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Application of doxycycline

A doxycycline and inflammatory response technology, applied in the direction of tetracycline active ingredients, digestive system, drug combination, etc., can solve the problem of low liver fibrosis activity, and achieve the effect of improving liver function status, easy acceptance and easy acquisition

Active Publication Date: 2015-01-07
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Aiming at the defect that the anti-hepatic fibrosis activity of the medicine for treating liver fibrosis is low in the prior art, the object of the present invention is to provide a kind of application of doxycycline in the preparation of the medicine for treating liver 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

[0057] Example 1 Establishment of mouse liver fibrosis model Doxycycline pharmacodynamics detection

[0058] 1. Establishment of mouse liver fibrosis model and drug treatment

[0059] 1.1 Establishment of mouse liver fibrosis model

[0060] The 36 mice were randomly divided into three groups: normal group, model group (no administration, ie, control group), and doxycycline group, with 12 mice in each group. In the normal group, 0.15ml of normal saline was subcutaneously injected into the back of each mouse; in the model group (no drug administration group for modeling) and the doxycycline group (doxycycline administration group for modeling) were injected with 0.15 ml of normal saline in the back of each mouse. ml of 40% CCl 4 CCl 4 - Suspension in edible oil; injected twice a week.

[0061] 1.2 Drug treatment of mice with liver fibrosis

[0062] In the third week after modeling, the mice were given drug treatment. The normal group and the model group were intragastricall...

Embodiment 2

[0071] Example 2 Doxycycline Effects on Mouse Fibroblast NIH-3T3 in Vitro

[0072] 1) MTT method to detect the inhibitory effect of doxycycline on the growth of mouse fibroblast NIH-3T3

[0073] 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 and ...

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Abstract

The invention provides an application of doxycycline in preparing a medicament for treating liver fibrosis. Shown by pharmacodynamics experimental data of a cell level, IC 50 of the doxycycline to mouse fibroblast cells NIH-3T3 is 11.84 microns; along with increase of concentration of the doxycycline, the inhibition action to growth of the mouse fibroblast cells NIH-3T3 is gradually strengthened, and proliferation of fibroblast cells in a liver can be well inhibited. Shown by pharmacodynamics experiments of an animal level, the doxycycline is capable of reversing and inhibiting liver fibrosis level of a body, inhibiting excess hyperplasia of the fibroblast cells in the liver, improving blood supply of the liver, promoting regeneration of liver cells and inhibiting inflammatory response of the liver and has good therapeutic effect on liver 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" (alias deoxyoxytetracycline, also known as doxycycline), belongs to the tetracycline antibiotics, is well known and widely used antibiotics. 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 intracellular substances such as nucleotides, inhibits DNA synthesis, and thus achieves antibacterial effects. Doxycycline is a type of tetracyclines with strong efficacy and wide application (Adimora AA., 2002; Kovacova E, et al., 2002). Doxycycline is mainly used clinically to treat upper respiratory tract infection, tonsillitis, bilia...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/65A61P1/16
CPCA61K31/65
Inventor 周红刚杨诚孙涛刘艳荣刘慧娟孙波张成玉张强王静李珊李咪
Owner NANKAI UNIV
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