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Application of a prazole compound in preparation of drugs for prevention and treatment of fibrotic diseases

A technology for azole compounds and fibrotic diseases, which is applied in the field of preparation of sulfoxide compounds or their derivatives, and can solve problems such as research reports on the preventive and therapeutic effects of pantoprazole on fibrotic diseases.

Active Publication Date: 2019-10-18
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no research report on the prevention and treatment of fibrosis diseases by pantoprazole and other prazole proton pump inhibitors

Method used

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  • Application of a prazole compound in preparation of drugs for prevention and treatment of fibrotic diseases
  • Application of a prazole compound in preparation of drugs for prevention and treatment of fibrotic diseases
  • Application of a prazole compound in preparation of drugs for prevention and treatment of fibrotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1. Cell hardness as a marker of fibrosis. The anti-pulmonary fibrosis, liver fibrosis, kidney fibrosis and cardiac fibrosis effects of the prazole compounds were investigated in vitro.

[0037] 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 LX-2, renal tubular epithelial cells CD3, and primary cardiac fibroblasts were pre-treated with 100 μM pantoprazole, lansoprazole, omeprazole, ilaprazole, ethanol Treated with someprazole, rabeprazole or vehicle, and then stimulated the above four kinds of cells to transform into myofibroblasts by 10ng / mL TGF-β1 to construct in vitro lung, liver, kidney and heart fibrosis models, detected by atomic force microscope The change of the cell stiffness of the above four kinds of cells after being stimulated by TGF-β1, and the degree of fibrosis was characterized by the cell stiffness (Young's modulus) ...

Embodiment 2

[0038] Example 2. Research on the in vitro anti-pulmonary fibrosis, liver fibrosis, kidney fibrosis and cardiac fibrosis of pantoprazole based on the fibrosis marker protein α-SMA.

[0039] Lung epithelial cells A549 cells, hepatic stellate cells LX-2, renal tubular epithelial cells CD3, and primary cardiac fibroblasts were pre-treated with 100 μM pantoprazole or vehicle, and then stimulated by 10 ng / mL TGF-β1. The cells were transformed into myofibroblasts to construct in vitro models of lung, liver, kidney and heart fibrosis, 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 LX-2, renal tubular epithelial cells CD3 and primary mouse cardiac fibroblasts for 48h, the fibrosis marker protein α-SMA Significantly up-regulated (P<0.01=demonstrates successful construction of classic lung, liver, kidney and heart fibrosis models). ...

Embodiment 3

[0040] Embodiment 3, research on anti-fibrosis effect of pantoprazole in vivo.

[0041] 1. Model preparation and administration:

[0042] Pulmonary fibrosis: select adult male C57 mice with a body weight of 20-24g, respectively set up a blank control group (normal saline), a model group, and a test drug group (pantoprazole, 50mg / kg, administered by intraperitoneal injection) , 10 animals per group. 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.

[0043] Hepatic fibrosis: select adult male C57 mice with body weight between 20-24g, set up blank control group (olive oil), model group, test drug group (pantoprazole, 50mg / kg, intraperitoneal injection) , 10 animals per group. 10% carbon tetrachloride (dissolved in olive oil) was administered by intraperitoneal injection at 5 mg / kg to prepare a ...

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Abstract

The invention belongs to the technical field of medicine, and relates to application of a prazole compound in preparation of drugs for prevention and treatment of fibrotic diseases. The pantozol compound is pantoprazole, lansoprazole, omeprazole, eprazole, esomeprazole, rabeprazole and other benzimidazole and pyridine substituted sulfoxide compounds or their derivatives. The fibrotic diseases include lung fibrosis, liver fibrosis, kidney fibrosis, heart fibrosis, endometrial fibrosis, eye fibrosis, pancreas fibrosis, spleen fibroplasia, bone marrow fibrosis, skin fibrosis or diseases induced by fibrosis. The prazole compound can be combined with one or more pharmaceutical carriers to form a pharmaceutical composition. The prazole compound or the pharmaceutical composition thereof can be used alone or in combination with other drugs. Moreover, the prazole compound has the advantages of having an obvious curative effect, few side effects and safe use in the treatment of the fibrotic diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the use of prazole compounds in the preparation of drugs for the prevention and treatment of fibrosis diseases, in particular to pantoprazole, lansoprazole, omeprazole, ilaprazole, and esomeprazole Use of sulfoxide compounds substituted with benzimidazole and pyridine, such as prazole and rabeprazole, or their derivatives in the preparation of medicines for preventing and treating different fibrotic diseases. Background technique [0002] Fibrosis is a pathological process in which the overexpression of cytokines induced by various etiologies leads to the activation and transformation of intrinsic function cells and mesenchymal cells, the accumulation of excess extracellular matrix, the destruction of tissue structure and the loss of function. Fibrosis can occur in many organs, including important organs such as the lung, liver, kidney, and heart. The main pathological changes are...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61P11/00A61P1/16A61P9/00A61P27/02A61P1/18A61P1/00A61P19/00A61P17/00A61P7/00
CPCA61K31/4439A61P11/00A61P1/16A61P9/00A61P27/02A61P1/18A61P1/00A61P19/00A61P17/00A61P7/00
Inventor 马恩龙王健李艳春刘禹彤田丽吴海瑞牛雪岩
Owner SHENYANG PHARMA UNIVERSITY
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