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Application of macrolide antibiotics or medicinal salts thereof in preparation of anti-hand, foot and mouth disease medicaments

A technology for macrolides and hand, foot and mouth disease, which is applied in the direction of antiviral agents, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve the problem of ineffective treatment of severe hand, foot and mouth disease and the absence of macrolides Reports on the activity of antibiotics against other viruses

Active Publication Date: 2018-08-28
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although topical tetracyclines can reduce the spread of the virus, they cannot effectively treat severe hand, foot and mouth disease
[0006] According to the literature search, except for the viruses that infect the respiratory tract, there is no report that macrolide antibiotics have anti-virus activity.

Method used

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  • Application of macrolide antibiotics or medicinal salts thereof in preparation of anti-hand, foot and mouth disease medicaments
  • Application of macrolide antibiotics or medicinal salts thereof in preparation of anti-hand, foot and mouth disease medicaments
  • Application of macrolide antibiotics or medicinal salts thereof in preparation of anti-hand, foot and mouth disease medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] EV71-MZ201405 and CVA16-MZ201509 were respectively infected into Vero or RD cells. At different drug concentrations, the inventors analyzed the expression of the reporter gene GFP carried by the virus genome by flow cytometry, and observed the cytopathic effect (CPE) caused by virus infection, And plaque analysis of progeny virus production, evaluated whether the above six macrolide antibiotics have inhibitory effects on the replication of viruses EV71 and CAV16, and whether they have protective effects on host cells.

[0031] 1.1 Cytotoxic effect of drugs: 293A-SCARB, RD and Vero cells were mixed with 1x10 4 / Each well was inoculated in 96 wells in 5% CO 2 , Cultured overnight at 37°C, treated cells with a series of doubly diluted macrolides for 48 hours, and tested the toxicity of the drugs to the cells by MTT method; cells cultured under the same conditions without drug treatment were used as controls ; Each group of cells had three replicate wells, and the growth i...

Embodiment 2

[0044] Enterovirus is a single-stranded positive-sense RNA virus with a genome length of about 7408nt, containing an open reading frame encoding a polyprotein, flanked by 5' and 3' non-translated regions (untranslated region, UTR). Viral structural and non-structural proteins are produced after polyproteolysis; 5'UTR contains RNA replication signal and polypeptide translation initiation signal IRES, which plays an important role in the synthesis and translation of viral genomic RNA by binding to host protein factors . Taking spiramycin against EV71 as an example, the present invention analyzes the possible action mechanism of macrolide antibiotics inhibiting enterovirus replication at the cell level by means of biochemical and molecular biology research.

[0045] 2.1 Detect the effect of drug addition time on the antiviral activity of the drug, and provide clues for the analysis of the link in which spiramycin blocks EV71 infection: combine 5x10 4 1 RD cells were inoculated i...

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PUM

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Abstract

The invention discloses application of macrolide antibiotics or medical salt thereof to preparation of medicine for resisting to hand-foot-and-mouth disease. It is proved by experiments that the macrolide antibiotics provided with a 14-elemnt macrocyclic lactones mother nucleus, a 15-element macrocyclic lactones mother nucleus and a 16-element macrocyclic lactones mother nucleus has activity of resisting to EV71 virus and CVA16 virus and has potential application value of being developed into medicine or a lead compound for treating hand-foot-and-mouth disease.

Description

technical field [0001] The invention belongs to the field of new application of medicine. More specifically, it relates to a new application of a series of macrolide antibiotics or their pharmaceutically acceptable salts in the preparation of anti-hand, foot and mouth disease drugs. Background technique [0002] Hand-foot-and-mouth disease (HFMD) is an acute infectious disease caused by enterovirus, mainly in children under 5 years old. The main clinical symptoms of HFMD are maculopapules and herpes on the hands, feet, mouth and other parts. Severe neurological diseases and even death may occur in severe patients. There are more than 20 enteroviruses (types) that cause HFMD, among which coxsackievirus A16 (CVA16) and enterovirus 71 (EV71) are the most common, and other different types of enteroviruses and coxsackieviruses are also Can cause disease. EV71 and CAV16 are highly contagious, and the infection is distributed globally, especially in the Asia-Pacific region. The ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K31/7052A61P31/14
CPCA61K31/7048A61K31/7052
Inventor 郭学敏曾施暖孟小斌黄清苑雷南风曾令斌
Owner SUN YAT SEN UNIV
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