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Method for inhibiting reproduction of HIV-1 (human immunodeficiency virus-1) drug-resistant virus

A technology for HIV-1 and drug resistance, applied in antiviral agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as decreased drug sensitivity

Inactive Publication Date: 2013-04-17
LP PHARM (XIAMEN) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the HIV-1 fusion inhibitor T20 has been reported to induce T20 drug-resistant variants in vitro, and the sensitivity of the mutants to T20 decreased by 5 to 684 times. T20 drug-resistant variants have also been isolated clinically, and their sensitivity to T20 decreased by 4 to 684 times. 422 times
For protease inhibitors commonly used in clinical practice, such as nelfinavir, saquinavir, lopinavir, etc., long-term use will also produce drug resistance and reduce drug sensitivity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Inhibitory effect of 1'(S)-acetoxypiperol acetate and 2,-difluoro-1'-acetoxypiperol acetate on replication of HIV-1 fusion inhibitor T20 resistant strain: in acute Infected C8166 cells, adding HIV-1 fusion inhibitor T20 drug-resistant strain pNL4-3 gp41(36G)V38A，N42T Stock solution at 37 °C, 5% CO 2 Incubate for 2 hours in the incubator. After washing by centrifugation for 2 times to wash away the free drug-resistant strain virus on the cell surface, 100 μl of C8166 cell suspension (4×10 5 / ml) were mixed with different concentrations of 100μl 1'(S)-acetoxypiperol acetate and 100μl 2,3-difluoro-1'-acetoxypiperol acetate, and added to the In each well, place at 37°C, 5% CO 2 Incubator for 3 days. Collect the cell culture supernatant, inactivate the virus with 5% Triton X-100, and use the ELISA method to measure the production of HIV-p24 antigen in the culture supernatant of the C8166 cell culture supernatant infected by the drug-resistant strain of HIV-1 fusion inhib...

Embodiment 2

[0020] Inhibitory effects of 1'(S)-acetoxypiperol acetate and 2,3-difluoro-1'-acetoxypiperol acetate on the replication of HIV-1 protease-resistant strains: in acute infection C8166 Add HIV-1 protease resistant strain HIV-1RF / V82F / 184V storage solution to the cells. at 37°C, 5% CO 2Incubate for 2 hours in the incubator. After centrifuging and washing twice to wash away the free drug-resistant strain virus on the cell surface, 100 μl of C8166 cell suspension (4×10 5 / ml) were mixed with different concentrations of 100μl 1'(S)-acetoxypiperol acetate and 100μl 2,3-difluoro-1'-acetoxypiperol acetate, and added to the In each well, place at 37°C, 5% CO 2 Incubator for 3 days. Collect the cell culture supernatant, inactivate the virus with 5% Triton X-100, and use the ELISA method to quantitatively measure the production of HIV-p24 antigen in the culture supernatant of C8166 cells infected with HIV-1 protease-resistant strains. A test drug group was added as a control group. R...

Embodiment 3

[0022] Cytotoxic effects of 1'(S)-acetoxypiperol acetate and 2,3-difluoro-1'-acetoxypiperol acetate on C8166 cells: 1'(S)-acetoxy Piperonyl acetate and 2,3-difluoro-1'-acetoxypiperol acetate were dissolved in dimethyl sulfoxide, diluted with C8166 cell culture medium to prepare sample test solutions with different concentrations, and 100 μl was added to To each well of a 96-well culture plate, no 1'(S)-acetoxypiperol acetate and 2,3-difluoro-1'-acetoxypiperol acetate group was added as a blank control . Then add 100 μl of 4×10 to each well 5 / ml C8166 cell suspension, cultured in an incubator with 5% carbon dioxide at 37°C for 3 days. Add 100 μl of MTT solution to each well and continue to incubate for 3 hours. The solution in each well was then removed, and dimethyl sulfoxide was added to dissolve the precipitate. Absorbance was measured at a wavelength of 570nm and compared with the blank. Results Neither 1.2nM 1'(S)-acetoxypiperol acetate nor 0.5nM 2,3-difluoro-1'-acet...

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PUM

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Abstract

The invention determines 1'-acetoxychavicol acetate and derivative thereof with a new function of inhibiting the reproduction of HIV-1 (human immunodeficiency virus-1) drug-resistant virus. The 1'-acetoxychavicol acetate and the derivative thereof can effectively inhibit the reproduction of the HIV-1 drug-resistant virus generated by an HIV-1 fusion inhibitor and a protease inhibitor under low consistency, and does not display cytotoxicity on host cells. Therefore, the 1'-acetoxychavicol acetate and the derivative thereof have potential application prospect in treating AIDS patients with drug resistance.

Description

technical field [0001] The present invention relates to a new field of medicine application. Involves a new method of inhibiting the replication of HIV-1 drug-resistant virus. Background technique [0002] At present, the main drugs used in the treatment of AIDS can be divided into nucleoside reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, protease inhibitors, and fusion inhibitors. The mechanism of action of these drugs is to act on different stages of HIV-1 replication, and their long-term use can make HIV resistant to drugs. For example, HIV-1 fusion inhibitor T20 has been reported to induce T20 drug-resistant variants in vitro, and the sensitivity of the mutants to T20 decreased by 5 to 684 times. T20 drug-resistant variants have also been isolated clinically, and their sensitivity to T20 decreased by 4 to 684 times. 422 times. For protease inhibitors commonly used in clinical practice, such as nelfinavir, saquinavir, lopinavir, etc....

Claims

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Application Information

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IPC IPC(8): A61K31/222A61P31/18
Inventor 叶英
Owner LP PHARM (XIAMEN) CO LTD
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