Suppressive activity of mango aglycone on PTP1B and application thereof
A technology of mangiferin and inhibitors, which is applied in the field of biopharmaceuticals and can solve problems such as insulin sensitivity that have not yet been seen
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Embodiment 1
[0026] Embodiment 1 Mangiferin aglycon is to the inhibitory activity determination of PTP1B (IC 50 Determination of value)
[0027] Mangiferin aglycon was dissolved in a small amount of DMSO and diluted with MOPS buffer, and 10 μl was added to a 100 μl reaction system (pH 7.0, 25 mM mops, 1 mM EDTA, 2 mM DTT, 0.1 M NaCl), so that the final concentrations were 1500, 150, 15, 1.5, 0.15 μM, add the substrate pNPP to 16mM, add 5ng of recombinant human PTP1B and place it at 37°C for 30min. Add 10 μl of 1M NaOH to terminate the reaction, place it on a microplate reader to measure the absorbance A at a wavelength of 405 nm, and use sodium metavanitate (NaVO 3 ) as a positive control, and without adding PTP1B as a blank control, the inhibition rate was calculated. Use the inhibition rate to plot the concentration to get the mangiferin aglycon IC 50 9.2 μM, sodium metavanate IC 50 is 0.32 μM.
Embodiment 2
[0028] Example 2 Determination of the inhibition kinetics of PTP1B by mangiferin aglycone
[0029] Different concentrations of pNPP (32, 16, 8, 4, 2mM) and different concentrations of NL solutions (1.25, 2.5, 5, 10, 20μM) were prepared respectively. Each NL concentration corresponds to 5 groups of pNPP concentrations for inhibitory activity determination, and V is calculated according to the change of OD405, and the corresponding substrate concentration is S, and the graphs are drawn according to the L-B equation. The results showed that the straight lines intersected on the Y axis, so it can be judged that NL is a competitive inhibitor of PTP1B.
Embodiment 3
[0030] Example 3 Effect of mangiferin on improving insulin sensitivity in normal mice
[0031] C57BL / 6 mice were randomly divided into 5 groups with 11 mice in each group, which were control group and NL administration group with different doses (100, 60, 40, 15 mg / kg). The treatment groups were intragastrically administered different concentrations of NL (suspended with 0.5% CMC-Na aqueous solution), and the control group were intragastrically administered 0.5% CMC-Na aqueous solution. Continuous administration for 7 days, fasting for 12 hours after the last administration, intraperitoneal injection of insulin at 1 U / kg, blood samples were taken at 0, 15, 30, 60, 90, and 120 minutes to measure blood glucose levels.
[0032] Insulin Tolerance Test (Insulin Tolerance Test, ITT) experiment shows that NL (5, 40mg / kg) can significantly improve the insulin sensitivity of C57BL / 6 mice, reduce its blood sugar, and there are significant differences in the last four time points (p< 0....
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