Application of aromatase inhibitor in preparation of anti-cirrhosis or anti-liver fibrosis drugs

A technology of anti-liver fibrosis and aromatase, applied in the application field of medicine

Active Publication Date: 2013-06-19
SHANGHAI INST OF ONCOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, anastrozole had no significant eff

Method used

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  • Application of aromatase inhibitor in preparation of anti-cirrhosis or anti-liver fibrosis drugs
  • Application of aromatase inhibitor in preparation of anti-cirrhosis or anti-liver fibrosis drugs
  • Application of aromatase inhibitor in preparation of anti-cirrhosis or anti-liver fibrosis drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0029] Example 2: Acquisition of Serum and Liver Specimens

[0030] a) Serum preparation: After 8 weeks, the rats were sacrificed. The blood was placed in a refrigerator at 4°C overnight, and the next day, the supernatant was drawn and centrifuged at 3000rpm for 20 minutes, and the supernatant was carefully drawn and stored at -20°C.

[0031] b) Treatment of the liver: cut the left liver lobe and wash it twice in PBS, then put it into a 50ml centrifuge tube and fix it by soaking in paraformaldehyde solution for paraffin sectioning.

Embodiment 3

[0032] Embodiment 3: detection of serum ALT and AST

[0033] Alanine aminotransferase (ALT) kit and aspartate aminotransferase (AST) kit were purchased from Shanghai Shensuo Youfu Medical Diagnostic Products Co., Ltd.

[0034] a) Take a 96-well plate, add 7.5 μl of rat serum respectively, and make three replicate wells for each sample. Then add 150 μl of the R-1 solution in the kit to the sample well, mix well and react for 5 minutes;

[0035] b) Add 50 μl of the R-2 solution in the kit and mix;

[0036] c) Measure the absorbance A1 at 340nm wavelength after 1 minute;

[0037] d) Measure the absorbance A2 at 340nm wavelength again after 4 minutes;

[0038] e) Calculation of rat serum ALT value:

[0039] ALT(U / L)=(A1-A2) / 4 minutes×207.5μl×1000 / (6.22×7.5μl×1cm)

[0040] AST(U / L)=(A1-A2) / 4 minutes×207.5μl×1000 / (6.22×7.5μl×1cm)

[0041] Carbon tetrachloride (CCl 4 ) induced rat liver fibrosis model is currently the most commonly used animal model for studying liver fibrosis...

Embodiment 4

[0042] Embodiment 4: making of paraffin section and section H&E staining and Sirius red staining

[0043] Hematoxylin, eosin and Sirius red were purchased from Sinopharm Chemical Reagent Co., Ltd., and saturated picric acid buffer was purchased from Yuanye Biotechnology Co., Ltd.

[0044] After paraformaldehyde-fixed rat liver tissue pieces were dehydrated, transparent, and soaked in wax, they were embedded in paraffin with an embedding machine, and the wax pieces were solidified and stored in a refrigerator at 4°C. Subsequently, the tissue wax blocks were made into paraffin sections for H&E staining and Sirius red staining.

[0045] (1) H&E staining

[0046] a) Dewaxing: dewaxing by xylene I and II for 10 minutes each;

[0047] b) Hydration: Put the slices in 100%, 95%, 85%, 75% alcohol solutions of various levels for 10 minutes each, rinse with tap water for 5 minutes, 1×PBS for 5 minutes, and incubate in 0.3% H2O2 at 37°C for 30 minutes. Minutes later, wash again with 1×...

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Abstract

The invention relates to application of an aromatase inhibitor in preparation of anti-cirrhosis or anti-liver fibrosis drugs. The aromatase inhibitor particularly can be exemestane, formestane, letrozole or anastrozole, and they can all reach good effects in anti-fibrosis and anti-cirrhosis aspects.

Description

technical field [0001] The invention relates to a new pharmaceutical application of an aromatase inhibitor, in particular, the application of the aromatase inhibitor in the preparation of anti-hepatic cirrhosis or anti-hepatic fibrosis drugs. Background technique [0002] Liver cirrhosis is one of the common chronic diseases that seriously endanger human health. Liver fibrosis is the pathological basis of liver cirrhosis. A variety of etiologies (such as viral hepatitis, alcoholic liver disease, non-alcoholic liver disease, drug and chemical factor damage, etc.) cause liver damage and inflammation, leading to liver fibrosis and eventually developing into cirrhosis of the liver. Liver fibrosis is the result of excessive deposition of extracellular matrix, and it is also the main intermediate link in the further development of liver cirrhosis. The activation and proliferation of hepatic stellate cells (Hepatic Stellate Cells, HSCs) is the central link in the formation of liv...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/566A61K31/4196A61P1/16
Inventor 张志刚覃文新王亚辉
Owner SHANGHAI INST OF ONCOLOGY
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