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Application of kukoamine in preparing medicine for treating type II diabetes mellitus

A technology of stegosine and diabetes drug, which is used in drug combination, metabolic diseases, pharmaceutical formulations, etc.

Active Publication Date: 2017-05-31
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing research reports believe that the organic acids and alkaloids in Digupi have hypoglycemic effects, but their specific components and mechanism need further study

Method used

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  • Application of kukoamine in preparing medicine for treating type II diabetes mellitus
  • Application of kukoamine in preparing medicine for treating type II diabetes mellitus
  • Application of kukoamine in preparing medicine for treating type II diabetes mellitus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Determination of DPP-4 inhibitory activity

[0032] DPP-4 inhibitor screening method was used to make diocetin into a solution with a concentration of 1 mmol / L; and the positive drug dipeptide A to be made into a solution with a concentration of 1 mmol / L. Take a 96-well plate, add 50 μmol / L specific DPP-4 enzyme activity detection fluorescent probe 2-[4-(1,2,2-triphenylethylene)phenoxy]-acetic acid-lysine-phenylpropanoid Amino acid-proline-glutamic acid (TPE-KFPE) 20 μL, dichotomin solution 5 μL, 0.1 U / mL DPP-4 enzyme solution 5 μL, after mixing, incubate at 37°C for 30 min, at an excitation wavelength of 320 nm, The fluorescence intensity value was measured at an emission wavelength of 450nm. Calculate the inhibitory rate of DPP-4 activity by diocetin. Among them, enzyme solution, sample solution and reaction substrate solution are all prepared with 0.5mmol / L, pH 7.0 HEPES buffer solution.

[0033]

[0034] I 给药组 : Contains substrate and enzyme, and the fluoresc...

Embodiment 2

[0040] Chinese medicine active compound preparation

[0041] Mix 0.5 g of the active compound of traditional Chinese medicine in Example 1 with 10.5 g of polyethylene glycol-6000, heat and melt, and transfer the material to a dripping tank, drop the drug solution into liquid paraffin at 6-8°C, and remove the oil. , made 400 dropping pills.

Embodiment 3

[0043] Chinese medicine active compound preparation

[0044] Take 0.5g of the active traditional Chinese medicine compound of Example 1, 4.5g of glucose, 0.9g of sodium thiosulfate and 1L of distilled water, mix the above components evenly, freeze-dry, and pack in 500 tubes to obtain the product.

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PUM

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Abstract

The invention discloses application of kukoamine in preparing medicine for treating type II diabetes mellitus and belongs to the field of Chinese medicine chemistry. The kukoamine can further realize a hypoglycemic effect by restraining activity of dipeptidyl peptidase4 (DPP-4), so that the kukoamine can be applied to preparing medicine for treating diabetes mellitus. The invention further provides a pharmaceutical composition containing the kukoamine serving as an effective ingredient and drug excipient or carrier which is acceptable in pharmaceutics, and the pharmaceutical composition with the kukoamine as the effective ingredient can effectively improve insulin to resist glucose consumption level of cells and provides novel medicine choice for preventing and treating diabetes mellitus.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine chemistry, in particular to a compound dicortisone with dipeptidyl peptidase 4 (DPP-4) activity inhibitory effect, and the application of the compound in the preparation of drugs for treating type II diabetes. Background technique [0002] Diabetes mellitus, obesity and hyperlipidemia are high and continuously increasing in the worldwide population. Diabetes mellitus is one of the chronic diseases in the general population, which occurs with the increase of obesity and age. With the prolongation of the disease course, various metabolic disorders can lead to various tissues, especially the eyes, kidneys, heart, blood vessels, nerves, etc. The chronic damage and dysfunction caused by diabetes, and the resulting cardiovascular and cerebrovascular diseases, renal failure, blindness, and gangrene of lower limbs have become the main reasons for the disability and death of diabetes. In additi...

Claims

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Application Information

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IPC IPC(8): A61K31/165A61P3/10
CPCA61K31/165
Inventor 赵筱萍
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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