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Application of myricetin to preparation of medicine for inhibiting human immunodeficiency virus infection

A technology related to human immunodeficiency and virus infection, which is applied in the field of medicine, can solve the problems of interfering with IN-LEDGF/p75 interaction and unsuccessful marketing, and achieve good inhibitory activity and high safety.

Inactive Publication Date: 2018-08-03
JIANGSU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, many foreign pharmaceutical companies and scientific research institutions are developing new anti-HIV-1 inhibitors that interfere with the IN-LEDGF / p75 interaction, but there is no such inhibitor that has been successfully marketed

Method used

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  • Application of myricetin to preparation of medicine for inhibiting human immunodeficiency virus infection
  • Application of myricetin to preparation of medicine for inhibiting human immunodeficiency virus infection
  • Application of myricetin to preparation of medicine for inhibiting human immunodeficiency virus infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0031] Example 2: Determination of activity of compound on integrase enzyme inhibition

[0032] 1. Experimental principle: IN can cut target DNA and integrate its donor DNA into target DNA. Based on this, digoxin was labeled at the 3 end of the target DNA, and biotin was labeled at the 5' end of the donor DNA. Since IN is able to cleave the target DNA, it integrates its donor DNA into the target DNA. Thus, a 5'biotin-3'digoxigenin double labeled DNA product will be formed. Streptavidin magnetic beads (SA-MB) are added, and the DNA product is captured on the surface of the magnetic beads through the specific reaction of 5' biotin and streptavidin. Then add alkaline phosphatase-labeled digoxin antibody (AP-anti-DIG AB), and connect alkaline phosphatase (AP) to the magnetic beads through the immune reaction between the antibody and digoxin. AP was finally detected by ELISA to detect the integration reaction catalyzed by IN.

[0033]2. Experimental procedure: the reaction was ...

Embodiment 3

[0035] Example 3. Determination of the binding affinity between the compound and integrase.

[0036] 1. Experimental principle: The bottom of the biosensor made of optical fiber is covered with a biomolecular compatibility layer, and after coupling with IN, a biofilm layer is formed, and then the ligand is used to react with small molecules. When a small molecule binds to the ligand coupled at the bottom of the sensor, the thickness of the biofilm layer will increase, and the reflected light interference spectrum curve will shift. The instrument can monitor the change of the phase shift in real time and convert it into a measurable intermolecular interaction. parameters.

[0037] 2. Experimental procedure: Bio-Layer Interferometry (BLI) was completed in Octet RED96 system. A 96-well plate matching the instrument (Fluotrace 600, LOT E110103S) was used in the experiment, and the reaction volume was 200 μl. The biotinylated IN was immobilized on the streptavidin-coated probe an...

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Abstract

The invention provides the application of myricetin and a pharmaceutically acceptable salt thereof to the preparation of a medicine for inhibiting the interaction of an integrase and an integrated cofactor for a human immunodeficiency virus infection-related disease. The pharmaceutically acceptable salt is an acid addition salt formed by a compound of formula I and an inorganic acid or an organicacid. The inorganic acid is one or more of hydrochloric acid, phosphoric acid or sulfuric acid, and the organic acid is one or more of acetic acid, maleic acid, citric acid, benzenesulfonic acid, methyl benzenesulfonic acid, fumaric acid or tartaric acid.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of myricetin in the preparation of integrase (Integrase, IN)-LEDGF / p75 interaction medicine for inhibiting human immunodeficiency virus infection. Background technique [0002] Human Immunodeficiency Virus (HIV) is a virus that causes the deficiency of the human immune system. It mainly attacks the helper T lymphocyte system of the human body. Once it invades the cells of the body, the virus will integrate with the cells and be difficult to eliminate for life; Widely present in the blood, semen, vaginal secretions, breast milk, cerebrospinal fluid, and brain tissue fluid with neurological symptoms of infected persons, among which blood, semen, and vaginal secretions have the highest concentration; the resistance to the external environment is weak, and infected persons Long incubation period and high mortality. HIV-1 IN is an effective target for the ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P31/18
CPCA61K31/352A61P31/18
Inventor 张大为许晓双徐锡明张莉许磊
Owner JIANGSU UNIV OF TECH
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