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Application of ilexsaponin in preparation of anti-diabetic medicines

An anti-diabetic and hair-holly technology, applied in the field of medicine, can solve the problems of serious side effects and single target

Inactive Publication Date: 2019-03-12
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemical drugs occupy a dominant position in the pharmaceutical market due to their variety, quick effect, convenient use, and low price, but there are problems such as single target and serious side effects
There is no report about the application of hollyris saponin in anti-diabetes

Method used

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  • Application of ilexsaponin in preparation of anti-diabetic medicines
  • Application of ilexsaponin in preparation of anti-diabetic medicines
  • Application of ilexsaponin in preparation of anti-diabetic medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of Ilex pubescens pentacyclic triterpene saponin 3-O-β-D-xylopyranosylspathodic acid and Flaccidoside I Weigh 10 kg of dry root of Ilex pubescens, add 70% ethanol to reflux and extract 3 times, 3h / time; combine the extracts, Concentrate under reduced pressure to obtain the total extract; weigh the total extract, add distilled water (2L / kg) to make a suspension, and extract with petroleum ether and n-butanol in turn to obtain the n-butanol extraction part; the n-butanol extraction part is decompressed Concentrate and dry in vacuum, dissolve in water and put on D101 macroporous resin column, carry out gradient elution with water, 30% methanol, 50% methanol and 95% methanol respectively, concentrate under reduced pressure and dry in vacuum to obtain 50% methanol elution site; take 50% methanol to wash Remove the site, mix the sample with silica gel (100-200 mesh), and then perform silica gel column chromatography (200-300 mesh), and then use dichlorome...

Embodiment 2

[0030] Example 2 Ilex pentacyclic triterpene saponin ilexoside A, ilexsaponin A1 and Ilexsaponin B 2 preparation of

[0031] Weigh 10 kg of dried root of Ilex pubescens, extract 3 times with 75% ethanol under reflux, 4h / time; combine the extracts, concentrate under reduced pressure to obtain the total extract; weigh the total extract, add distilled water (2L / kg) to make a suspension liquid, and then sequentially extracted with petroleum ether and n-butanol to obtain the n-butanol extraction part; the n-butanol extraction part was concentrated under reduced pressure and vacuum-dried, dissolved in water and placed on a macroporous resin column, and respectively water, 30% methanol, 50% methanol, Gradient elution with 95% methanol, concentration under reduced pressure and vacuum drying to obtain the elution site of 50% methanol; take the elution site of 50% methanol, mix the sample with silica gel (100-200 mesh), and then perform silica gel column chromatography (200-300 mesh), ...

Embodiment 3

[0035] Example 3 α-glucosidase inhibitory activity screening

[0036] 1. Experimental materials

[0037] 1.1 Reagents

[0038] α-glucosidase (sigma); PNPG (sigma); disodium hydrogen phosphate, potassium dihydrogen phosphate, Nanjing Chemical Reagent Factory.

[0039] 1.2 Instruments

[0040] Pure water machine (Yipu Yida), ultrasonic instrument (Jiangsu Kunshan Ultrasonic Instrument Factory), microplate reader (Moleculardevices plus 384), pH meter (Mettler).

[0041] 2. Reagent preparation

[0042] α-glucosidase (sigma) was formulated with 0.067mol / L PH6.8 phosphate buffer solution to make 1U / mL, and the substrate PNPG (sigma) was made into 3mg / mL with water.

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Abstract

The invention discloses application of pentacyclic triterpenoid saponins in ilex pubescens, namely Ilexsaponin B2, ilexoside A, Ilexsaponin A1,3-O-beta-D-xylopyranosylspathodic acid and flaccidoside I, in preparation of anti-diabetic medicines. Five pentacyclic triterpenoid saponins in ilex pubescens are obtained by large-scale preparation, and the inhibitory activity of the five pentacyclic triterpenoid saponins on alpha-amylase is screened by a large number of experiments. Experimental results show that the five pentacyclic triterpenoid saponins have better inhibitory activity on alpha-glucuronide. Especially, the IC50 of Silverside A and ilexsaponin A1 for alpha-amylase is respectively 0.0849mg / ml and 0.2184mg / ml, thereby obtaining excellent technical effects.

Description

technical field [0001] The invention relates to the new application of hollyrin saponin in the preparation of antidiabetic drugs, and belongs to the technical field of medicine. Background technique [0002] Diabetes is a group of metabolic diseases characterized by hyperglycemia. Hyperglycemia is due to defective insulin secretion or impaired biological action, or both. The main means of preventing and treating diabetes at present is chemical medicine. Chemical drugs occupy a dominant position in the pharmaceutical market due to their variety, quick effect, convenient use, and low price. However, there are problems such as single target and serious side effects. At present, the development of antidiabetic drugs with high biological activity and multiple targets has become a new trend of development. Studies have shown that some traditional Chinese medicines have a good inhibitory effect on diabetes, and have the advantages of low side effects and relative safety. Therefo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K31/7024A61P3/10C07J63/00C07H1/08C07H15/256C07H13/08
CPCA61K31/704A61K31/7024A61P3/10C07H1/08C07H13/08C07H15/256C07J63/008
Inventor 林丽萍
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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