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Compound with alpha-glucosaccharase inhibitory activity in mulberry leaf and application of compound

A technology for glucosidase and inhibitory activity, which is applied in the field of preparation of drugs for the treatment of diabetes, can solve problems such as difficulty in screening with α-glucosidase inhibitors, and achieve reduced preparation and separation steps, shortened screening time, and reproducible Good results

Inactive Publication Date: 2012-12-12
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing screening methods for α-glucosidase inhibitors mainly use in vitro enzyme activity inhibition experiments, which can only evaluate the activity of pure compounds, and are difficult to screen α-glucosidase inhibitors in complex mixtures such as traditional Chinese medicines

Method used

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  • Compound with alpha-glucosaccharase inhibitory activity in mulberry leaf and application of compound
  • Compound with alpha-glucosaccharase inhibitory activity in mulberry leaf and application of compound
  • Compound with alpha-glucosaccharase inhibitory activity in mulberry leaf and application of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Preparation of magnetic beads bound to α-glucosidase

[0024] 1. Reagent and solution preparation:

[0025] α-glucosidase (Saccharomyces cerevisiae, simga company); carboxyl magnetic beads Dynabeads® MyOne Carboxylic Acid, specification: 10 mg / ml (invitrogen company); 1-ethyl-3-(3-dimethylaminopropyl) carbon Diimine hydrochloride (EDC, sigma company); 2-(N-morpholine) ethanesulfonic acid (MES, sigma company); N-hydroxysuccinimide (NHS, sigma company).

[0026] Preparation of 25 mmol / L MES solution Weigh an appropriate amount of MES, add water to dissolve, add 1 mol / L sodium hydroxide solution to adjust the pH to 6, and prepare a MES solution with a concentration of 25 mmol / L.

[0027] Preparation of 50 mg / ml EDC solution Weigh an appropriate amount of EDC and quickly dissolve it in cold 25mmol / L MES solution to prepare an EDC solution with a concentration of 50mg / ml. Prepared fresh just before use.

[0028] Preparation of 50 mg / ml NHS solution Weigh an appr...

Embodiment 2

[0034] Example 2 Screening of compounds with α-glucosidase inhibitory activity in the water-soluble extract of mulberry leaves

[0035] 1. Preparation of drugs, reagents and solutions;

[0036] Standard products of ascarin and isoquercetin (Shanghai Ronghe Pharmaceutical Technology Development Co., Ltd.).

[0037] Water-soluble extract of mulberry leaves: 500 g of mulberry leaves were refluxed with 8 times the amount of 50% ethanol and extracted twice, each time for 1 h. Concentrate the extract and degrease with petroleum ether, adjust the pH value of the water layer to 2 with hydrochloric acid, extract with ethyl acetate, recover the solvent to dryness, and obtain the water-soluble extract of mulberry leaves.

[0038] Preparation of 10 mmol / L ammonium acetate solution: Weigh an appropriate amount of ammonium acetate, dissolve it in water, and make a 10 mmol / L ammonium acetate solution.

[0039] Preparation of α-glucosidase-bound magnetic bead solution: Take the above-mentio...

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Abstract

The invention provides a compound with an alpha-glucosaccharase inhibitory activity in a mulberry leaf. The preliminary screening from the mulberry leaf is carried out by immunomagnetic separation and liquid chromatography-mass spectrometry and a nuclear magnetic resonance method; and a separation or configuration target compound is prepared for verifying the alpha-glucosaccharase inhibitory activity, and thus the compound with the alpha-glucosaccharase inhibitory activity is obtained. Compared with a traditional method, no separation compound for preliminary screening is needed, so that the screening efficiency is remarkably increased, the screening time is shortened and the preparation and separation steps of the marked compound are reduced. In addition, the screening method disclosed by the invention has the characteristics of quickness, accuracy, favorable reproducibility and the like. The quick screening of the compound with the alpha-glucosaccharase inhibitory activity in a natural medicament or traditional Chinese mixture can be popularized. The compound with the alpha-glucosaccharase inhibitory activity, which is obtained by the method disclosed by the invention, can be applied to preparation of medicaments for resisting diabetes mellitus.

Description

technical field [0001] The invention belongs to the field of drug screening methods, and relates to compounds with α-glucosidase inhibitory activity in mulberry leaves, in particular to the application of magnetic bead separation, liquid chromatography-mass spectrometry and nuclear magnetic resonance analysis techniques to obtain compounds with α-glucosidase inhibitory activity from mulberry leaves. A compound with glucosidase inhibitory activity and its application in the preparation of medicaments for treating diabetes. Background technique [0002] Diabetes is a chronic metabolic disorder, and its main intervention methods are diet control, reduction of ingested carbohydrates, and drug treatment. The carbohydrates ingested by the human body are hydrolyzed by enzymes in the epithelial cells of the small intestine (such as amylase and α-glucosidase) to generate glucose before being absorbed into the blood circulation. Acarbose and other α-glucosidase inhibitors can inhibit...

Claims

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Application Information

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IPC IPC(8): C12Q1/34C07H17/07A61K31/7048A61P3/10
Inventor 程翼宇王毅
Owner ZHEJIANG UNIV
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