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Application of lapachol to preparation of anti-human-immunodeficiency-virus-1 (HIV-1) medicine

A technology of HIV-1 and Lappaol, which is applied in the field of medicine and biology, can solve problems such as the report of no compound Lappaol, and achieve the effect of solving the problem of drug resistance

Inactive Publication Date: 2013-01-23
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In the prior art, there is no report on compound lapacol in the preparation of anti-HIV-1 virus medicines

Method used

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  • Application of lapachol to preparation of anti-human-immunodeficiency-virus-1 (HIV-1) medicine
  • Application of lapachol to preparation of anti-human-immunodeficiency-virus-1 (HIV-1) medicine
  • Application of lapachol to preparation of anti-human-immunodeficiency-virus-1 (HIV-1) medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Compound Lappaol inhibits Vpu down-regulation of BST-2 on the cell surface

[0032] Hela-Vpu cells stably expressing Vpu protein were constructed and screened by Cen Shan et al. (Cen Shan et al.. Screening of antiviral drugs that antagonize the activity of Vpu degrading BST-2. Patent application number: 201010123002.1), and BST-2 on its surface was screened by Vpu Down-regulated, lower than normal Hela.

[0033] Seed Hela cells and Hela-Vpu cells in a 96-well plate with 1.0×10 cells per well 4 indivual. At 37°C, 5% CO 2 After culturing in the incubator for 24 hours, dimethyl sulfoxide (DMSO) and Lappaol were added to treat them respectively. After continuing to culture for 24 hours, the expression level of BST-2 on the cell membrane surface was detected by Cell-ELISA. The detection process is as follows: suck off the old culture medium, wash twice with PBS, 2 min each time. Add 100 μl of 4% paraformaldehyde to each well and fix at room temperature for 20 m...

Embodiment 2

[0035] Effect of Example 2 Compound Lappaol on the Transcription of BST-2mRNA

[0036] In order to determine the effect of the compound lapachol on BST-2 mRNA transcription, Hela-Vpu cells were seeded in 6-well plates with 2.0×10 cells per well. 5 indivual. 37°C, 5% CO 2 After culturing in the incubator for 24 hours, DMSO and Lappaol were added for treatment, and after culturing for another 24 hours, total cellular RNA was extracted according to the instructions of Invitrogen's TRIZOL. After the concentration was determined, 2 μg of total RNA was taken, and the RNA was reverse-transcribed into cDNA using M-MLV reverse transcriptase and random primers.

[0037] cDNA amplification reaction system: SsoFast EvaGreen Supermix 10 μl, forward primer (10 μM) 1 μl, reverse primer (10 μM) 1 μl, template cDNA 0.5 μl, RNase-free water 7.5 μl. The reaction condition is 95°C, 30 sec; then 40 cycles, each cycle condition is 95°C, 5 sec; 60°C, 20 sec. The melting curve is 65°C-95°C, conti...

Embodiment 3

[0043] The influence of the Vpu expression level of embodiment 3 compound Lappaol

[0044] Hela-Vpu cells were seeded in a 6-well plate with 2.0×10 cells per well 5 indivual. 37°C, 5% CO 2 After culturing in the incubator for 24 hours, add dimethyl sulfoxide, concanavalin A, and lapachol for treatment, and continue culturing for 24 hours. Scrape the cells in the 6-well plate, resuspend in 1ml pre-cooled PBS, 2×10 3 Collect the cells by centrifugation at g for 5 minutes, remove the supernatant, add 50 μl of pre-cooled PBS to resuspend, then add 50 μl of 2× loading buffer to lyse the cells, bathe in boiling water for 10 minutes, and vortex every 3 minutes. SDS-PAGE separated protein samples. After transferring to PVDF membrane, it was incubated with primary antibody and secondary antibody successively, and then developed by ECL. The primary antibody uses the following concentrations of rabbit polyclonal BST-2 antibody (1:5000), rabbit polyclonal Vpu antibody (1:1000), mouse...

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Abstract

The invention relates to the application of lapachol to the preparation of an anti-human-immunodeficiency-virus-1 (HIV-1) medicine. The medicine can prevent host limiting factor BST-2 from being degraded by HIV-1 accessory protein Vpu, and improve content of BST-2 on cell surfaces, thereby preventing the liberation of HIV-1.

Description

technical field [0001] The invention belongs to the field of medicine and biology, and in particular relates to the application of lapacol in the preparation of anti-HIV-1 virus medicines. Background technique [0002] Virus drug resistance is the most urgent problem to be solved in current AIDS drug treatment. Drug resistance is the result of mutations in the virus's drug-targeting protein. Because drug-resistant strains are often resistant to a group of antiviral drugs, and cross-resistance between the same class of drugs is very common. The main reason why HIV-1 can rapidly develop drug resistance against the existing clinically used antiviral drugs is that the targets of these drugs are the virus itself. The pathogenic virus is naturally highly mutated, and under the selection pressure of drugs, it is easy to cause rapid mutation of the virus and thus drug resistance. Therefore, one of the keys to solving the drug resistance problem of HIV-1 is to break through the tr...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61P31/18
Inventor 岑山张全米泽云李晓宇周金明殷霄马铃
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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