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Application of dihydromyricetin in preparation of medicine for inhibiting new coronavirus or pulmonary fibrosis

A technology of dihydromyricetin and fibrosis, applied in the field of medicine, can solve the problems of high treatment costs, unmet clinical needs, and inability to effectively improve the survival of patients, and achieve the effect of inhibiting lung inflammation

Pending Publication Date: 2021-08-13
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are only two drugs on the market for this disease, namely Roche’s pirfenidone and Boehringer Ingelheim’s nintedanib, but neither can effectively improve the survival of patients, the treatment cost is high, and the clinical needs are far from being met
However, there is no report that dihydromyricetin can inhibit the new coronavirus or slow down pulmonary fibrosis

Method used

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  • Application of dihydromyricetin in preparation of medicine for inhibiting new coronavirus or pulmonary fibrosis
  • Application of dihydromyricetin in preparation of medicine for inhibiting new coronavirus or pulmonary fibrosis
  • Application of dihydromyricetin in preparation of medicine for inhibiting new coronavirus or pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] 1.1 Perform M on 71 drugs or compounds pro Proteasome in vitro enzyme activity inhibition assay

[0061] 1.1.1 Experimental method

[0062] Evaluation of 71 Compounds Against SARS-CoV-2M Using Fluorescence Resonance Energy Transfer pro Inhibition of protease activity: selection of 26 traditional Chinese medicine monomers and 25 M predicted by computer-aided drug design pro Inhibitors and 20 reported new crown-related marketed drugs pro In vitro enzyme activity screening, the concentration of the drug stock solution was 10mM.

[0063] 1.1.2 Experimental process

[0064] The volume of the enzymatic reaction system is 100 μL. m pro The final concentration of protease was 0.3 μM, and the final concentration of drug was 50 μM. The buffer solution of the reaction system includes 50 mM Tris, 150 mM NaCl, 1 mM EDTA, pH7.3, and the final concentration of the reaction substrate is 20 μM.

[0065] Blank control wells consisted of 93 μL of reaction buffer, 5 μL of DDMSO and...

Embodiment 2

[0081] 2.1 Dihydromyricetin inhibits bleomycin-induced lung inflammation

[0082] 2.1.1 Model establishment and administration

[0083] Select C57BL / 6J mice aged 6-8 weeks and weighing between 22-24g, and divide the mice into groups according to experimental requirements on Day 0. Weigh and record the body weight of the mouse and fix it on the operating table. The neck is disinfected with 70% alcohol, and a 1 cm long opening is vertically cut in the neck of the mouse with a scalpel, and the tissue is separated with surgical forceps to expose the trachea. Pierce the trachea through the space of the tracheal cartilage ring toward the end of the heart, slowly inject bleomycin in a volume appropriate to its body weight at a dose of 2 U / kg in the operation group, immediately turn the animal upright and turn it left and right, so that the liquid medicine is evenly distributed in the lungs; The mice in the sham operation group were injected with the same amount of normal saline for ...

Embodiment 3

[0094] 3.1 Dihydromyricetin inhibits bleomycin-induced pulmonary fibrosis in mice

[0095] 3.1.1 Model establishment and administration

[0096] Select C57BL / 6J mice aged 6-8 weeks and weighing between 20-22 g, and group the mice according to experimental requirements. Weigh and record the body weight of the mouse and fix it on the operating table. The neck is disinfected with 70% alcohol, and a 1 cm long opening is vertically cut in the neck of the mouse with a scalpel, and the tissue is separated with surgical forceps to expose the trachea. Pierce the trachea through the space of the tracheal cartilage ring toward the end of the heart, slowly inject bleomycin in a volume appropriate to its body weight at a dose of 2 U / kg in the operation group, immediately turn the animal upright and turn it left and right, so that the liquid medicine is evenly distributed in the lungs; The mice in the sham operation group were injected with the same amount of normal saline for injection in...

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PUM

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Abstract

The invention provides an application of dihydromyricetin in preparation of a medicine for inhibiting new coronavirus or pulmonary fibrosis, the dihydromyricetin has an inhibiting effect on the new coronavirus, can be combined with SARS-CoV-2Mpro and inhibit the in-vitro enzymatic activity of the SARS-CoV-2Mpro, and the IC50 value of the dihydromyricetin on the main protease Mpro of the new coronal virus is 1.716 + / -0.419 [mu]M, and the treating effect is remarkable.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of dihydromyricetin in the preparation of drugs for inhibiting new coronavirus or pulmonary fibrosis. Background technique [0002] The International Committee on Taxonomy of Viruses named the new coronavirus as SARS-CoV-2, and it has spread rapidly to 213 countries around the world. So far, a total of 144,617,554 cases have been diagnosed worldwide, with a total of 3,067,367 deaths. Since the emergence of new coronary pneumonia, the US FDA has approved the clinical trials of a variety of drugs, such as Remdesivir, Favipiravir and Arbidol. The results of the trial showed that the clinical efficacy of these drugs was not significant. There is still a lack of and an urgent need to develop effective drugs for the treatment of COVID-19. [0003] The SARS-CoV-2 genome consists of approximately 30,000 nucleotides, and its replicase gene encodes two overla...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K36/87A61P31/14A61P11/00
CPCA61K31/352A61K36/87A61P31/14A61P11/00
Inventor 杨诚周红刚肖婷李霄鹤崔梦奇魏玉丽
Owner NANKAI UNIV
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