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Application of sphingosine kinase inhibitor to preparation of medicine for treating hepatic fibrosis

A sphingosine kinase, liver fibrosis technology, applied in the field of medicine, can solve the problems of single treatment mechanism and unsatisfactory treatment effect, etc.

Inactive Publication Date: 2018-05-29
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above methods have the problems of single treatment mechanism and unsatisfactory treatment effect.

Method used

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  • Application of sphingosine kinase inhibitor to preparation of medicine for treating hepatic fibrosis
  • Application of sphingosine kinase inhibitor to preparation of medicine for treating hepatic fibrosis
  • Application of sphingosine kinase inhibitor to preparation of medicine for treating hepatic fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] This example provides a clinical application of a sphingosine kinase inhibitor in the preparation of a drug for treating liver fibrosis. The sphingosine kinase inhibitor is SphK1 inhibitor 5C.

[0039] The SphK1 inhibitor 5C was purchased from Juyan Biomedical Technology Co., Ltd. (Cayman China), the product number is: CAY10621 (5C), its molecular weight is 435.6, and its molecular formula is C 26 h 45 NO 4 , the molecular structure formula is:

[0040]

Embodiment 2

[0042]This example provides a clinical application of a sphingosine kinase inhibitor in the preparation of a drug for treating liver fibrosis. The sphingosine kinase inhibitor is SphK2 inhibitor ABC294640. The SphK2 inhibitor ABC294640 was purchased from Shanghai Bluewood Biotechnology Co., Ltd. (Selleck China), with a molecular weight of 380.91 and a molecular formula of C 23 h 25 ClN 2 O, its structural formula is as follows:

[0043]

Embodiment 3

[0045] This example provides a clinical application of a sphingosine kinase inhibitor in the preparation of a drug for treating liver fibrosis. Sphingosine kinase inhibitors are SphK inhibitors SK I-II. The SphK inhibitor SK I-II was purchased from Shanghai Bluewood Biotechnology Co., Ltd. (Selleck China), with a molecular weight of 302.78 and a molecular formula of C 15 h 11 ClN 2 OS, its structural formula is as follows:

[0046]

[0047] Pharmacodynamic experiment verification:

[0048] 50 male C57BL / 6 mice were randomly divided into 5 groups, 10 in each group, specifically blank control group A1, inhibitor negative control group B1, SphK1 inhibitor group C1 provided in Example 1, and SphK1 inhibitor group C1 provided in Example 2. SphK2 inhibitor group D1 and the SphK inhibitor group E1 provided in Example 3.

[0049] Among them, 10 mice in the blank control group A1 were intraperitoneally injected with corn oil solution according to the injection standard of body ...

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Abstract

The invention provides application of a sphingosine kinase inhibitor to preparation of a medicine for treating hepatic fibrosis. The sphingosine kinase inhibitor is an SphK1 inhibitor 5C or an SphK2 inhibitor ABC294640 or SphK inhibitors SK I to II. The medicine prepared from the SphK inhibitor is used for blocking inflammatory reaction and collagen deposition, which promote the hepatic fibrosis,so that the activation of hepatic stellate cells is inhibited and a pathological process of the hepatic fibrosis is alleviated, and furthermore, the development of the hepatic fibrosis is radically prevented. The invention provides a novel medicine source for the medicine for treating the hepatic fibrosis. The technology provided by the invention is financially aided through Key Project of NaturalScience Foundation of China (81530102), Key Project of Natural Science Foundation of Guangdong (2016A030311014) and Guangdong Technology Plan (2017A020211007).

Description

technical field [0001] The invention belongs to the field of medicine and relates to a medicine for treating liver fibrosis, in particular to the application of a sphingosine kinase inhibitor in the preparation of medicine for treating liver fibrosis. Background technique [0002] Liver fibrosis is a dynamic process from chronic liver injury to liver cirrhosis. It is characterized by a large amount of extracellular matrix (ECM) synthesis and secretion, but its degradation is absolutely or relatively insufficient, resulting in diffuse deposition of extracellular matrix in the liver. It starts with hepatocyte necrosis, followed by inflammatory response, release of inflammatory factors and pro-fibrotic factors, activation of hepatic stellate cells (HSC), and finally a significant imbalance between synthesis and degradation of liver collagen. Liver fibrosis is a common pathological result of the development of various chronic liver diseases. At present, various studies have pro...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/421A61K31/4409A61K31/426A61P1/16
CPCA61K45/00A61K31/421A61K31/426A61K31/4409
Inventor 兰天郭姣李昌正
Owner GUANGDONG PHARMA UNIV
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