Pharmaceutical composition with alpha-glycosidase inhibiting activity and application thereof
A technology of glycosidase inhibition and glycosidase inhibitor, which is applied in the field of medicine and biology, can solve the problems of high dosage of α-glycosidase inhibitor and large side effects, achieve good hypoglycemic effect, reduce postprandial blood sugar, and improve drug efficacy. Effect
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Embodiment 1
[0052] Synergistic inhibition of baicalin and acarbose on rat intestinal α-glucosidase (substrate is maltose)
[0053] SD rats (200-220g) were fasted for 16h, sacrificed under ether anesthesia, and the small intestine was taken out, opened, washed with pre-cooled PBS (0.1M, pH 7.0) buffer solution, and then added at a ratio of 1:10 (W / V) PBS buffer. The small intestine was cut into pieces and homogenized, centrifuged at 10,000 r / min at 4°C for 15 min, and the supernatant was taken as the α-glucosidase mother solution for the test.
[0054] The total volume of the enzyme reaction system is 500 μL, including 100 μL each of enzyme solution, baicalin, acarbose, starch solution, and buffer, wherein baicalin is dissolved in 50% DMSO. First, mix the enzyme with the two inhibitors, incubate at 37°C for 30 minutes, and add 100 μL of maltose solution to start the reaction. Incubate at 37°C for 30 minutes. The sample was placed in boiling water for 10 minutes to terminate the reaction...
Embodiment 2
[0060] Synergistic inhibition of baicalin and acarbose on rat intestinal α-glucosidase (substrate is starch)
[0061] The preparation of α-glucosidase and the method for measuring the inhibition rate are close to Example 1, except that the substrate is changed into starch solution. When 37.03, 74.07, 111.11, 148.15μM baicalinin was combined with 0.31, 0.62, 0.93, 1.24μM acarbose respectively, the inhibition rate of combined use at each dose point was significantly higher than that of single use, CI value are 0.45, 0.45, 0.49 and 0.65 ( figure 1 ), the results showed that the combination of baicalin and acarbose had a strong synergistic inhibitory effect on the hydrolysis of starch by α-glucosidase.
Embodiment 3
[0063] Synergistic inhibition of baicalin and acarbose on rat intestinal α-glucosidase (substrate is sucrose)
[0064] The preparation of α-glucosidase and the method for measuring the inhibition rate are similar to Example 1, except that the substrate is changed into sucrose. Combining 74.07, 148.15, 370.37, 740.74 μM baicalin with 0.062, 0.12, 0.31, 0.62 μM acarbose, respectively, the inhibition rate at each dose point was significantly improved, and the CIs were all less than 0.9. And with the increase of the dose of baicalinin, the CI value decreased gradually, and the synergistic effect was enhanced ( figure 2 ). The results showed that the combination of baicalin and acarbose had a strong synergistic inhibitory effect on the hydrolysis of sucrose by α-glucosidase.
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