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Application of Aspochalasin compounds to preparation of anti-HIV (human immunodeficiency virus)-latency drugs and acquired immune deficiency syndrome treating drugs

A compound and AIDS technology, applied in the field of preparation of anti-HIV latent drugs and AIDS drugs, can solve the problems of weak activation effect and obvious adverse reactions, and achieve the effect of accelerated clearance

Active Publication Date: 2016-01-27
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above drugs under research all have different deficiencies, such as weak activation effect, obvious adverse reactions, etc.

Method used

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  • Application of Aspochalasin compounds to preparation of anti-HIV (human immunodeficiency virus)-latency drugs and acquired immune deficiency syndrome treating drugs
  • Application of Aspochalasin compounds to preparation of anti-HIV (human immunodeficiency virus)-latency drugs and acquired immune deficiency syndrome treating drugs
  • Application of Aspochalasin compounds to preparation of anti-HIV (human immunodeficiency virus)-latency drugs and acquired immune deficiency syndrome treating drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] HIV Latency Induction Activation Experiment

[0021] The cells used for activity screening were divided into 2 × 10 per well 4Each was planted in a 96-well plate, and 100 microliters of 1640 medium (Gibco) containing 10% FBS (fetal bovine serum, Gibco) was added to each well. After 24 hours, a certain concentration of Aspochalasin compounds was added. After the cells were treated with drugs for 72 hours, the expression of GFP in the cells was observed under a fluorescence microscope, and the cells were collected for flow cytometry detection to analyze the proportion of fluorescent cells.

Embodiment 2

[0023] With a final concentration of 20 μg / ml AspochalasinE (R 1 , R 2 , R 3 , R 4 and R 5 Treat HIV latently infected cell models with OH, OH, OH, H and H) respectively, and analyze the activation of HIV latently infected cells by fluorescent microscope observation and flow cytometry detection of the reporter gene green fluorescent protein after 3 days of its action Efficiency, the results showed that the relative activation rate of HIV latently infected cells was 62% after AspochalasinE treatment.

Embodiment 3

[0025] With final concentration of 20 μg / ml aspochlasinC (R 1 , R 2 , R 3 Respectively H, OH, OH, R 4 and R 5 Forming double bonds) to treat the HIV latent infection cell model, after 3 days of its action, through the fluorescent microscope observation and flow cytometry detection of the reporter gene green fluorescent protein, the activation efficiency of HIV latent infection cells was analyzed, the results showed that HIV latent infection The relative activation rate of the cells after treatment was 80%.

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Abstract

The invention discloses application of Aspochalasin compounds to preparation of anti-HIV (human immunodeficiency virus)-latency drugs and acquired immune deficiency syndrome treating drugs. The Aspochalasin compounds are of the structure shown as formula I, wherein R1, R2, R3, R4 and R5 are one or more than two of hydrogen, hydroxyl, carbonyl, double bond, epoxy, methyl and alkane amide respectively and are the same or different from one another. The Aspochalasin compounds have HIV latency activating effect, can be used with antiretroviral drugs and are capable of removing activated latent infection cells to accelerate latent virus reservoir removal so as to be used for treating the acquired immune deficiency syndrome. Formula I.

Description

technical field [0001] The invention relates to the technical field of drugs for treating AIDS, in particular to the application of Aspochalasin compounds in the preparation of anti-HIV latent drugs and drugs for treating AIDS. Background technique [0002] Acquired immunodeficiency syndrome (AIDS) is an infectious disease caused by HIV (HIV) infection that seriously endangers people's lives and health. Currently, the highly active antiretroviral therapy (HAART) used clinically can Greatly improve the survival time and quality of AIDS patients, but after HIV infects the human body, it will integrate with host cells to form a virus pool that cannot be cleared by HAART. These latent viruses will reactivate and rebound quickly after stopping HAART, so AIDS patients need long-term medication, and long-term medication will cause virus mutation, increased drug resistance, and increased adverse drug reactions to cause treatment failure (Ho, D.D.TowardHIVeradicationorremission:theta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/403A61P31/18
Inventor 马忠俊余立雁丁婉婧朱焕章
Owner ZHEJIANG UNIV
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