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Application of lapatinib and/or medicinal derivatives thereof in preparation of anti-enterovirus drugs

A technology of lapatinib and enterovirus, applied in the field of application of lapatinib and/or its pharmaceutically acceptable derivatives in the preparation of anti-enterovirus drugs, can solve the problem of limited treatment methods, large individual differences, Difficult to promote and other issues, to achieve strong anti-virus, simple synthesis process, and enhance the effect of cell survival

Active Publication Date: 2021-12-24
武汉市金银潭医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment methods for EV71 virus infection are also quite limited. The main treatment methods are symptomatic supportive treatment and broad-spectrum antiviral therapy. The curative effect is limited, individual differences are large, and it is difficult to promote

Method used

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  • Application of lapatinib and/or medicinal derivatives thereof in preparation of anti-enterovirus drugs
  • Application of lapatinib and/or medicinal derivatives thereof in preparation of anti-enterovirus drugs
  • Application of lapatinib and/or medicinal derivatives thereof in preparation of anti-enterovirus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1, the cytotoxicity detection of lapatinib

[0043] Cytotoxicity of lapatinib was tested in RD cells. RD cells were seeded in 96-well plates at 37 °C, 5% CO 2 After culturing in the incubator for 12-16 hours, the cell culture medium was discarded, and the cell maintenance medium containing different concentrations of tested lapatinib was added to continue the culture, with 3 replicate wells in each group, and the same amount of PBS was added to the control group. After 48 hours of treatment, stain with MTT and detect OD 492 nm, analysis of cell viability.

[0044] Result analysis: The test results are as follows: figure 1 As shown, the Prism7 software calculates the median toxic concentration (Median cyctoxic concentration, CC 50 ), CC of lapatinib 50 is 41368nM. In subsequent examples, the maximum concentration of lapatinib used is 20000 nM, which is within the safe and non-toxic range.

Embodiment 2

[0045] Example 2, lapatinib inhibits the cytopathic effect of EV71 virus replication

[0046] Plate RD cells on 96-well cell culture plates at 37 °C, 5% CO 2 After culturing in the incubator for 12-16h, 100TCID 50 The cells were infected with the EV71 virus solution for 2 hours, and the cell maintenance solution containing different concentrations of lapatinib was added to continue culturing for about 48 hours, and the same volume of PBS was added to the negative control. When about 90% of the CPE lesions appeared in the virus control wells, the cytopathic effect (CPE) was observed under a microscope.

[0047] Result analysis: The test results are as follows: figure 2 As shown, lapatinib inhibited the CPE effect of RD cells induced by EV71 in a concentration-dependent manner. EV71-infected RD cells became round and detached from the cell wall. Treatment with different concentrations of experimental compounds had a significant inhibitory effect on the lesion effect, effectiv...

Embodiment 3

[0048] Example 3, detection of lapatinib inhibiting EV71 antiviral activity

[0049] RD cells were seeded in 24-well cell culture plates at 37°C, 5% CO 2 Cultivate in the incubator for 12-16h, use 100TCID 50 After 2 hours of infection with the EV71 virus liquid, the cell maintenance solution containing different concentrations of experimental lapatinib was used for treatment, and the negative control was added with the same volume of PBS. After 24 hours of treatment, the effect of inhibiting virus proliferation was detected by real-time fluorescent quantitative PCR.

[0050] Result analysis: The test results are as follows: image 3 As shown, under different concentration conditions, the compound lapatinib has a significant inhibitory effect on the replication of EV71. Lapatinib is used as an anti-EV71 virus drug, and when the concentration of lapatinib is 20 μM, the inhibition rate to EV71 virus is 93.9%.

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Abstract

The invention provides application of lapatinib and / or medicinal derivatives thereof in preparation of anti-enterovirus drugs. According to the application, it is proved that the lapatinib has relatively high antiviral activity on enteroviruses such as EV71 and coxsackie virus and can be used for remarkably inhibiting a cytopathic effect (CPE) generated by the enteroviruses on host cells RD, and the cell survival rate is enhanced; and the nortriptyline hydrochloride can be used for inhibiting replication of the enteroviruses, showing a relatively high antiviral effect at a cellular level, and has an obvious technical effect. Results of the invention show that the compound lapatinib has potentials to prepare specific therapeutic drugs for resisting enterovirus infection, and has relatively good clinical application prospects.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to the application of lapatinib and / or its pharmaceutically acceptable derivatives in the preparation of anti-enterovirus drugs. Background technique [0002] Enterovirus 71 (Enterovirus, EV71) is a member of the Enterovirus genus of the Picornaviridae family. It is a non-enveloped virus. Positive RNA strand, about 7.5kb in length, is one of the most important pathogens causing hand, foot and mouth disease in infants and young children. Children with HFMD are sometimes accompanied by severe central nervous system complications, including aseptic meningitis, encephalitis, poliomyelitis-like paralysis, neurogenic cardiopulmonary failure, etc., and even death. Human is the only natural host of enterovirus, and the virus spreads through close contact between people (through fingers, utensils and food). Infected people have virus in their throat and intestines, and the virus can be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61P31/14
CPCA61K31/517A61P31/14Y02A50/30
Inventor 杨庆雨张定宇黄朝林
Owner 武汉市金银潭医院
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