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Application of monoiodoaromatic acids as CVB3 virus inhibitor

A technology of virus inhibitors and aromatic acids, which is applied in the direction of antiviral agents, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems that the inhibitory activity has not been reported, and achieve enhanced cell survival rate, simple structure, Good anti-CVB3 virus effect

Active Publication Date: 2020-03-24
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the antiviral activity of iodocarboxylic acids, including the inhibitory activity against CVB3 virus, has not been reported so far.

Method used

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  • Application of monoiodoaromatic acids as CVB3 virus inhibitor
  • Application of monoiodoaromatic acids as CVB3 virus inhibitor
  • Application of monoiodoaromatic acids as CVB3 virus inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: Monoiodoaromatic acid L 1 , L 2 , L 3 Toxicity to host Hep-2 cells

[0032] Hep-2 cells were plated in 96-well plates at 37°C, 5% CO 2 After the incubator grows a monolayer, discard the cell culture medium and add different concentrations of L 1 , L 2 , L 3 After 48 hours, the cytotoxicity was recorded under a microscope, and the cell viability was measured by MTT method. The specific steps of the MTT method are as follows: add 30 μL of MTT (5 mg·mL -1 ), after incubation for 3-4 h, the supernatant was removed, and 50 μL of DMSO was added to dissolve the precipitate. Read the corresponding absorbance (OD) at 492 nm with a microplate reader 492 value).

[0033] SPSS 11.5 software was used to calculate the median toxic concentration (Median cyctoxic concentration, CC50) of the drug on the cells.

[0034] Cell viability=(average OD of drug group 492 Value / average OD of cell control group 492 value)×100%

Embodiment 2

[0035] Embodiment 2: Monoiodoaromatic acid L 1 , L 2 , L 3 Inhibitory activity against CVB3

[0036] Hep-2 cells were plated in 96-well plates at 37°C, 5% CO 2 After the monolayer was grown in the incubator, discard the culture medium, infect the cells with 100TCID50 CVB3 virus solution for 1h, and add different concentrations (2.5μg / mL, 5μg / mL, 10μg / mL, 20μg / mL, 40μg / mL, 80μg / mL) of compound L 1 , L2 , L 3 (ribavirin as a positive control drug) to incubate the cells. After continuing to culture for about 48 hours, when about 90% of the CPE lesions appeared in the virus control wells, the cytopathic effect (CPE) was observed under a microscope. Observation and recording method of CPE: No cytopathic disease is marked as -, cytopathic disease of less than 25% is recorded as +, 25%-50% cytopathic disease is recorded as ++, 50%-75% cytopathic disease is recorded as +++, more than 75% Cytopathy was recorded as ++++.

[0037] After the observation of CPE, the inhibitory rat...

Embodiment 3

[0049] Embodiment 3: monoiodoaromatic acid L 3 Inhibition of CVB3 Progeny Virus Yield

[0050] Hep-2 cells in the logarithmic growth phase were plated in 24-well plates, and 100TCID after the monolayer was overgrown 50 CVB3 infected cells, incubated at 37°C for 1.5h, removed the virus solution, washed three times with PBS, and added cell maintenance solution containing 50 μg / mL L3 respectively. Cells and supernatant culture fluid were collected at 12h and 36h respectively, and after three freeze-thaw lysis at -20°C and 37°C, TCID 50 Methods To determine the titer of CVB3 virus.

[0051] The result is as image 3 As shown, the CVB3 virus control group showed obvious virus titers at 12 hours after infection, and the virus titers rose rapidly by about 3.0log until 36 hours after infection. while 50μg / mL L 3 The virus titer of the treatment group was lower than that of the virus control group under the same time conditions, the increase was small from 12h to 36h after virus ...

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Abstract

The invention discloses application of monoiodoaromatic acids as a CVB3 virus inhibitor. Through the research experiment on the anti-CVB3 activity of monoiodoaromatic acids, it shows that the monoiodoaromatic acids have a certain inhibitory activity on CVB3 virus, including inhibiting the cytopathic effect (CPE) of CVB3 on the host cell Hep-2 and enhancing cell survival rate. The monoiodoaromaticacids have an inhibitory effect on CVB3 virus, and it shows that the monoiodoaromatic acids have the potential to be applied in preparing anti-CVB3 virus drugs.

Description

technical field [0001] The invention relates to the technical field of antiviral drugs, in particular to the application of a monoiodoaromatic acid as a coxsackie virus inhibitor. Background technique [0002] Coxsackievirus (CV) is a member of Picornaviridae Enterovirus, its infection can cause a variety of diseases, such as hand, foot and mouth disease, aseptic meningitis, encephalitis, myocarditis , epidemic myositis, herpetic angina, etc. There are 29 serotypes of CV reported, which can be divided into two groups, A and B, according to their pathogenic characteristics and cell sensitivity to suckling mice, namely CVA (CVA1-22, 24) and CVB ( CVB1-6). CVBs infection is the most common, among which CVB3 is the most pathogenic type among the six CVB serotypes, and is the main cause of viral myocarditis. According to the statistics of the US Centers for Disease Control and Prevention (CDC), CVB (type 1-6) can cause about 5 million people to suffer from intestinal system di...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61P31/14
CPCA61K31/192A61P31/14A61K2300/00
Inventor 王龙胜郭超魏艳红李妮朱茂春王悦袁子月彭超华
Owner HUBEI UNIV OF TECH
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