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Napyradiomycin A4 and application thereof in resisting porcine pseudorabies virus

A porcine pseudorabies and virus technology, applied in antiviral agents, medical preparations containing active ingredients, organic chemistry, etc., can solve the problems of unreported research on antiviral activity, and achieve excellent activity in inhibiting porcine pseudorabies virus , the effect of high drug safety

Pending Publication Date: 2022-07-29
HUBEI BIOPESTICIDE ENG RES CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Napyradiomycin compounds have a unique structure and diverse biological activities, which have important biological significance, but there is no report on the antiviral activity

Method used

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  • Napyradiomycin A4 and application thereof in resisting porcine pseudorabies virus
  • Napyradiomycin A4 and application thereof in resisting porcine pseudorabies virus
  • Napyradiomycin A4 and application thereof in resisting porcine pseudorabies virus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] In the screening of drugs targeting veterinary viruses, the applicant discovered a new compound of the Napyradiomycin class, Napyradiomycin A4, which has strong inhibitory activity against porcine pseudorabies virus, and its structural formula is as follows:

[0018]

[0019] At the same time, the applicant also screened out two other new Napyradiomycin compounds, which are:

[0020] A80915H:

[0021]

[0022] A80915I:

[0023]

[0024] The applicant used the existing Napyradiomycin compounds as a control group:

[0025] Napyradiomycin A1

[0026]

[0027] Napyradiomycin B1:

[0028]

[0029] Naphthomevalin:

[0030]

[0031] A80915G:

[0032]

[0033] A80915G-8″-acid:

[0034]

Embodiment 2

[0036] Determination of the median inhibitory concentration of Napyradiomycin compounds on porcine pseudorabies virus by MTT method

[0037] 1. Cells and viruses

[0038] African green monkey kidney cells (Vero) and porcine pseudorabies virus (PRV) were provided by Professor Tan Chen from Huazhong Agricultural University.

[0039] 2. Viral TCID50 assay

[0040] Half of the tissue culture infectious dose of PRV TCID50 was measured in 96-well plates overgrown with monolayer cells. The virus solution was serially diluted 10 times in maintenance solution, with 8 replicates for each concentration, and cytopathic changes (CPE) were observed daily. , record the virus dilution above 50% and below 50% of the lesions, and calculate the ratio according to the Reed–Muench method to obtain TCID50.

[0041] 3. The median toxic concentration of the drug (CC 50 ) measure

[0042] The 96-well plate was covered with a monolayer of Vero cells, the supernatant was discarded, PBS was added to ...

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Abstract

The invention belongs to the field of novel compounds and antivirus, and particularly relates to Napradiomycin A4 and application of the Napradiomycin A4 in resisting porcine pseudorabies virus. According to the application disclosed by the invention, it is found for the first time that the in-vitro median inhibitory concentration (LC50) of the Nafyradiomycin sA4 on the porcine pseudorabies virus is 0.74 mu g / mL, and the therapeutic index (TI) of the drug of the Nafyradiomycin sA4 is 14.29; the IC50 (14.16 [mu] g / mL) and the TI (2.82) of a positive control ribavirin are obviously higher than those of the positive control ribavirin. According to the present invention, the Napyradiomycin sA4 has characteristics of high drug safety, excellent porcine pseudorabies virus inhibition activity and good application prospect, and can be prepared into the veterinary antiviral preparation so as to be used.

Description

technical field [0001] The invention belongs to the field of novel compounds and antiviral, in particular to Napyradiomycin A4 and its application in anti-porcine pseudorabies virus. Background technique [0002] Pseudorabies virus (PRV) belongs to the alphaherpesvirus subfamily in the family herpesviridae, which causes infectious diseases in domestic animals and some wild animals, among which it is the most harmful to pigs and causes huge economic losses to the world pig industry every year. . Porcine pseudorabies (pseudorabies, PR) is an acute, highly contagious infectious disease caused by porcine pseudorabies virus (PRV) in pigs at different growth stages, characterized by nervous system disorders and organ damage. The disease is harmful to pigs of different ages, and adult pigs become a long-term source of poisoning and detoxification after they are resistant. The World Organization for Animal Health (OIE) classifies the disease as a Class B animal disease, and my cou...

Claims

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Application Information

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IPC IPC(8): C07D311/92A61K31/352A61P31/22
CPCC07D311/92A61P31/22C07B2200/07
Inventor 张亚妮方伟刘曼莉王开梅万中义张志刚刘芳吴兆圆柯少勇石丽桥
Owner HUBEI BIOPESTICIDE ENG RES CENT