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Purpose of coumarin compound in preparation of monoamine oxidase inhibitor

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

Inactive Publication Date: 2018-09-04
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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  • Purpose of coumarin compound in preparation of monoamine oxidase inhibitor
  • Purpose of coumarin compound in preparation of monoamine oxidase inhibitor
  • Purpose of coumarin compound in preparation of monoamine oxidase inhibitor

Examples

Experimental program
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Embodiment 1

[0022] Embodiment 1: the test of compound of the present invention to monoamine oxidase inhibitory activity

[0023] 1. Experimental reagents

[0024] Compounds of the present invention, MAO-A (Active Motif, Cat.No.31502), MAO-B (Active Motif, Cat.No. 31503), Clorgyline (Sigma, Cat.No.M3778), Sylvia 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 in the multi-well plate, transfer the compound to the multi-well plate, and reduce the concentration of DMSO to 1%.

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

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

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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 preparing monoamine oxidase inhibitors. Background technique [0002] Monoamine neurotransmitters mainly include norepinephrine, epinephrine, dopamine and serotonin. These neurotransmitters and their metabolites play a wide range of regulatory roles in the nervous, cardiovascular, endocrine and other tissues and systems of the human body. The metabolic disorder of monoamine neurotransmitters will lead to changes in their expression levels in the body, affecting human behavior and emotion, and causing a series of related diseases. Monoamine oxidase (MAO) is located on the mitochondrial membrane of dopaminergic neurons, and is mainly distributed in the brain, intestine, liver and other tissues. It is an important regulatory enzyme for the degradation of monoamines. Concentrations of amine neur...

Claims

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Application Information

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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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