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Application of Ruboxistaurin in preparation of medicine for preventing and treating pulmonary fibrosis and hepatic cirrhosis and medicinal preparation thereof

A pulmonary fibrosis and drug technology, applied in drug combination, digestive system, medical formula, etc., can solve problems such as unsatisfactory curative effect

Inactive Publication Date: 2018-04-06
吴殿青 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are also glucocorticoids, pirfenidone, colchicine, cyclosporine, interferon (IFN)-γ1b, bosentan, etanercept and other drugs for monotherapy, but the curative effect is generally unsatisfactory

Method used

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  • Application of Ruboxistaurin in preparation of medicine for preventing and treating pulmonary fibrosis and hepatic cirrhosis and medicinal preparation thereof
  • Application of Ruboxistaurin in preparation of medicine for preventing and treating pulmonary fibrosis and hepatic cirrhosis and medicinal preparation thereof
  • Application of Ruboxistaurin in preparation of medicine for preventing and treating pulmonary fibrosis and hepatic cirrhosis and medicinal preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Ruboxistaurin inhibits the migration of mouse fibroblasts (in vitro fibrosis markers) experiment

[0020] In the Transwell cell migration assay, mouse fibroblasts were starved overnight in serum-free culture, and then the cells were resuspended in DMEM medium containing 0.1% fetal bovine serum, and seeded into the upper chamber of the Transwell of a 24-well plate, and inoculated in each well 5×104 cells. Add 0.1% fetal bovine serum to the DMEM medium in the lower chamber and figure 1 Indicates the inclusion or absence of lysophosphatidic acid (LPA, lysophosphatidic acid) or Ruboxistaurin (Rbx). There are 4 cell treatment methods (from left to right in the upper picture): the first one, adding DMEM medium containing 0.1% fetal bovine serum to the lower chamber of Transwell; the second method, adding 0.1% fetal bovine serum to the lower chamber of Transwell and DMEM medium of 5 μM LPA; the third type, the DMEM medium containing 0.1% fetal bovine serum, 5 μM L...

Embodiment 2

[0022] Example 2: Ruboxistaurin inhibits migration of human fibroblast cell line (LL29) derived from patients with idiopathic pulmonary fibrosis (IPF)

[0023] In the Transwell cell migration assay, LL29 cells were starved overnight in serum-free culture, and then the cells were resuspended in DMEM medium containing 0.1% fetal calf serum, and seeded into the upper chamber of the Transwell of a 24-well plate, with 5×10 cells per well. 4 cell. In the lower chamber, DMEM medium with 0.1% fetal bovine serum was added with or without LPA, PP242 (an mTOR inhibitor) or Ruboxistaurin (Rbx) as shown in the upper figure. 6 cell processing methods ( Figure 4 From left to right) are: the first one, DMEM medium containing 0.1% fetal bovine serum was added to the lower chamber of Transwell; the second one was cultured in DMEM containing 0.1% fetal bovine serum and 2 μM LPA in the lower chamber of Transwell base; the third type, the DMEM medium containing 0.1% fetal bovine serum and 0.5 μ...

Embodiment 3

[0025] Example 3: Delayed induction of the role of Ruboxistaurin in the formation of pulmonary fibrosis in the model of pulmonary fibrosis in mice

[0026] (1) The reagents used in the experiment were prepared as follows:

[0027] Preparation of Ruboxistaurin solution and blank control:

[0028] 1. Prepare a 0.8% water-soluble hydroxyethylcellulose 250HHX solution (Natrosol, 250HHX) with purified water;

[0029] 2. Add Tween80 to the above polymer solution, the final concentration of Tween80 is 0.5%;

[0030] 3. Add a solid sample of Ruboxistaurin to the above polymer solution at a concentration of 0.5 mg / ml, and stir evenly.

[0031] The above solution is prepared before use and should be used within one hour.

[0032] (2) The experiment operates as follows:

[0033] 1. 10-week-old C57BL / 6 mice were instilled with 50 μl of bleomycin by nasal feeding every day at a dose of 2.5 mg / kg to induce pulmonary fibrosis.

[0034] 2. After 7 days of instillation, the mice were divi...

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Abstract

The invention discloses an application of Ruboxistaurin in preparation of a medicine for preventing and treating pulmonary fibrosis and hepatic cirrhosis and a medicinal preparation thereof. The invention provides the application of Ruboxistaurin in preparation of the medicine shown in a formula I for preventing and treating pulmonary fibrosis and hepatic cirrhosis. The invention also provides themedicine for preventing and treating pulmonary fibrosis and hepatic cirrhosis, Ruboxistaurin is taken as an active component and is individually prepared, or one or a plurality of pharmaceutical adjuvants can be added, and the medicine is obtained; and a dosage form is preferably oral preparations, spray preparation or injection preparations. The invention provides an effective method for preventing and treating pulmonary fibrosis and hepatic cirrhosis application of Ruboxistaurin.

Description

technical field [0001] The invention belongs to the field of organic synthesis and chemical medicine, and specifically relates to the application of rubesta in the preparation of medicines for preventing and treating pulmonary fibrosis and liver cirrhosis and its pharmaceutical preparations. Background technique [0002] Pulmonary fibrosis (PF) is characterized by the proliferation of fibroblasts (FB) and the accumulation of a large amount of extracellular matrix (ECM), and is organized by diffuse alveolitis, pulmonary interstitial inflammation and interstitial fibrosis. A group of disease groups with medical characteristics, covering a variety of diseases. Pulmonary fibrosis is a progressive fatal disease, the incidence rate is increasing year by year, the mortality rate is quite high, and the average survival time is 2-2.5 years; most diseases currently lack effective treatment methods, and the prognosis is extremely poor. There are many factors that cause pulmonary fibro...

Claims

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Application Information

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IPC IPC(8): A61K31/407A61P11/00A61P1/16
CPCA61K31/407
Inventor 吴殿青李小锋邓冠华
Owner 吴殿青
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