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Application of labetalol in preparation of medicine for preventing and treating fibrotic diseases

A technology for fibrotic diseases and fibrosis, applied in the field of medicine, can solve problems such as lack of organ donors, uncertainty of curative effect, and low surgical survival rate

Inactive Publication Date: 2019-03-26
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The clinical treatment plan for fibrotic diseases is mainly based on the synergistic effect of immune response and inflammatory response in the process of fibrosis. Anti-inflammatory and immunosuppressive drugs are used in combination to delay the process of fibrosis. Due to the uncertainty of curative effect and adverse reactions Many but not widely used
Although organ transplantation is the only effective treatment for end-stage fibrosis, it also faces problems such as lack of organ donors, low surgical survival rate, and difficulty in postoperative recovery.
It can be seen that the discovery of anti-fibrotic drugs with strong specificity, definite curative effect and no obvious adverse reactions is of great significance, but there is still a lack of safe and effective anti-fibrotic drugs in clinical practice.

Method used

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  • Application of labetalol in preparation of medicine for preventing and treating fibrotic diseases
  • Application of labetalol in preparation of medicine for preventing and treating fibrotic diseases
  • Application of labetalol in preparation of medicine for preventing and treating fibrotic diseases

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Example 1. Research on the anti-pulmonary fibrosis, liver fibrosis, kidney fibrosis and cardiac fibrosis of labetalol based on the fibrosis marker protein α-SMA in vitro.

[0031] Lung epithelial cells A549 cells, hepatic stellate cells LX2, renal tubular epithelial cells CD3, and primary cardiac fibroblasts were pre-treated with 30 μM labetalol or vehicle, and then stimulated by 10 ng / mL TGF-β1 to stimulate the above four cells to Myofibroblasts were transformed to construct lung, liver, kidney and heart fibrosis models in vitro, and the fibrosis marker protein α-SMA was used to characterize the degree of fibrosis. Such as figure 1 As shown, after 10ng / ml TGF-β1 stimulated human lung epithelial cells A549, hepatic stellate cells LX2, renal tubular epithelial cells CD3 and primary mouse cardiac fibroblasts for 48 hours, the fibrosis marker protein α-SMA was significantly up-regulated (P<0.01) proved the successful construction of classic lung, liver, kidney and heart f...

Embodiment 2

[0032] Example 2. Cell hardness as a marker of fibrosis To investigate the anti-pulmonary fibrosis, liver fibrosis, kidney fibrosis and cardiac fibrosis effects of labetalol in vitro.

[0033] Our previous results demonstrated that cell stiffness can be used as a biomarker to characterize the degree of fibrosis. Lung epithelial cells A549 cells, hepatic stellate cells LX2, renal tubular epithelial cells CD3, and primary cardiac fibroblasts were pre-treated with 30 μM labetalol or vehicle, and then stimulated by 10 ng / mL TGF-β1 to stimulate the above four cells to Transformation of myofibroblasts to construct fibrosis models of lung, liver, kidney and heart in vitro. Atomic force microscopy was used to detect the changes in the stiffness of the above four cells after being stimulated by TGF-β1, and the cell stiffness (Young's modulus) was used as a marker to characterize degree of fibrosis. the result shows( figure 2 ), in the above lung fibrosis, liver fibrosis, kidney fibr...

Embodiment 3

[0034] Example 3. Research on the anti-fibrosis effect of labetalol in vivo.

[0035] 1. Model preparation and administration:

[0036]Select adult male C57 mice with a body weight of 20-24 g, respectively set up a blank control group (normal saline), a model group, and a test drug group (labetalol, 10 mg / kg, intraperitoneal injection), and each group has 10 only animals. Bleomycin was administered at 3 mg / kg via tracheal perfusion to prepare a mouse model of pulmonary fibrosis; different test drugs were given on the 7th day after the bleomycin model was established, once a day for 21 consecutive days.

[0037] 2. Pathological tissue sampling:

[0038] On the 28th day after administration, the mouse was anesthetized by intraperitoneal injection of 0.1ml / 10g chloral hydrate, the chest cavity was opened, the left atrium was cut open, and pre-cooled normal saline was slowly injected into the heart from the right ventricle, and perfused through the pulmonary circulation until th...

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Abstract

The invention belongs to the technical field of medicine, and relates to application of labetalol in the preparation of a medicine for preventing and treating fibrotic diseases. The labetalol is labetalol or a pharmaceutical derivative thereof. The fibrotic diseases include pulmonary fibrosis, hepatic fibrosis, renal fibrosis, cardiac fibrosis, endometrial fibrosis, ocular fibrosis, pancreatic fibrosis, splenic fibroplasia diseases, myelofibrosis diseases, or fibrosis-induced diseases. The labetalol can be combined with one or a plurality of pharmaceutical carriers to form a pharmaceutical composition. The labetalol or the pharmaceutical composition thereof can be used alone or combined with other drugs. Moreover, the labetalol has the advantages of remarkable curative effect, fewer toxicor side effects and safe use in the aspect of treating the fibrotic diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to the use of labetalol in the preparation of medicines for preventing and treating fibrotic diseases. Background technique [0002] Fibrosis refers to the pathological process in which inflammation leads to necrosis of organ parenchymal cells and abnormal increase and excessive deposition of extracellular matrix in tissues. Essentially, fibrosis is a repair response to tissue damage to protect the relative integrity of tissues and organs. Although the proliferating fibrous connective tissue repairs the defect, it does not have the structure and function of the original organ parenchymal cells. If this repair response is excessive, strong, and out of control, it will cause organ fibrosis and lead to a decline in organ function. [0003] Fibrosis can occur in many organs, including vital organs such as the lungs, liver, kidneys, and heart. The main pathological changes are the forma...

Claims

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Application Information

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IPC IPC(8): A61K31/609A61P11/00A61P1/16A61P13/12A61P9/00A61P15/00A61P1/18A61P19/08A61P17/00
CPCA61K31/609A61P1/16A61P1/18A61P9/00A61P11/00A61P13/12A61P15/00A61P17/00A61P19/08
Inventor 马恩龙李艳春刘禹彤马超王健
Owner SHENYANG PHARMA UNIVERSITY
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