCE has not independently confirmed the accuracy of these methods. They are for reference only

14、.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Agric Food Chem. 2018 Mar 21;66(11):2758-2764. Molecules. 2019 May 8;24(9). pii: E1776. Molecules. 2017 Sep 26;22(10). pii: E1616. J Pharm Biomed Anal. 2015 Jun 20;114:447-454. J Pharm Biomed Anal. 2015 May 10;109:177-83.See more customer validations on HYPERLINK www.MedChemE www.MedC

15、hemEREFERENCES1. Mena-Barragn T, et al. Inhibitor versus chaperone behaviour of d-fagomine, DAB and LAB sp2-iminosugar conjugates againstglycosidases: A structure-Page 2 of 3 www.MedChemEactivity relationship study in Gaucher fibroblasts. Eur J Med Chem. 2015 Aug 31. pii: S0223-5234(15)30222-1.2. Ra

16、mos-Romero S, et al. Effect of (D)-fagomine on excreted Enterobacteria and weight gain in rats fed a high-fat high-sucrose diet. Obesity (SilverSpring). 2014 Apr;22(4):976-9.3. Molinar-Toribio E, et al. D-Fagomine attenuates metabolic alterations induced by a high-energy-dense diet in rats. Food Funct. 20