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Application of Cetrorelix in the Preparation of Drugs for Treating AIDS

A cetrorelix, AIDS technology, applied in the direction of antiviral agents, pharmaceutical formulations, medical preparations containing active ingredients, etc. methods, etc.

Active Publication Date: 2020-03-17
KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the method of quickly and accurately predicting and discovering the anti-HIV activity of existing drugs in the prior art, and there is no report on the anti-HIV activity of cetrorelix

Method used

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  • Application of Cetrorelix in the Preparation of Drugs for Treating AIDS
  • Application of Cetrorelix in the Preparation of Drugs for Treating AIDS
  • Application of Cetrorelix in the Preparation of Drugs for Treating AIDS

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Testing the anti-HIV effect of Cetrorelix:

[0029] 1. Purpose of the experiment: To test the anti-HIV effect of Cetrorelix

[0030] 2. Experimental materials

[0031] 2.1. Determination of Drugs and Compounds

[0032] The sample to be tested, Cetrorelix, was purchased from Dalian Meilun Biotechnology Co., Ltd. The positive control compound azidothymidine (3'-Azido-3'-deoxythymidine, AZT) was purchased from Sigma. The sample to be tested is dissolved in RPMI-1640 complete medium or DMSO according to solubility, the sample stock solution concentration dissolved in DMSO is 50mM, and the sample stock solution concentration dissolved in RPMI-1640 complete medium is 10mM, 5mM or 2mM ( According to the solubility), the storage conditions are: -20°C; AZT is dissolved in RPMI-1640 complete medium, sterilized by filtration with a 0.22 μm filter membrane, the concentration of the stock solution is 6 mg / ml, and stored at -20°C after aliquoting.

[0033] 2.2. Reagents and solut...

Embodiment 2

[0064] Add 30% acetic acid solution to the compound cetrorelix, pH = 4, filter and dry to prepare the acetate compound.

Embodiment 3

[0066] Add 4% hydrochloric acid solution to the compound cetrorelix, pH = 4, filter and dry to prepare the hydrochloride compound.

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Abstract

The invention relates to application of Cetrorelix to preparation of medicine for treating AIDs. The invention provides a compound of Cetrorelix and a pharmaceutically acceptable salt and application thereof to preparation of medicine for treating AIDs. The human T lymphoid cell series C8166 and HIV-1 experiment strain HIV-1<NL4-3> are used for performing in-vitro cytotoxicity and anti-HIV activity detection; the cytotoxicity is detected by an MTT colorimetric method; the anti-HIV activity is detected by two methods including a synplasm inhibition experiment method and an HIV-1p24 antigen quantitative method. The result proves that the cytotoxicity of the Cetrorelix is very low; CC<50> is higher than 200 muM; when the concentration is EC<5>0(1.788 muM), the Cetrorelix completely has no toxicity on the cell C8166. Therefore the Cetrorelix can be used as the anti-HIV medicine.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of Cetrorelix and pharmaceutically acceptable salts thereof in the preparation of medicines for treating AIDS. [0002] technical background [0003] AIDS is a serious infectious disease caused by Human Immunodeficiency Virus (HIV) infection. As a chronic infectious disease that can directly destroy the human immune system, AIDS has become one of the diseases that seriously threaten human health in the world. According to data from the United Nations Program on AIDS (UNAIDS), as of the end of 2011, a total of 34.2 million people worldwide were infected with HIV. At present, the AIDS epidemic in my country is in a period of rapid growth, with more than 780,000 infected people (UNAIDS, 2011). Therefore, the prevention and treatment of HIV / AIDS has become a social problem and a major scientific research topic that cannot be ignored. The development of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/09A61P31/18
CPCA61K38/09
Inventor 代绍兴黄京飞陈欢郑永唐李功华李文兴
Owner KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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