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Application of hydroxyoctadecadienoic acid in preparation of alpha-glucosidase inhibitor drugs and separation method of alpha-glucosidase inhibitor drugs

A technology of octadecadienoic acid and glucosidase, which is applied in the field of hypoglycemic drugs, can solve the problems of easy loss of active compounds, heavy workload, and tediousness, and achieve good application prospects and the effect of lowering blood sugar

Inactive Publication Date: 2020-08-25
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main reason is that the research on bioactive components in complex extracts is laborious and time-consuming. Bioassay-guided fraction has been used as a classic way to find new active compounds in medicinal plants for many years. The separation and activity test of fractions, the workload is very large and cumbersome, and it is easy to lose active compounds with small content

Method used

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  • Application of hydroxyoctadecadienoic acid in preparation of alpha-glucosidase inhibitor drugs and separation method of alpha-glucosidase inhibitor drugs
  • Application of hydroxyoctadecadienoic acid in preparation of alpha-glucosidase inhibitor drugs and separation method of alpha-glucosidase inhibitor drugs
  • Application of hydroxyoctadecadienoic acid in preparation of alpha-glucosidase inhibitor drugs and separation method of alpha-glucosidase inhibitor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Identification of α-glucosidase inhibitory activity of 9-hydroxyl-10,12-octadecadienoic acid

[0036] Buy two standard products of 9-hydroxy-10,12-octadecadienoic acid: (9S,10E,12Z)-9-hydroxy-10,12-octadecadienoic acid (9S-HODE for short) and (9R,10E,12Z)-9-hydroxyl-10,12-octadecadienoic acid (abbreviated as 9R-HODE) (Cayman Chemical Company, MI, USA), was determined for its α-glucosidase inhibitory activity, expressed as A Carbose was used as a positive control.

[0037] The determination method is as follows:

[0038] The sample was dissolved in DMSO, prepared into a 40mg / mL solution, diluted with DMSO into different concentration gradients, 10 μL each was placed in a 96-well plate, and 90 μL of 0.1M phosphate buffer (pH7.5, 0.02% NaN 3 ), add 80 μL of α-glucosidase dissolved in the above-mentioned phosphate buffer solution with a concentration of 0.05 U / mL, mix the mixture thoroughly and place it in an incubator at 28°C for 10 min, and then add 20 μL of p...

Embodiment 2

[0040] Example 2 Separation of 9-antelope-10,12-octadecadienoic acid in Digupi

[0041] The purpose of this example is to separate 9-hydroxy-10,12-octadecadienoic acid from Cortex Dictica.

[0042] The separation steps are as follows:

[0043] 1. Rough extraction

[0044] Crush Digupi, weigh 10 g of the sample into a stoppered Erlenmeyer flask, add 100 mL of ethyl acetate, shake for 1 hour, place it for 48 hours, shake for 10 minutes, filter, and dry the filtrate in a vacuum dryer to obtain a crude extract.

[0045] 2. Separation

[0046] The crude extract was dissolved in methanol to prepare a 40 mg / mL solution, filtered through a 0.45 μm pore-diameter filter membrane, and analyzed by liquid chromatography, and a fraction was collected every 1 min.

[0047] The chromatographic conditions are: the mobile phase flow rate is 0.5mL / min, and the mobile phase consists of (A) 5% acetonitrile dissolved in water (comprising 0.1% formic acid) and (B) 95% acetonitrile dissolved in wate...

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Abstract

The invention discloses application of hydroxyoctadecadienoic acid in preparation of alpha-glucosidase inhibitor drugs, and belongs to the field of hypoglycemic drugs. The inventor finds that 9-hydroxy-10,12-octadecadienoic acid is an important component for inhibiting alpha-glucosidase by researching substances for inhibiting alpha-glucosidase in the traditional Chinese medicine cortex lycii radicis. 9-hydroxy-10,12-octadecadienoic acid is used as an active component in the alpha-glucosidase inhibitor medicine, and is expected to replace the existing alpha-glucosidase inhibitor medicine, so that the application prospect is good.

Description

technical field [0001] The invention belongs to the field of hypoglycemic drugs. Background technique [0002] According to relevant statistics reported by the World Health Organization in 2016, there are about 442 million diabetic patients worldwide. According to a survey in 2010, China has as many as 114 million diabetic patients, accounting for 11.6% of adults, and pre-diabetic patients have reached as many as 50%. China has become the country with the highest incidence of diabetes in the world, and new cases of diabetes each year (Xu Y. et al., Journal of the American Medical Association, 2013, 310:948-958.). Type 2 diabetes accounts for 90% of diabetes cases, and the astonishing incidence of diabetes has become one of the biggest burdens on the social medical system after cancer, cardiovascular disease, and chronic respiratory disease. [0003] α-glucosidase, also known as glucosyltransferase (α-glucosidase, EC.3.2.1.20), is systematically named α-D-glucoside glucohyd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/201A61P3/10A61P3/04C07C51/47C07C59/42G01N30/02G01N30/06G01N30/72
CPCA61K31/201A61P3/04A61P3/10C07C51/47G01N30/02G01N30/06G01N30/72G01N2030/027G01N2030/062C07C59/42
Inventor 龚萌刘月秋
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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