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Application of phenylamine acid compound in preparing anti-HIV latent medicament

A technology of aniline acid and compounds, applied in the field of preparation of anti-HIV latent drugs, can solve the problems that MGCD0103 and MS275 have anti-HIV latent therapeutic effects, etc.

Inactive Publication Date: 2011-04-06
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] So far, there is no report that MGCD0103 and MS275 have anti-HIV latent therapeutic effect

Method used

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  • Application of phenylamine acid compound in preparing anti-HIV latent medicament
  • Application of phenylamine acid compound in preparing anti-HIV latent medicament
  • Application of phenylamine acid compound in preparing anti-HIV latent medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Embodiment 1.MGCD0103 or the effect concentration of MS275 compound on the influence of HIV latent induction activation efficiency

[0062] A7 cells were planted in a 96-well plate at 2×10E4 cells per well, and 100 ul of 1640 medium (Gibco) containing 10% FBS (Gibco) was added to each well. After 24 hours, different concentrations of MGCD0103 and MS275 were added to make the final concentrations 0nM, 25nM, 50nM, 100nM, 200nM, 400nM, 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 to analyze the proportion of fluorescent cells.

[0063] The results showed that as the concentration of MGCD0103 and MS275 compounds increased, the number of cells expressing green fluorescence in the cell model increased; HIV latent infection c...

Embodiment 2

[0064] Example 2. Effect of the action time of MGCD0103 or MS275 compound on the efficiency of HIV latent induction and activation

[0065] 2×10E4 A7 cells per well were planted in a 96-well plate, and 100 ul of 1640 medium (Gibco) containing 10% FBS (Gibco) was added to each well. After 24 hours, MGCD0103 and MS275 were added at a final concentration of 200 nM. After 24h, 48h, 72h, and 96h of drug-treated cells, the expression of GFP in the cells was observed under a fluorescent microscope, and the cells were collected for flow cytometry detection to analyze the proportion of fluorescent cells. There were at least 3 replicate wells at each time point, and each experiment was repeated 3 times. Analyze and compare the kinetic characteristics of induced activation induced activation.

[0066] The results showed that when MGCD0103 or MS275 treated the HIV latent infection cell model respectively, the number of green fluorescent positive cells gradually increased as time went on...

Embodiment 3

[0067] Example 3. Toxic effect of MGCD0103 or MS275 on cells

[0068] 2×10E4 normal human embryonic kidney cells (293HEK) were planted in a 96-well plate per well, and 100 ul of DMEM medium (Gibco) containing 10% FBS (Gibco) was added to each well. After 24 hours, different concentrations of MGCD0103 and MS275, and the positive control drug Trichostatin A (TSA) were added, so that the final concentrations were 0nM, 25nM, 50nM, 100nM, 200nM, 400nM, 800nM. 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, MTT reagent (0.5 mg / mL) (purchased from SIGMA) was added to each well, shaken for 1 hour, and the OD value was measured at 570 nm on a microplate reader. Calculate CC50=(OD value of experimental group / OD value of control group)×100%.

[0069] The results showed that the half toxic concentrations of MGCD0103 or MS275 to human normal cells were CC50=612nM and CC50=370nM respectively...

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Abstract

The invention belongs to the field of medicaments, and relates to application of a phenylamine acid compound in preparing a medicament for inducing activation of HIV latent cells. The phenylamine acid compound comprises MGCD0103 or MS275. One important reason that the HIV is difficult to be completely cleared in vivo is that the HIV-1 can be concealed in resting memory CD4+T cells. The phenylamine acid compound has the effect of inducing the activation of HIV latent cells; when being added into cell culture solution, the phenylamine acid compound can induce the activation of HIV latent cells; and the phenylamine acid compound also can form an anti-HIV medicinal composition together with methyltransferase inhibitor or cytokine or NF-kB signal activating agent, and also can be used with the conventional HIV medicament to well inhibit and eliminate HIV viruses. Compared with similar compounds, the phenylamine acid compound has good effect of inducing the activation of HIV latent cells, and mainly has low toxicity to cells.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the application of aniline acid compounds in the preparation of anti-HIV latent drugs. It specifically relates to the application of aniline acid compounds MGCD0103 and MS-275 in the preparation of anti-HIV latent 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 to completely eliminate HIV in the body by virtue of HAART, so as to achieve t...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K31/4406A61P31/18C12N5/0786C12N5/0783C12N5/0784C12N5/0787C12N5/0793C12N5/079C12N5/071
Inventor 朱焕章英昊
Owner FUDAN UNIV
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