Application of a kind of coumarin compound in the preparation of monoamine oxidase inhibitor

A technology of monoamine oxidase and coumarins, applied in the field of medicine

Inactive Publication Date: 2020-08-28
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, in the prior art, there are no related reports on the coumarin-derived compounds involved in the present invention and their inhibitory activities on monoamine oxidase A and monoamine oxidase B

Method used

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  • Application of a kind of coumarin compound in the preparation of monoamine oxidase inhibitor
  • Application of a kind of coumarin compound in the preparation of monoamine oxidase inhibitor
  • Application of a kind of coumarin compound in the preparation of monoamine oxidase inhibitor

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Effect test

Embodiment 1

[0022] Example 1: Test of inhibitory activity of the compound of the present invention on monoamine oxidase

[0023] 1. Experimental reagents

[0024] The compound of the present invention, MAO-A (Active Motif, Cat.No.31502), MAO-B (Active Motif, Cat.No.31503), Clorgyline (Sigma, Cat.No.M3778), Selenium Gillan (R(-)-deprenyl) (Abcam, Cat. No. ab120604), 384-well plate (Perkin Elmer, Cat. No. 6007299).

[0025] 2. Experimental method

[0026] 1) Dissolve the compound of the present invention to 10 mM with 100% DMSO, add HEPES as a buffer to the multiwell plate, transfer the compound to the multiwell plate, and reduce the DMSO concentration to 1%.

[0027] 2) Dissolve the enzyme and the substrate in the buffer solution respectively, transfer 10 μL of the enzyme solution to the multi-well plate, and let it stand for 15 minutes to room temperature.

[0028] 3) Add 10μL of substrate solution, start the reaction, let stand for 60 minutes, add 20μL of fluorescein, mix well, let stand for 20 mi...

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Abstract

The invention discloses a purpose of a coumarin compound shown as a general formula (I) in preparation of a monoamine oxidase inhibitor, which belongs to the technical field of a medicine. Through in-vitro enzyme activity tests, the compound has good inhibition activity for monoamine oxidases A and B, and provides reference and novel thinking for developing the novel MAO inhibitor.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and relates to a new pharmaceutical application of a coumarin compound, especially a new application in the preparation of monoamine oxidase inhibitors. Background technique [0002] Monoamine neurotransmitters mainly include norepinephrine, epinephrine, dopamine and serotonin. These neurotransmitters and their metabolites play a broad regulatory role in the human body's nerve, cardiovascular, endocrine and other tissues and systems. Metabolism of monoamine neurotransmitters will cause changes in their expression levels in the body, affect human behavior and emotions, and cause a series of related diseases. Monoamine oxidase (MAO) is located on the mitochondrial membrane of dopaminergic neurons and is mainly distributed in the brain, intestines, liver and other tissues. It is an important regulatory enzyme for the degradation of monoamines. It regulates monoamines by catalyzing the oxidative deamina...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/37A61K31/433A61K31/428A61P25/24A61P25/00A61P25/04A61P25/06A61P25/28A61P25/16
CPCA61K31/37A61K31/428A61K31/433A61P25/00A61P25/04A61P25/06A61P25/16A61P25/24A61P25/28
Inventor 孔德信王栋左之利王雅琪
Owner HUAZHONG AGRI UNIV
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