Applications of coumarin compounds in preparing HIV-latency-resisting treatment medicine

A technology for coumarins and therapeutic drugs, which is applied in the field of medicine to achieve the effects of low cytotoxicity and accelerated clearance

Inactive Publication Date: 2016-06-29
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, so far, there has been no report about the latent therapeutic effect of coumarin compounds on HIV

Method used

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  • Applications of coumarin compounds in preparing HIV-latency-resisting treatment medicine
  • Applications of coumarin compounds in preparing HIV-latency-resisting treatment medicine
  • Applications of coumarin compounds in preparing HIV-latency-resisting treatment medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The effect concentration of embodiment 1.Hymecromone and Scoparone compound is on the influence of HIV latent induction activation efficiency

[0043] C11 cells were planted in a 96-well plate at 2×10E4 cells per well, and 100ul of 1640 medium (Gibco) containing 10% FBS (Gibco) was added to each well. After 24 hours, Hymecromone and Scoparone of different concentrations were added to make the final The concentrations are 0 μM, 300 μM, 400 μM, 500 μM, 600 μM, respectively. At least 3 replicate wells for each concentration, and each experiment was repeated 3 times. 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, and the proportion of fluorescent cells was analyzed;

[0044] The results showed that with the increase of the compound concentration of Hymecromone and Scoparone, the number of cells expressing green fluorescence in th...

Embodiment 2

[0045] Embodiment 2.The effect of the action time of Hymecromone and Scoparone compounds on the efficiency of HIV latent induction and activation

[0046] 2 × 10E4 C11 cells were planted in a 96-well plate per well, and 100ul of 1640 medium (Gibco) containing 10% FBS (Gibco) was added to each well. After 24 hours, Hymecromone and Scoparone were added with a final concentration of 500 μM. After treating the cells for 24h, 48h, 72h, and 96h, observe the expression of GFP in the cells under a fluorescent microscope, and collect the cells for flow cytometry detection to analyze the proportion of fluorescent cells. At least 3 replicate wells at each time point, each Each experiment was repeated 3 times, and the kinetic characteristics of induced activation were analyzed and compared;

[0047] The results showed that when Hymecromone and Scoparone respectively treated the HIV latent infection cell model, the number of green fluorescent positive cells gradually increased with the ext...

Embodiment 3

[0048] Example 3. Hymecromone and Scoparone Toxic Effects on Cells

[0049] 2×10E4 normal human peripheral blood mononuclear cells (PBMC) were planted in a 96-well plate, and 100ul of DMEM medium (Gibco) containing 10% FBS (Gibco) was added to each well. After 24 hours, different concentrations were added Hymecromone and Scoparone, so that the final concentrations were 0 μM, 100 μM, 500 μM, 1000 μM, 2500 μM, 5000 μM, each concentration was at least 3 replicate wells, and each experiment was repeated 3 times. After drug treatment of cells for 72 hours, add MTT reagent (0.5mg / mL) (purchased from SIGMA), shake for 1h, measure the OD value at 570nm on the microplate reader;

[0050]The results showed that the half toxic concentration of Hymecromone and Scoparone to human normal cells were CC50=2100μM and CC50=2400μM respectively. The results showed that the toxicity of Hymecromone and Scoparone was lower at the activation concentration, which laid the foundation for clinical appli...

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Abstract

The invention belongs to the field of medicines, and in particular relates to applications of coumarin compounds in preparing an HIV-latency-resisting treatment medicine. The experiment shows that the coumarin compounds provided by the invention have the effect of inducing cells with HIV latency to be activated, and have lower toxicity on cells compared with similar compounds, especially, after the compounds are combined with the medicines capable of resisting the retroviruses, the activated cells with latent infection can be killed, so that the latent viral reservoir can be rapidly cleared, and the coumarin compounds can provide a novel treatment medicine path for the radical cure of AIDS.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of coumarin compounds in the preparation of anti-HIV latent therapeutic drugs. Background technique [0002] Acquired Immunodeficiency Syndrome (AIDS) is an infectious disease caused by HIV infection that seriously endangers people's life and health. According to WHO statistics, there are more than 40 million AIDS patients in the world, with 5 million new patients and 3 million deaths each year. At present, the clinical treatment of AIDS is mainly Highly active antiretroviral therapy (HAART), which not only effectively controls HIV replication, but also can rebuild the immune function of AIDS patients, opening the door of hope for the treatment of AIDS. People once hoped that HAART could completely eliminate HIV in the body, thereby achieving the goal of completely curing AIDS, but subsequent research practice has proved that although HAART can suppress virus ...

Claims

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Application Information

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IPC IPC(8): A61K31/37A61K31/7048A61P31/18
Inventor 朱焕章曲喜英曾汉献刘琳
Owner FUDAN UNIV
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