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Medical composition having maltose hydrolase inhibitory activity, and application of medical composition

A technology for inhibiting activity and maltase, applied in the field of medicine and biology, can solve the problem of large side effects of maltohydrolase inhibitors, and achieve the effects of improving drug efficacy, reducing postprandial blood sugar, and solving hypoglycemia

Active Publication Date: 2020-06-05
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to solve the problems of relatively large side effects of maltose hydrolase inhibitors in the prior art, the present invention provides a pharmaceutical composition comprising 5,6,7-trihydroxyl-substituted flavonoids and 1-deoxynojirimycin. The drug can not only make the combined drugs have a synergistic effect and improve the drug effect, but also the pharmaceutical composition is a natural product active ingredient, with low side effects, can reduce postprandial blood sugar, prevent or treat diabetes and obesity

Method used

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  • Medical composition having maltose hydrolase inhibitory activity, and application of medical composition
  • Medical composition having maltose hydrolase inhibitory activity, and application of medical composition
  • Medical composition having maltose hydrolase inhibitory activity, and application of medical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 Synergistic inhibition of baicalein and 1-DNJ on maltose hydrolase in the small intestine of mice

[0057] Kunming mice (20~23g) were fasted for 16 hours, and the small intestines were taken after the neck was severed, cut open, washed with pre-cooled PBS (0.1M, pH7.0) buffer, and then according to 1:10 (W / V) Add PBS buffer. The small intestine was cut into fragments and homogenized, centrifuged at 4°C, 10000r / min, for 15min, and the supernatant was taken as the mother liquor of α-glucosidase for the test.

[0058] The total volume of the enzyme reaction system is 250 μL, including 50 μL of enzyme solution, baicalein, 1-DNJ, maltose, and buffer solution, in which baicalein is dissolved in 50% DMSO. First, mix the enzyme with the two inhibitors, incubate at 37°C for 30 minutes, and add 50 μL of maltose solution to start the reaction. Incubate at 37°C and react for 20 minutes. The sample was placed in boiling water for 5 minutes to stop the reaction. Use the gluc...

Embodiment 2

[0062] Example 2 Synergistic inhibition of wild scutellarin and 1-DNJ on maltose hydrolase in the small intestine of mice

[0063] The method for the preparation and inhibition rate determination of α-glucosidase is similar to that of Example 1, except that the flavonoids are replaced with scutellarin. Combining 21.5, 43, 86, 172, 344 μM scutellaria with 0.023, 0.046, 0.092, 0.184, 0.368 μM 1-DNJ, respectively, the inhibition rate of the combined use was significantly higher than that of single use at each dose point ( Table 2), CI values ​​are all less than 0.6, and some representative CI values ​​of synergistic inhibition are as follows image 3 As shown, the results show that the combined use of scutellarin and 1-DNJ has a strong synergistic inhibitory effect on the process of maltose hydrolase hydrolyzing maltose.

[0064] Table 2. The CI index of scutellarin and 1-DNJ synergistically inhibit the intestinal maltose hydrolase of mice

[0065]

[0066]

Embodiment 3 6

[0067] Example 3 Synergistic inhibition of hexahydroflavonoids and 1-DNJ on maltose hydrolase in the small intestine of mice

[0068] The method for the preparation of α-glucosidase and the determination of inhibition rate is similar to that of Example 1, except that the flavonoids are replaced with hexahydroflavonoids. Combining 25, 50, 100, and 200 μM hexahydroxyflavonoids with 0.023, 0.046, 0.092, 0.184 μM 1-DNJ, respectively, the inhibition rate of the combined use was significantly higher than that of the single use at each dose point (Table 3), CI values ​​are all less than 0.8, and some representative CI values ​​of synergistic inhibition are such as Figure 4 As shown, the results indicate that the combined use of hexahydroxyflavone and 1-DNJ has a strong synergistic inhibitory effect on the process of maltose hydrolase hydrolyzing maltose.

[0069] Table 3. The CI index of hexahydroflavonoids and 1-DNJ synergistically inhibiting maltose hydrolase in the mouse intestine

[0...

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Abstract

The invention discloses a medical composition having maltose hydrolase inhibitory activity, and an application of the medical composition. The medical composition having maltose hydrolase inhibitory activity comprises a flavonoid compound and 1-deoxynojirimycin, wherein the flavonoid compound is selected from at least one of monomers, organic salts of the monomers, or inorganic salts of the monomers: baicalein, wild baicalein and quercetagetin. The medical composition disclosed by the invention can effectively reduce postprandial blood sugar, can restrain the activity of maltose hydrolase using maltose as a substrate, and less uses maltose hydrolase inhibitors, so that medicine effects can be increased; and the medical composition is a natural product active component, is low in side effects, can reduce the postprandial blood sugar and can prevent or treat diabetes.

Description

Technical field [0001] The invention relates to a pharmaceutical composition with maltose hydrolase inhibitory activity and its application, and belongs to the field of medical biology. Background technique [0002] Diabetes (diabetes) is a type of chronic hyperglycemia disease, which can be mainly classified into type 1 (insulin-dependent diabetes) and type 2 (non-insulin-dependent diabetes). Type 2 diabetes is the most common form, accounting for all diabetes patients More than 90%, in addition, when the blood sugar is higher than the normal blood sugar range and lower than the diabetic blood sugar range, the state is pre-diabetes, also called pre-diabetes. Prediabetes is the pre-stage of type 2 diabetes. If prediabetes patients do not change their living conditions, more than 70% of patients will develop type 2 diabetes (The Lancet, 2012, 379: 2279-2290). Diabetes and pre-diabetes are accompanied by disorders of glucose, lipid, and protein metabolism caused by insulin secreti...

Claims

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Application Information

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IPC IPC(8): A61K31/445A61K31/352A61P3/10A61P3/04
CPCA61K31/445A61K31/352A61P3/10A61P3/04A61K2300/00Y02A50/30
Inventor 董悦生余娜李夏修志龙
Owner DALIAN UNIV OF TECH
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