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Application of loratadine or ebastine in preparation of medicine for preventing and/or treating COVID-19 inflammation

A technology of COVID-19 and loratadine, which is applied in the field of biomedicine, can solve the problems of lack of immune regulation means and unclear cellular mechanism, and achieve the effect of reducing inflammatory factor response, preventing lung injury, and reducing inflammatory response

Inactive Publication Date: 2021-09-24
GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the cellular mechanism of SARS-CoV-2 virus-induced inflammatory cytokine storm in the body is unclear, and clinical immunotherapy for COVID-19 inflammation still lacks effective immune regulation means

Method used

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  • Application of loratadine or ebastine in preparation of medicine for preventing and/or treating COVID-19 inflammation
  • Application of loratadine or ebastine in preparation of medicine for preventing and/or treating COVID-19 inflammation
  • Application of loratadine or ebastine in preparation of medicine for preventing and/or treating COVID-19 inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091]This example is used to verify that loratadine or ibastine can inhibit LAD2 degranulation.

[0092] (1) Divide 5×10 5 LAD2 cells / well were inoculated in a 24-well cell culture plate, and ebastine (3 μg / mL) and loratadine (5 μg / mL) were added to incubate for 20 hours;

[0093] (2) Stimulate the cells with SARS-CoV-2 sipke-RBD (10 μg / mL) (that is, to obtain the experimental group Eba. pseudovirus and Lor.+pseudovirus), the cells were collected at 30 minutes and 2 hours, respectively;

[0094] (3) Cells were fixed with 4% paraformaldehyde (PFA) at room temperature for 30 minutes, washed 3 times with PBS, then incubated with anti-Avidin-FITC at 4°C in the dark for 1 hour, washed 3 times with PBS, and then flow cytometry was performed;

[0095] Income like figure 1 As shown, spike-RBD protein or spike-packaged lentivirus can induce mast cell degranulation, and after treatment with ibastine or loratadine, the level of degranulation of cells was significantly lower than spik...

Embodiment 2

[0097] This example is used to verify the inhibitory effect of loratadine and ibastine on the storm of inflammatory factors caused by SARS-CoV-2.

[0098] (1) Divide 5×10 5 LAD2 cells / well were inoculated in a 24-well cell culture plate, and ebastine (3 μg / mL) and loratadine (5 μg / mL) were added to incubate for 20 hours;

[0099] (2) After stimulating the cells with sipke-RBD (10 μg / mL) for 2 hours, the cell supernatant was collected for culturing A549 cells to obtain Eba.+RBD group and Lor.+RBD group;

[0100] (3) A549 cells were collected after 24 hours, and the expression of cytokines was determined by quantitative mRNA production and intracellular immunostaining with specific antibodies;

[0101] (4) At the mRNA level, Trizol lysed cells to extract RNA, reverse-transcribed it into cDNA using ReverTra qPCR RT Master Mix gDNA remover, and detected IL-6, IL-8, TNFα and Expression of IL-1β;

[0102] The primer sequences used are shown in SEQ ID NO.1-16;

[0103] Use ebasti...

Embodiment 3

[0109] In this example, the ACE2 humanized mouse model was used to verify the inhibitory effect of loratadine and ibastine on the inflammatory factor storm caused by SARS-CoV-2 and the protective effect on lung injury.

[0110] (1) The ACE2 humanized mouse model is C57BL / 6N-Ace2 em2(hACE2-WPRE,pgk-puro) / CCLA Mice, on the day before the mice were challenged, intraperitoneal injection of ebastine (5mg / kg) or loratadine (10mg / kg), the challenge dose was 5×10 6 TCID50;

[0111] (2) Inject the same dose of ebastine or loratadine every day thereafter until the fourth day;

[0112] (3) On the 5th day after infection, the lungs of the mice were anesthetized and euthanized for RNA extraction and histopathological staining (H&E, toluidine blue); IL-6, IL-8, TNFα were detected by qPCR , the expression of IL-1β, INFγ, CRP, CCL20 and CCL5, the primers and probe sequences used are shown in SEQ ID NO.17-37;

[0113] Lung pathological damage and mast cell degranulation were detected by H&E...

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Abstract

The invention provides an application of loratadine or ebastine in preparation of a medicine for preventing and / or treating COVID-19 inflammation. In-vivo and in-vitro experiments prove that the loratadine or the ebastine can reduce the inflammatory reaction caused by SARS-CoV-2spike protein by inhibiting mast cell degranulation and inhibit inflammatory factor storm, and has certain protection on tissue damage. Therefore, the combination of the loratadine or the ebastine and an antiviral drug has important clinical application value in the aspect of treating the severe infection of the COVID-19.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to the application of loratadine or ebastine in the preparation of drugs for preventing and / or treating COVID-19 inflammation. Background technique [0002] Loratadine (Loratadine, C 22 h 23 CIN 2 o 2 ), the systematic name is 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-enyl)-1-piper Ethyl pyridinecarboxylate, its structural formula is shown in formula I; Ebastine (Ebastine, C 32 h 39 NO 2 ), the system name is 1-(4-tert-butylphenyl)-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone, and its structural formula is shown in formula II . [0003] [0004] Loratadine and Ibastine belong to the second-generation antihistamine drugs, which are clinically used to treat allergic diseases, including allergic rhinitis in children, perennial rhinitis in adults, seasonal rhinitis, hay fever and chronic urticaria Wait. [0005] Novel coronavirus...

Claims

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Application Information

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IPC IPC(8): A61K31/4545A61K31/445A61K45/06A61P11/00A61P31/14
CPCA61K31/4545A61K31/445A61K45/06A61P11/00A61P31/14A61K2300/00
Inventor 王建华郑永唐吴梦丽刘丰亮李欣
Owner GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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