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Terminaliia chebula Retz extract, Terminaliia chebula Retz extract monomer compound and application thereof in inhibition of activity of monoamine oxidase B

A technology of monoamine oxidase and extract, which is applied in the direction of drug combination, preparation of sugar derivatives, sugar derivatives, etc., to achieve the effect of inhibiting the activity of monoamine oxidase B

Inactive Publication Date: 2018-08-31
CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no literature report on the inhibitory activity of Xiqingguo to monoamine oxidase B

Method used

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  • Terminaliia chebula Retz extract, Terminaliia chebula Retz extract monomer compound and application thereof in inhibition of activity of monoamine oxidase B
  • Terminaliia chebula Retz extract, Terminaliia chebula Retz extract monomer compound and application thereof in inhibition of activity of monoamine oxidase B
  • Terminaliia chebula Retz extract, Terminaliia chebula Retz extract monomer compound and application thereof in inhibition of activity of monoamine oxidase B

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Experimental program
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Effect test

Embodiment 1

[0038] Preparation of Terminalia chebula Retz. extract XQG-EA-7.

[0039] 1. Extract with methanol

[0040] 250g of raw material of Cynanchum serrata, washed and crushed; 80% methanol extraction, material-liquid ratio (weight ratio) 1:5, methanol reflux extraction three times, the extraction times were 2h, 1.5h, 1h respectively, the three filtrates were combined, and the filtrate was concentrated under reduced pressure To no methanol smell. Take 1ml of the concentrated liquid and evaporate to dryness to calculate its mass. The mass of the total extract is calculated to be 97.9g, and the extraction rate of Celosia serrata is 39.16%.

[0041] 2. Extraction

[0042] Take 1g of the total extract as a sample, and then extract the remaining 96.9g with petroleum ether, ethyl acetate and n-butanol. Respectively concentrating each part of the extract solution to obtain petroleum ether (PET) part 0.54g, ethyl acetate (EA) part 42.18g, n-butanol (NBA) part 34.00g, water (H 2 O) Part 19.38g.

[...

Embodiment 2

[0049] Preparation and identification of monomer compounds XQG-EA-7-2, XQG-EA-7-3, XQG-EA-7-5, XQG-EA-7-6, XQG-EA-7-7.

[0050] 1. XQG-EA-7-2, XQG-EA-7-3, XQG-EA-7-5, XQG-EA-7-6, XQG-EA-7-7 reversed phase column separation preparation

[0051] Take 60g of C18 reversed-phase silica gel and dissolve it in methanol, soak it overnight, and load it into a column. After loading, flush the chromatographic column with 400 mL of methanol, and then equilibrate the column with 400 mL of the starting mobile phase (water: methanol = 3:1). Take a 2 g sample of Celosia serrata extract XQG-EA-7 obtained in Example 1, dissolve it with as little as possible 25% methanol, and load the sample by wet method. Medium pressure glass chromatography column: 75cm high, 2.5cm inner diameter, 3cm outer diameter, column temperature: room temperature, flow rate: 2ml / min, pressure: 1.5MPa, gradient elution with water-methanol system (3:1~0:1 ), specific elution conditions: water-methanol (2:1) 3.3h, water-metha...

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Abstract

The invention discloses a Terminaliia chebula Retz extract, a Terminaliia chebula Retz extract monomer compound and an application thereof in inhibition of activity of monoamine oxidase B. The Terminaliia chebula Retz extract XQG-EA-7 is obtained by the following steps: sequentially extracting the Terminaliia chebula Retz methanol extract through petroleum ether and ethyl acetate, and subjecting the ethyl acetate part to gradient elution and separation by a normal-phase column dichloromethane-acetone-formic acid system, and obtaining the part with the strongest activity of inhibiting the monoamine oxidase B in the component. The five monomer compounds of the Terminaliia chebula Retz extract are obtained by carrying out reversed phase column separation on the Terminaliia chebula Retz extract; the separation system is a medium-pressure glass chromatographic column, and the five monomer compounds are obtained through gradient elution with a water- methanol system. The invention provides the application of the five monomer compounds of the Terminaliia chebula Retz extract in inhibition of the activity of the monoamine oxidase B. The invention further provides an HPLC identification method of the monomer compound XQG-EA-7-6.

Description

Technical field [0001] The present invention relates to an extract of western green fruit, a monomer compound of the extract of western green fruit, and the application of the two in inhibiting the activity of monoamine oxidase B. It belongs to the field of natural product chemistry. Background technique [0002] Monoamine oxidase (MAO) is an oxidoreductase located in the outer mitochondrial membrane of neurons and non-neuronal cells. It can catalyze the oxidative deamination of endogenous monoamine neurotransmitters and amine xenobiotics. The human body contains two types of monoamine oxidase, namely monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). Changes in MAO activity are related to certain central nervous system diseases and peripheral nervous system diseases. Abnormal MAO-A activity is related to depression, anxiety and mental disorders, and patients with Alzheimer’s disease, Huntington’s disease, and Parkinson’s disease have abnormally increased MAO-B activi...

Claims

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Application Information

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IPC IPC(8): C07H13/08C07H1/08C07D493/06A61P25/22A61P25/24A61P25/18A61P25/28A61P25/16A61P25/00G01N30/74A61K36/185
CPCA61K36/185A61P25/00A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28C07D493/06C07H1/08C07H13/08G01N30/74
Inventor 廖循蒋晓兰吴桂芳袁韫聪白小琳
Owner CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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