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Use of catechin for preparing retrovirus integrase inhibitors

An integrase inhibitor, retrovirus technology, applied in the direction of antiviral agents, drug combinations, medical preparations containing active ingredients, etc. Small side effects, good therapeutic effect and low cost

Inactive Publication Date: 2010-06-30
赵亚力 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The cost of the drug is high, the side effects are large, and it can only reduce the viral load to a certain extent, relieve the condition, and the treatment effect is poor

Method used

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  • Use of catechin for preparing retrovirus integrase inhibitors
  • Use of catechin for preparing retrovirus integrase inhibitors
  • Use of catechin for preparing retrovirus integrase inhibitors

Examples

Experimental program
Comparison scheme
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specific Embodiment 1

[0031] Specific embodiment one, taking HIV as an example the mechanism of action of the present invention is described in detail:

[0032] Integrase is a key enzyme in the life cycle of HIV, and its importance is no less than that of protease and reverse transcriptase. It is the key enzyme for the integration of HIV into the human genome. Therefore, designing drugs that inhibit HIV against integrase can prevent HIV from entering the human genome, thereby completely curing AIDS. At the same time, there is no protein structure homologous to HIV integrase in the human body, so the toxic and side effects of the enzyme-related drugs are reduced.

[0033] Each HIV virion carries 40-100 integrases. The main function of integrase is to integrate the viral cDNA into the host genome. After reverse transcription, HIV forms double-stranded cDNA, and in the host cell cytoplasm, HIV begins to mediate 3'-processing under the action of integrase. The integrase first recognizes the two ter...

specific Embodiment 2

[0041] Specific embodiment two, taking human T lymphotropic virus as an example:

[0042] Human T-cell Lymphotropic Virus (HTLV) belongs to retrovirus in virus classification. There are two types of human T-lymphotropic virus: HTLV-I and HTLV-II. Studies have shown that HTLV-I is the pathogenic factor of adult T-lymphoblastic leukemia (ATL), and tumor cells in the patient's blood or tissue are expressed as CD + 4 Mainly, it is often accompanied by enlarged liver, spleen, and lymph nodes, as well as elevated serum calcium, bilirubin, lactate dehydrogenase, and leukocytes. The condition of adult T-lymphoblastic leukemia is progressive, and the prognosis is extremely poor.

[0043] HTLV-I can also cause tropical spastic paraplegia, HTLV-I-associated myelopathy (TSP / HAM) and other diseases. TSP / HAM is a chronic, progressive neurological disorder characterized by degeneration of the spinal cord and CD in peripheral blood and cerebrospinal fluid + 4 Infiltration of cytotoxic T ...

specific Embodiment 3

[0046] Through a large number of experimental screening, the catechin compounds with galloyl groups have inhibitory effect on HIV-1 integrase, can prevent HIV from entering the human genome, hinder its stable expression, and bring hope for a complete cure of AIDS.

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Abstract

The invention discloses use of catechin for preparing retrovirus integrase inhibitors; the catechin is added in the retrovirus integrase inhibitors; the retrovirus integrase inhibitors can be combined in the vicinity of flexible ring of integrase of AIDS virus, human T-lymphotropic virus or other retrovirus so as to influence processing function and chain transfer function; furthermore, the catechin can be combined in the vicinity of divalent metal of integrase so as to influence the combination of integrase and divalent metal and reduce the activity; and the catechin can interfere combination of integrase and cofactor, and reduce probability of integrating the retrovirus into host gene. Simultaneously, the integrase does not have highly homologous protein structure in human body, thus the inhibitor thereof has little side effect. The catechin is used for preparing the medicine for treating the diseases such as AIDS, leukemia T-cell prolymphocytic caused by retrovirus; and the medicine has good treating effects, low cost and little side effect.

Description

technical field [0001] The invention relates to a retrovirus integrase inhibitor, in particular to the application of catechin in the preparation of the retrovirus integrase inhibitor. Background technique [0002] Retroviruses, such as human immunodeficiency virus (HIV), also known as HIV, are the main cause of AIDS. There are two types of HIV, namely HIV-1 and HIV-2. Among them, HIV-1 is the main pathogen that causes AIDS and is also an important direction of HIV research. [0003] Acquired immunodeficiency syndrome (AIDS for short), also known as AIDS, is a worldwide epidemic. AIDS spreads quickly, has a high mortality rate, and is still incurable. It is a serious worldwide epidemic and poses great harm to people's health. [0004] In the prior art, most of the drugs for preventing and treating AIDS are reverse transcriptase and protease against HIV-1. There are more than 20 kinds of AIDS drugs on the market, mainly protease inhibitors and reverse transcriptase inhibit...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61P31/18A61P35/02A61P35/00
Inventor 赵亚力姜凡易可佳
Owner 赵亚力
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