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Application of doxycycline

A technology for doxycycline and pulmonary fibrosis, which is applied to the active ingredients of tetracycline, respiratory diseases, drug combinations, etc., can solve the problem of low activity of pulmonary fibrosis, achieve the inhibition of pulmonary fibrosis, wide sources, easy to accept Effect

Inactive Publication Date: 2015-04-01
NANKAI UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the defects of low pulmonary fibrosis inhibitory activity of the medicine for treating pulmonary fibrosis in the prior art, the object of the present invention is to provide a kind of application of doxycycline in the preparation of medicine for treating pulmonary fibrosis

Method used

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  • Application of doxycycline
  • Application of doxycycline
  • Application of doxycycline

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The establishment of embodiment 1 mouse pulmonary fibrosis model Doxycycline pharmacodynamics detection

[0053] 1. Establishment of mouse pulmonary fibrosis model and drug treatment

[0054] 1.1 Establishment of mouse pulmonary fibrosis model

[0055] The 36 mice were randomly divided into three groups: normal group, control group and doxycycline group, 12 in each group. Each rat in the normal group was given 0.15 mL of 0.9% normal saline at one time; each rat in the control group and doxycycline group was given 0.15 mL of methyl viologen hydrate aqueous solution at one time.

[0056] 1.2 Administration and treatment of mice with pulmonary fibrosis

[0057] In the third week after modeling, the mice were given drug treatment. The normal group and the control group were fed with 0.9% normal saline of 0.1 mL each time, and the doxycycline group was fed with 0.1 mL of doxycycline aqueous solution each time. Stomach. Once every 2 days.

[0058] 1.3 Pathological detect...

Embodiment 2

[0067] Example 2 Effect of doxycycline on proliferation of mouse fibroblast NIH-3T3

[0068] Inhibitory effect of doxycycline on the growth of mouse fibroblast NIH-3T3 detected by MTT assay

[0069] The experimental method is MTT colorimetric method: the detection principle is that succinate dehydrogenase in the mitochondria of living cells can reduce exogenous MTT to water-insoluble blue-purple crystalline formazan (Formazan) and deposit in the cells, while dead cells have no this function. Dimethyl sulfoxide (DMSO) can dissolve formazan in cells, and its light absorption value is measured at a wavelength of 490nm by an enzyme-linked immunosorbent detector, which can indirectly reflect the number of living cells. Within a certain cell number range, the amount of formazan crystal formation is proportional to the cell number. This method has been widely used in the activity detection of some biologically active factors, large-scale antitumor drug screening, cytotoxicity test ...

Embodiment 3

[0083] Example 3 Effect of doxycycline on migration of NIH-3T3 cells

[0084] 1. Experimental method:

[0085] After trypsinization, the cells were dispersed into single cells and suspended in the corresponding medium. Cells were seeded on 96-well culture plates, 4000 cells / well. Place in a 37°C carbon dioxide (5%) incubator for overnight culture to allow the cells to adhere to the wall. The next day, the medium was discarded and a medium containing a series of concentrations of the test substance (doxycycline) was added. The next day, discard the culture medium, wash the cells twice with PBS, add Hochest 33342 (dissolved in pH 7.4 phosphate buffer, the final concentration is 5 μg / mL) staining solution 50 μL / well, 37 ° C carbon dioxide (5%) Incubate in the incubator for 20min. Aspirate and discard the staining solution, wash twice with PBS, and add culture solution containing a certain concentration of the drug to be tested. Then put it on the high-content analysis platfo...

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Abstract

The invention provides an application of doxycycline in the preparation of a medicine for treating pulmonary fibrosis. Experimental data show that IC50 of mouse fibroblast cells NIH-3T3 by doxycycline is 11.84 microns. With increased concentration of doxycycline, the inhibiting effect on growth of mouse fibroblast cells NIH-3T3 is enhanced gradually. In addition, doxycycline can inhibit pulmonary fibroblast cell migration, inhibit excess deposition of a pulmonary extracellular matrix, reverse and inhibit pulmonary fibrosis level of an organism, improve pulmonary blood-supply, increase pulmonary blood-supply quantity and alleviate dyspnea, and has a good effect of treating pulmonary fibrosis.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the application of doxycycline. Background technique [0002] Doxycycline "Doxycycline" (also known as doxycycline), belonging to the tetracycline class of antibiotics, is a well-known and widely used antibiotic. Tetracyclines mainly act on the 30S subunit of bacterial nucleosomes, interfere with the binding of amino acid tRNA to the action site on the 30S subunit, block the binding of aminoacyl tRNA to the ribosome-mRNA complex, inhibit protein synthesis, and also change The permeability of the cell membrane exposes important substances such as nucleotides in the cell, inhibits DNA synthesis, and thus achieves the antibacterial effect. Doxycycline is a type with stronger drug efficacy and wider application among tetracyclines (Adimora AA., 2002; Kovacova E, et al., 2002). About doxycycline is currently mainly used clinically for the treatment of upper respiratory tract infec...

Claims

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Application Information

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IPC IPC(8): A61K31/65A61P11/00
CPCA61K31/65
Inventor 周红刚杨诚孙涛刘慧娟刘艳荣王静张成玉张强张向明秦源张鹏
Owner NANKAI UNIV
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