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Use of aminopropionitrile in preparation of medicine

An aminopropionitrile, a technology for preparing drugs, applied in the field of biomedicine, can solve the problems of lack of treatment plans for patients with liver fibrosis and cirrhosis, difficulty in predicting the disease process of patients, unapproved and other problems, and achieves improvement in liver cirrhosis, easy absorption, and good quality. water soluble effect

Inactive Publication Date: 2017-03-15
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment of liver fibrosis and cirrhosis also faces many challenges, such as the lack of markers to characterize the process of fibrosis, the staging of the disease severity of patients with fibrosis, the difficulty in predicting the course of the patient's disease, and the lack of accurate diagnosis of liver fibrosis and cirrhosis. effective treatment options for patients
[0003] With the development of modern biology and medicine, the pathogenesis of liver fibrosis and the changes of molecular signals are becoming clearer, and more and more evidences show that liver fibrosis may be reversible, which also promotes the research and development of liver fibrosis drugs. Confidence, but at present, in addition to removing the underlying pathogenic factors (such as hepatitis B, hepatitis C virus, etc.), there is no effective treatment for liver fibrosis
So far, FDA has not approved drugs and treatments for liver fibrosis and cirrhosis.

Method used

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  • Use of aminopropionitrile in preparation of medicine
  • Use of aminopropionitrile in preparation of medicine
  • Use of aminopropionitrile in preparation of medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] In this embodiment, 10 healthy experimental mice were induced with chronic liver injury for 10 weeks to obtain experimental mice with severe fibrosis in the liver. Specifically, in this embodiment, each intraperitoneal injection of 2.5mL / kg of CCl was performed according to the weight of the mouse 4 The mixed solution with the volume ratio of 1:4 to olive oil was injected twice a week, and the induction period was 10 weeks. In addition, healthy mice were selected as controls for model construction.

[0042] The results of the histological identification of the liver tissue of the mouse that induced chronic liver injury for 10 weeks in this embodiment, such as figure 1 .b and figure 1 shown in d. The structure and collagen fibers of healthy mouse liver such as figure 1 a and figure 1 as shown in c. figure 1 In .b, the H&E stained liver tissue structure shows obvious portal vein-portal vein bridging, and also portal vein-central vein bridging, indicating that the de...

Embodiment 2

[0046] In this example, the administration experiment of BAPN was carried out on 5 mice with chronic liver injury in Example 1. Specifically, in this embodiment, 100 mg / kg of BAPN was injected intraperitoneally according to the weight of the mice, once a day, and the experimental period was 2 weeks. After 2 weeks, the mice were anesthetized with trichloroethanol, and the liver tissues were collected for analysis.

Embodiment 3

[0050] In this example, for all mouse liver tissues of the BAPN group in Example 2 and all mouse liver tissues of the control group in Comparative Example 1, RNA was extracted and reverse-transcribed into cDNA, and qPCR was performed to detect the expression of fibrosis marker genes. Express the situation. Specifically, in this embodiment, the fibrosis marker genes are selected from col 1a1, Acta2 and Desmin, respectively.

[0051] The expression situation of the fibrosis marker gene of 2 groups of mouse livers of this embodiment, such as figure 2 shown. Depend on figure 2 It can be seen that, compared with the drug carrier (Vehicle)-PBS group of the comparative example, the expressions of the fibrosis marker genes col1a1, Acta2 and Desmin in the BAPN group of Example 2 all decreased. t test (Student's t test) was performed on the difference genes among them, and it was found that there were significant differences in the fibrosis marker genes (*p<0.05, significant differ...

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Abstract

A use of aminopropionitrile in preparation of a medicine is provided. The medicine is used for treating late-stage hepatic fibrosis and cirrhosis. When compared with a contrast group free of aminopropionitrile, the medicine containing the aminopropionitrile can effectively reduce expression of fibrosis marker genes which are col lal, Acta2 and Desmin of mice with F3-stage hepatic fibrosis (based on METAVIR staging criteria), and can allow mouse liver tissue structures to be complete, collagenous fiber deposition to be reduced, collagenous fibers to be thinner, a collagen structure to be loose and dispersed, and activated astrocytes to be reduced, and therefore it is proved that the aminopropionitrile has obvious improving effects on hepatic fibrosis and cirrhosis.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular, the invention relates to the use of aminopropionitrile in the preparation of medicines. More specifically, the present invention relates to the use of aminopropionitrile in the preparation of medicines and the pharmaceutical composition for treating advanced liver fibrosis and liver cirrhosis. Background technique [0002] Liver cirrhosis is the fourteenth leading cause of death in the world, with a higher incidence in developed countries and the fourth leading cause of death in Europe. The treatment of liver fibrosis and cirrhosis also faces many challenges, such as the lack of markers to characterize the process of fibrosis, the staging of the severity of fibrosis patients, and the difficulty in predicting the course of the patient's disease, and the lack of accurate diagnosis of liver fibrosis and cirrhosis. effective treatment options for patients. [0003] With the development of ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/275A61P1/16
CPCA61K45/06A61K9/0019A61K31/275
Inventor 杜亚楠刘龙伟尤志峰
Owner TSINGHUA UNIV
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