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Drugs that cause neuroinflammation-mediated neuronal damage following HIV infection

A technology of AIDS and drugs, which is applied in the application field of drugs for the prevention and treatment of neuron damage caused by HIV-1 Tat protein, and can solve the problems of limited activity and limited effect of lignan compounds

Inactive Publication Date: 2020-06-26
XUZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, naturally derived kalinoids have limited activity, especially in the treatment of neuroinflammation-mediated neuronal damage following HIV infection

Method used

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  • Drugs that cause neuroinflammation-mediated neuronal damage following HIV infection
  • Drugs that cause neuroinflammation-mediated neuronal damage following HIV infection
  • Drugs that cause neuroinflammation-mediated neuronal damage following HIV infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1: synthetic embodiment

[0019]

[0020]

[0021] resolve resolution:

[0022] Compounds with similar structures to lignan were obtained according to CN201110439347.X, amantadine was purchased from Sigma Chemical Reagent Company, and others were regular reagents in the laboratory. Dissolve triethylamine in ethyl acetate, add lignan structurally similar compounds and amantadine at a molar ratio of 1:1, add HOBT and DCC in excess molar ratio in turn under stirring conditions, filter to remove the precipitate after the reaction is completed, and the filtrate Concentrate to dryness under reduced pressure, add diethyl ether to extract twice, combine the diethyl ether layers, wash with saturated brine, and dry. Filtrate, concentrate under reduced pressure to remove diethyl ether, and pass the residue through a silica gel column with petroleum ether: ethyl acetate = 1:4 to obtain a white solid which is the target product. MS m / z=471 (M + ) for elemental an...

Embodiment 2

[0025] Embodiment 2: pharmacodynamic experiment

[0026] (1) Main reagents, cells and instruments

[0027] HIV-1Tat protein was purchased from Shenzhen Baiwansen Bio-Trade Co., Ltd. (Prospec, USA). Rat adrenal pheochromoma cell line (PC12) was purchased from Shanghai Institute of Cells, Chinese Academy of Sciences. MTT was purchased from Sigma Company; LDH (lactate dehydrogenase) detection kit was purchased from Nanjing Jiancheng Institute of Bioengineering; Tunel detection kit was purchased from Promega Company of the United States. Inactivated fetal bovine serum was purchased from Hangzhou Sijiqing Bioengineering Materials Co., Ltd.; horse serum, DMEM medium and MEM medium were purchased from Gibco; other reagents were of analytical grade. Microplate reader (USA BIOTEK company); Olympus microscopic imaging system (Olympus,

[0028] FV10); Mcllwain automatic tissue slicer (CAMPDEN, 220-240); oscillating slicer (LR59590, USA).

[0029] PC12 cells are rat adrenal pheochromo...

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Abstract

The invention discloses a drug for treating neuroinflammation-mediated neuron injury after HIV infection, and the drug contains active ingredients shown in the following formula.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and relates to lignanin derivatives and applications thereof, that is, the application of lignanin derivatives in the preparation of drugs for the prevention and treatment of AIDS nervous system damage, especially in the prevention and treatment of nervous system damage caused by HIV-1 Tat protein. Applications in meta-damaging drugs. Background technique [0002] AIDS is Acquired Immunodeficiency Syndrome, which is an immune dysfunction disease caused by infection with Human Immunodeficiency Virus (HIV). HIV belongs to the human lentivirus group in the genus Lentivirus of the Retroviridae family. After entering the human body, HIV selectively invades CD4 + T lymphocytes lead to severe impairment of the body's cellular immunity, which increases the susceptibility of the body to tumors and the incidence of opportunistic infections. Monocytes infected with HIV can enter the central nervous syste...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/166A61K45/06A61P31/18A61P25/00
CPCA61K31/166A61K45/06
Inventor 周峰郑葵阳高殿帅汤仁仙刘晓梅左冬姣高林曹倩文李小翠
Owner XUZHOU MEDICAL UNIV