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Application of 2-furan acrolein compounds in the preparation of anti-human gamma herpes virus drugs

A furan acrolein and compound technology, which is applied in the directions of antiviral agents, antitumor drugs, and drug combinations, can solve the problems of single drug type, obvious toxic and side effects, and weakened curative effects, and achieves increased lethality, reduced morbidity, and improved The effect of immunity

Active Publication Date: 2019-08-23
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, the types of drugs are too single, and the activity is poor, and the toxic and side effects are obvious.
Although new purine nucleoside analogue drugs such as acyclovir (Acyclovir) and its derivatives are effective against α- and β-subtype herpesvirus infections, the curative effect on tumor viruses EBV and KSHV is significantly weakened. Clinically, there is no drug specifically targeting the cleavage and replication of human gamma herpesvirus

Method used

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  • Application of 2-furan acrolein compounds in the preparation of anti-human gamma herpes virus drugs
  • Application of 2-furan acrolein compounds in the preparation of anti-human gamma herpes virus drugs
  • Application of 2-furan acrolein compounds in the preparation of anti-human gamma herpes virus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Compound screening, the steps are as follows:

[0049] 1. Compound library preprocessing: The virtual screening compound library is a self-prepared compound database. The compound database is processed as follows: removing ions and complexing water molecules, adding charges, protonating, and generating three-dimensional conformations. These processes were completed in the drug design software package Discovery Studio 3.0. Wherein the protonation is carried out under the condition of pH 6.5-8.5. Prepare small molecule libraries for virtual screening.

[0050] 2. Searching the database for substructure matching based on the structure of 2-furan acrolein to find out the compound containing the parent nucleus. Finally, 26 compounds were selected for cytological experiments.

Embodiment 2

[0052] KSHV, EBV cleavage replication inhibitory activity assay, the specific steps are as follows:

[0053] 1. Cell culture: BCBL-1 (latent KSHV infected cell line) and P3HR-1 cells (EBV latent infected cell line) were cultured in vitro. The RPMI 1640 medium containing 10% fetal bovine serum was used for routine maintenance and passage at 37°C and 5% carbon dioxide concentration.

[0054] 2. Drug intervention: adjust the logarithmic growth phase so that the cell density of BCBL-1 (KSHV positive cells) and P3HR-1 (EBV positive cells) is 3×10 5 cells / ml, use 20ng / mL TPA+0.3mM butyrate for induction treatment to induce the virus in the cells to enter the lytic replication phase. After the cells were treated with the inducer for 3 hours, the cells were treated with different concentrations of compounds (C10, H1-H25), and three parallel wells were set up for each concentration, and a control group without TPA induction and without compound treatment was set up. Compare.

[0055...

Embodiment 3

[0060] Embodiment 3 suppresses KSHV, EBV virus particle release experiment

[0061] 1. Cell culture: BCBL-1 cells were cultured in vitro. RPMI 1640 medium containing 10% fetal bovine serum, 100 U / ml penicillin, and 100 μg / ml streptomycin was used for routine maintenance and passage at 37° C. and 5% carbon dioxide concentration.

[0062] 2. Drug intervention: adjust the density of BCBL-1 cells in the logarithmic growth phase to 3×10 5 cells / ml, use 20ng / mlTPA to induce BCBL-1 cells to enter the lytic replication phase. The compounds to be tested were prepared in different concentrations using DMSO. After BCBL-1 cells were treated with TPA for 3 hours, the cells were treated with different concentrations of compounds (C10, H1~H25), and three parallel wells were set up for each concentration, and no compound treatment and no TPA-induced controls were set up. group for comparison.

[0063] 3. Test method: After the cells were induced by TPA for 5 days, the cell culture solutio...

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Abstract

The invention discloses application of a 2-furan acrylaldehyde compound to preparation of a medicine for resisting human gamma-herpes virus. The 2-furan acrylaldehyde compound provided by the invention can be used for inhibiting lytic replication of the human gamma-herpes virus; compared with a marketing drug, namely acyclovir, the 2-furan acrylaldehyde compound has relatively small toxicity and the activity is equivalent. Therefore, the compound has a good application prospect in treatment of related diseases caused by KSHV (Kaposi's Sarcoma-associated Herpesvirus) and EBV (Ebola Virus) infection.

Description

technical field [0001] The invention relates to the field of biopharmaceuticals, in particular to the application of 2-furan acrolein compounds in the preparation of anti-human gamma herpes virus drugs. Background technique [0002] There are two subtypes of human gammaherpesviruses, including Kaposi's sarcoma-associated herpesvirus (KSHV) and Epstein-Barr virus (EBV). Kaposi's sarcoma-associated herpesvirus, also known as human herpesvirus type 8 (HHV-8), belongs to the gamma subtype herpesvirus. Epstein-Barr virus is also called human herpes virus type 4 (HHV-4). KSHV and EBV belong to the same genus of herpes virus and have strong homology. Often called sister herpes virus. [0003] KSHV was first discovered in the sarcoma tissues of Kaposi's sarcoma (Kaposi's sarcoma, KS) patients by the pathologist Chang et al. of Columbia University in 1994 by means of representative difference analysis. It is a double-stranded DNA virus with a genome length of about 140kb. Epstei...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/351A61K31/506A61K31/381A61P31/22A61P35/00
Inventor 徐峻袁岩徐梦阳钟灿榕
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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