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Application of Monoiodoaromatic Acids as CVB3 Virus Inhibitors

A technology of aromatic acid and iodine, which is applied in the direction of antiviral agents, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of unreported inhibitory activity, achieve enhanced cell survival rate, high therapeutic index, reduce Effect of Progeny Virus Yield

Active Publication Date: 2022-01-14
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 Inhibitors
  • Application of Monoiodoaromatic Acids as CVB3 Virus Inhibitors
  • Application of Monoiodoaromatic Acids as CVB3 Virus Inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0032] Plate Hep-2 cells in 96-well plates at 37°C, 5% CO 2 After the incubator is full of monolayers, discard the cell culture medium, and add different concentrations of L 1 , L 2 , L 3 The cytotoxicity was recorded by microscope after 48 hours, and the cell viability was determined by MTT method. The specific steps of the MTT method are as follows: add 30 μL of MTT (5 mg·mL to each well) -1 ), the supernatant was removed after incubation for 3-4 h, 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] The Median cyctoxic concentration (CC50) of the drug to cells was calculated by SPSS 11.5 software.

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

Embodiment 2

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

[0036] Plate Hep-2 cells in 96-well plates at 37°C, 5% CO 2 After the incubator was full of monolayers, the culture medium was discarded, the CVB3 virus solution of 100 TCID50 was used to infect the cells for 1 h, and different concentrations (2.5 μg / mL, 5 μg / mL, 10 μg / mL, 20 μg / mL, 40 μg / mL, 80 μg) were added respectively. / mL) of compound L 1 , L2 , L 3 (ribavirin as a positive control drug) cells were incubated. After culturing for about 48 hours, when about 90% of CPE lesions appeared in the virus control wells, the cytopathic effect (CPE) was observed under a microscope. CPE observation and recording method: no cytopathic lesions are recorded as -, 25% or less cytopathic lesions are recorded as +, 25%-50% cytopathic lesions are recorded as ++, 50%-75% cytopathic lesions are recorded as +++, more than 75% cytopathic lesions are recorded as +++ Cytopathies were recorded as ++++...

Embodiment 3

[0049] Example 3: Monoiodoaromatic Acid L 3 Inhibition of CVB3 Progeny Virus Yield

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

[0051] The result is as image 3 As shown, the CVB3 virus control group showed obvious virus titer at 12h of infection, and the virus titer rose rapidly until 36h of infection, with an increase of about 3.0 log. 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 range was small in the time period from 12h ...

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Abstract

The invention discloses the application of monoiodo aromatic acid as CVB3 virus inhibitor. Through the research on the anti-CVB3 activity of several monoiodoaromatic acids, it was shown that the monoiodoaromatic acid exhibited certain inhibitory activity on CVB3 virus, including inhibiting the cytopathic effect (CPE) produced by CVB3 on the host cell Hep‑2 , enhance cell viability, monoiodoaromatic acid has inhibitory effect on CVB3 virus, indicating that monoiodoaromatic acid has the potential to be used in the preparation of 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] Coxsaekievirus (CV) is a member of the Enterovirus genus of Picornaviridae, and its infection can cause a variety of diseases, such as hand, foot and mouth disease, aseptic meningitis, encephalitis, myocarditis , epidemic myositis, herpetic angina, etc. A total of 29 serotypes of CV have been reported. According to their pathogenic characteristics and cell susceptibility to suckling mice, they can be divided into two groups, A and B, namely CVA (CVA1-22, 24) and CVB ( CVB1-6). The infection of CVBs is the most common, among which CVB3 is the most pathogenic type among the six serotypes of CVB, and is the main pathogenic cause of viral myocarditis. According to the US Centers for Disease Control and Prevention (CDC) statistics, CVB (types 1-6) can cause about 5 milli...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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