Alpha-gluconase activity inhibiter and application thereof in preparation of diabetic medicament

An activity inhibitor, a technology of glucosidase, applied in the field of α-glucosidase activity inhibitor, can solve the problems of side effects and few types, achieve good hypoglycemic effect, inhibit α-amylase activity, and strongly inhibit α- Effect of glucosidase activity

Inactive Publication Date: 2011-03-30
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After clinical application, all have achieved good curative effect, but there are too few types of them, and there are side effects of one kind or another, so there is no more choice in clinical practice.

Method used

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  • Alpha-gluconase activity inhibiter and application thereof in preparation of diabetic medicament
  • Alpha-gluconase activity inhibiter and application thereof in preparation of diabetic medicament
  • Alpha-gluconase activity inhibiter and application thereof in preparation of diabetic medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Preparation of Agrimony Extract

[0021] In the implementation, take the Agrimonia pilosa (Agrimonia pilosa Ledeb.) collected near Guangzhou (identified as Rosaceae (Rosaceae) plant Agrimonia pilosa Ledeb.) by Professor Cai Yuewen of Guangdong Central Research Institute) as an example, first get 1 kg of dry Agrimonia pulverization, pass 60 Mesh sieve, take Agrimony by weighing the powder 100g that crosses 60 mesh sieves gained after being pulverized by traditional Chinese medicine pulverizer, in the 2000ml round bottom flask, add the mass concentration of 1000ml and be that the ethanol of 60% is extraction solvent, be heated to 80 ℃ and carry out thermal reflux, Reflux extraction 3 times, 1 hour each time, combine the alcohol extracts, concentrate, and make an extract. The extract is dissolved in water, and the aqueous solution is extracted with petroleum ether, ethyl acetate, and n-butanol successively according to the polarity, and the solvent of the ethyl acetate par...

Embodiment 2

[0024] Preparation of PBS solution

[0025] Also known as phosphate buffer solution, generally choose K 2 HPO 4 and KH 2 PO 4 Preparation, because the sodium salt dissolves slowly. According to the solution of different pH, weigh the phosphate of different quality, also can use the pH meter to adjust the pH of the solution. PBS is generally used as a supporting electrolyte. The configuration method is as follows: use deionized water, KH 2 PO 4 and Na 2 HPO 4 2H2O prepares PBS solution according to the following steps: (1) Prepare 1 / 15mol / L KH 2 PO 4 , that is, 9.078 grams of KH are dissolved per liter of water 2 PO 4 (2) prepare 1 / 15mol / LNa 2 HPO 4 2H 2 O, that is, 11.876 grams of Na dissolved per liter of water 2 HPO 4 2H 2 O; (3) 18.2% (volume fraction) KH 2 PO 4 solution and 81.8% Na 2 HPO 4 2H 2 O mixed; the final pH value of the PBS solution is about 7.4.

Embodiment 3

[0027] Extraction of intestinal α-glucosidase

[0028] Male rats, weighing 230-280g, were fasted for 24 hours at about the body weight, and sacrificed by decapitating the cervical spine (decapitation). On the ice platform, use thick toilet paper to dry the mucus on the small intestine, scrape off the small intestinal mucosa with a slide, weigh it, add PBS solution at a ratio of 1:10 to homogenate, centrifuge at 14000xg for 30min at 4°C, discard the supernatant, and precipitate Wash twice with pre-cooled PBS, centrifuge at 14000xg for 30min at 4°C, and dilute the pellet 1:5 with PBS, centrifuge at 500xg for 10min at 4°C, and use the supernatant for the experiment. Protein concentration was determined by Bradford method.

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Abstract

The invention discloses an alpha-gluconase activity inhibiter and application thereof in preparation of a diabetic medicament. Rosaceous plant agrimonia pilosa is used as a raw material and ethanol is used as an extraction solvent in the method. The method comprises the following steps of: performing hot reflux, combining ethanol extraction liquid, concentrating the combined ethanol extraction liquid to form extract, dissolving the extract by using water, extracting the aqueous solution by using petroleum ether, acetic ether and n-butyl alcohol in turn according to the magnitude of polarities, and volatilizing the solvent of the acetic ether part to obtain the extract of the acetic ether part, namely agrimonia pilosa extract which is the alpha-gluconase activity inhibiter. In the reaction of the agrimonia pilosa extract, alpha-gluconase and 4-nitrophenol-alpha-D-pyran glucoside serving as a substrate, the extract has the function of inhibiting the activity of the alpha-gluconase to reduce sugar can be deduced according to the variation value of the glucose quantity after the extract is added; and a medicinal composition or a food composition, which is added with the extract and has the sugar reducing function, can be used for preventing and treating diabetes.

Description

technical field [0001] The invention relates to an inhibitor of alpha-glucosidase activity and its application in the preparation of diabetes drugs. Background technique [0002] The incidence of diabetes in the world is increasing year by year. In developed countries, it has been listed as the third largest disease after cardiovascular diseases and tumors. Among them, type 2 diabetes accounts for 90% of diabetic patients. At present, diabetes is the most harmful to human health because of various chronic complications on the basis of arteriosclerosis and microvascular lesions, such as diabetic heart disease, diabetic cerebrovascular disease, diabetic nephropathy, etc. Pay attention to. [0003] Compared with other hypoglycemic drugs, traditional Chinese medicine has the advantage that it can not only lower blood sugar, but also adjust the body by taking advantage of the multi-target and multi-channel advantages of the compound formula. Through syndrome differentiation and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/73A61P3/10
Inventor 张焜陈优生杜志云赵肃清
Owner GUANGDONG UNIV OF TECH
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