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Application of ingenol compound and derivative thereof in anti-HIV treatment

A compound and composition technology, applied in the field of medicine, can solve the problems of high toxicity and side effects, unsatisfactory, etc.

Pending Publication Date: 2020-12-22
SHANGHAI XINHAO BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this strategy has several treatment options in clinical practice, the results are still unsatisfactory. Either the activator is ineffective, or it is effective but has severe side effects. In China, there is only one anti-inflammatory drug with independent intellectual property New AIDS drug launched

Method used

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  • Application of ingenol compound and derivative thereof in anti-HIV treatment
  • Application of ingenol compound and derivative thereof in anti-HIV treatment
  • Application of ingenol compound and derivative thereof in anti-HIV treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0254] Embodiment 1 Preparation of ingenol compound EK-5A of the present invention

[0255] Gansui (E. kansui) root and rhizome 5Kg were extracted twice with 8 times the amount of 95% ethanol under reflux, each time for two hours, and the obtained extract was recovered until it had no alcohol smell to obtain an extract. Add water to dilute to 1000mL, extract three times with an equal volume of dichloromethane, recover the dichloromethane solvent, and obtain 101.2g of dichloromethane extract.

[0256] The conditions of the silica gel column chromatography: the mobile phase used is a petroleum ether-ethyl acetate solution with a volume ratio of 10-2:1. The conditions of the reversed-phase chromatography purification: the filler used is octadecyl bonded silica gel, the mobile phase used is isocratic elution with a volume ratio of 90% methanol-water, and the compound EK-5A ( 80mg), light yellow viscous solid, UV absorption 268nm.

[0257] The separation and purification include:...

Embodiment 2

[0260] Example 2 Preparation of Ingenol compound EK-1A of the present invention

[0261] The roots and rhizomes of E. kansui 5Kg were extracted twice with 8 times the amount of 95% ethanol, respectively, for two hours each time. Add water to dilute to 1000 mL, extract three times with equal volume of dichloromethane, and recover the dichloromethane solvent to obtain 101.2 g of dichloromethane extract.

[0262] The conditions of the silica gel column chromatography: the mobile phase used is a petroleum ether-ethyl acetate solution with a volume ratio of 10-2:1. The condition of described reversed-phase chromatography purification: the filler adopted is octadecyl bonded silica gel, and the mobile phase adopted is that the volume ratio is the isocratic elution of the solution of 86% methanol-water, and the compound EK-1A (15 minutes) is obtained. 30mg), pale yellow viscous solid, UV absorption 268nm.

[0263] The separation and purification includes: after concentrating the ext...

Embodiment 3

[0265] Example 3 Ingenol compounds of the present invention and derivatives thereof efficiently activate the expression of HIV-1 in latent cells

[0266] J-Lat-A10.6 or C11 cells were seeded in a 96-well plate at 2×10E4 cells per well, and 100 μl of 1640 medium (Gibco) containing 10% FBS (Gibco) was added to each well. After the cells were treated with the compounds of Examples 1 and 2 for 48 hours, the green fluorescence expression of the cells was observed under a fluorescence microscope, and the cells were collected for flow cytometry detection to analyze the proportion of fluorescent cells.

[0267] The result is as figure 1 and figure 2 shown. The results showed that the proportion of HIV-positive cells in the latently infected cells treated with no inducer was only about 1-2% of the background activation ( Picture 1-1 and Figure 1-2 ). After treatment with 5ng / ml EK-5A (ie 5A), the proportion of cells expressing green fluorescence in the cell model increased sign...

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Abstract

The invention provides application of an ingenol compound and a derivative thereof in anti-HIV treatment, and in particular provides application of an ingenol compound or pharmaceutically acceptable salts thereof. The ingenol compound or the pharmaceutically acceptable salts thereof can be used for (a) interfering HIV latency; (b) inhibiting HIV infection; and / or (c) reducing the expression of a CD4 cell HIV infected surface receptor. When the compound provided by the invention is used in combination with an AIDS therapeutic agent (such as an anti-retroviral drug, an immunomodulator, a therapeutic antibody or a combination thereof), the elimination of a latent virus reservoir can be accelerated; and the cure rate of AIDS can be easily improved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of ingenol compounds and derivatives thereof in anti-HIV treatment. Background technique [0002] Acquired Immune Deficiency Syndrome (AIDS) is an infectious disease caused by HIV infection that seriously endangers people's lives and health. According to WHO statistics, there are more than 40 million AIDS patients in the world, with 5 million new patients every year, and about 3 million deaths every year. At present, the clinical treatment method of AIDS is mainly highly active antiretroviral therapy (HAART). It blocks the production of HIV at various stages such as recording, virus replication and virus release, thereby significantly reducing the plasma virus of patients, improving the health of HIV patients, prolonging the lifespan of patients, greatly reducing the risk of HIV transmission, and making AIDS a chronic controllable disease. People had hoped that HAART co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/231A61K31/22A61K31/235A61P31/18
CPCA61K31/231A61K31/22A61K31/235A61P31/18
Inventor 朱豫琪张龙飞杨鹤李玄朱焕章
Owner SHANGHAI XINHAO BIOLOGICAL TECH
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