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Furoate glucoside analogue 1 and purpose thereof of using as alpha-glycosidase inhibitor

A technology of analogs and furoate, applied in the field of α-glucosidase inhibitors, can solve problems such as flatulence and diarrhea, and cumbersome synthesis steps

Inactive Publication Date: 2015-08-26
JILIN AGRICULTURAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, α-glucosidase inhibitors such as acarbose and voglibose have been used as oral hypoglycemic agents in the clinical treatment of diabetes, which can effectively control postprandial blood glucose levels, but these α-glucosides After all, there are only a few enzyme inhibitors on the market, and most of them contain sugar groups, and the synthesis steps are extremely cumbersome. In addition, they have certain side effects in clinical aspects such as flatulence and diarrhea.

Method used

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  • Furoate glucoside analogue 1 and purpose thereof of using as alpha-glycosidase inhibitor
  • Furoate glucoside analogue 1 and purpose thereof of using as alpha-glycosidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Preparation of α-glucosidase inhibitor furoate glycoside analog I

[0024] 1. Preparation of furoate glycoside analog I

[0025] (1) Take 500g of red ginseng, 800g of Poria cocos, 800g of Atractylodes macrocephala, 600g of astragalus, 600g of kudzu root, 1000g of sealwort, 200g of rhubarb, 200g of coptis, 400g of medlar, 200g of schisandra, and 100g of licorice, crush them, mix them well, add 50 L of water to decoct 2 times, 1 hour each time, filter and combine the filtrates;

[0026] (2) Concentrate the filtrate in step (1) to a relative density of 1.25, add 95% ethanol to make the ethanol concentration reach 60%, stand at room temperature for 18 hours, filter, collect the filtrate, evaporate the filtrate to dryness, and suspend in water;

[0027] (3) The aqueous suspension in step (2) was extracted 3 times with an equal volume of ethyl acetate, the ethyl acetate layer was discarded, and the aqueous layer was extracted with an equal volume of water-saturate...

Embodiment 2

[0057] Embodiment 2: the preparation of furoate glycoside analog I soft capsule

[0058] Take furoate glycoside analog I, suspend with soybean oil and beeswax as solvent, and make soft capsules.

Embodiment 3

[0059] Embodiment 3: the preparation of furoate glycoside analog I tablet

[0060] Take the furoate glycoside analog I, add dextrin to granulate, dry, granulate, compress into tablets, and make tablets.

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Abstract

The invention refers to the field of traditional Chinese medicine, and especially relates to furoate glucoside analogue 1 and purpose thereof of using as alpha-glycosidase inhibitor. The structure of the furoate glucoside analogue 1 is 3-(furan-2-methylcarbonyl)oxyglucopyranose aldehyde acid-1 alpha-4-D-glucopyranose-1 alpha -4-D-glucopyranose. The furoate glucoside analogue 1 has strong inhibition ability to alpha-glucosidase, and can be further developed to be drugs for treating and assisting the treatment of 2 type diabetes.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine, in particular to an alpha-glucosidase inhibitor. Background technique [0002] Diabetes mellitus (diabetes mellitus) is a chronic disease of carbohydrate, fat and protein metabolism disorder caused by relative or absolute deficiency of insulin in the body or decreased sensitivity of target cells to insulin, or structural defects of insulin itself. Its main features are hyperglycemia and diabetes. It is clinically manifested as polydipsia, polyphagia, polyuria, and weight loss (i.e. "three excesses and one less"), which can cause morphological structural changes and dysfunction in some tissues or organs, accompanied by ketoacidosis, limb gangrene, multiple Neuritis, blindness and renal failure. The disease incidence rate is increasing day by day, and has become a worldwide common disease and frequently-occurring disease. [0003] According to the Asian Diabetes Society, as of 2012, t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H13/10C07H1/08A61K31/7048A61P3/10
Inventor 赵岩解朝霞解德俊蔡恩博郜玉钢何忠梅许永华张爱华杨鹤刘双利刘学周
Owner JILIN AGRICULTURAL UNIV
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