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Application of Compound C in preparation of medicine used for treating non-alcoholic fatty liver disease

A compoundc, non-alcoholic technology, applied in the fields of medicine and biochemistry, can solve problems that have not yet been seen, and achieve the effect of improving formation, inhibiting inflammasome and inflammatory response

Active Publication Date: 2018-06-05
THE THIRD XIANGYA HOSPITAL OF CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, there have been no reports about the AMPK inhibitor compound C, which is used to prepare drugs for the prevention and treatment of NAFLD by inhibiting chronic inflammatory reactions

Method used

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  • Application of Compound C in preparation of medicine used for treating non-alcoholic fatty liver disease
  • Application of Compound C in preparation of medicine used for treating non-alcoholic fatty liver disease
  • Application of Compound C in preparation of medicine used for treating non-alcoholic fatty liver disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1 The present invention relates to the preparation of Compound C tablet

[0035] Take 5 grams of Compound C, add 195 grams of dextrin, mix well, and routinely press into 1000 tablets.

Embodiment 2

[0036] Embodiment 2 The present invention relates to the preparation of Compound C capsules

[0037] Take 5 grams of Compound C, add 195 grams of starch, mix well, and make 1000 capsules.

Embodiment 3

[0038] Example 3 Compound C inhibits LPS+PA to stimulate THP-1 cells to secrete various inflammatory factors

[0039] Configure 5mM storage solution: ①Compound C (25mg) was purchased from Selleck Company, centrifuged at 1000r / min for 5mins; ②Pipe 1ml DMSO into the drug tube in the ultra-clean workbench, blow and mix repeatedly; ③Take a new 50ml centrifuge tube, add 11.52ml DMSO, transfer all the liquid obtained in the drug tube into a 50ml centrifuge tube, and mix well; ④Cap the 50ml centrifuge tube tightly, and vortex briefly on the vortex to mix well; Store at 20 degrees.

[0040] Prepare 25uM working solution: ①Take the aliquoted compound C storage solution and place it in a 37°C water bath for rewarming; ②Add 5ul of storage solution per 1ml of culture medium to make a working solution for the following cell experiments.

[0041] Use 1640 medium to culture THP-1 cells in a six-well plate, and change the medium every other day. When the cell density is 1*10^6, divide them i...

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Abstract

The invention discloses application of a Compound C in preparation of a medicine used for treating a non-alcoholic fatty liver disease (NAFLD). Experimental results show that the Compound C is provedto be capable of effectively inhibiting NLRP3 inflammasome and inflammation reaction by virtue of experiments, so that formation of the NAFLD is obviously reduced. Therefore, a research foundation anda theoretical basis are provided for development of medicines used for treating the NAFLD.

Description

technical field [0001] The invention belongs to the technical field of medicine and biochemistry, and relates to the application of compound C in the preparation of drugs for the treatment of nonalcoholic fatty liver, in particular to the application of compound C, an adenylate-activated protein kinase (AMPK) inhibitor, in the preparation and treatment of non-alcoholic fatty liver New applications in nonalcoholic fatty liver disease (NAFLD) preparations. Background technique [0002] Compound C(6-[4-(2-piperidin-1-yl-etoxy)-phenyl]-3-pyridin-4-yl-pyrrazolo[1,5-a]pyrimidine), also known as dorsomorphin, the molecular formula is C 24 h 25 N 5 O, belongs to pyrazolopyrimidine protein kinase inhibitors. Existing studies have proved that compound C is not only an inhibitor of AMPK, but also has the effect of inhibiting other signal transduction pathways, and this effect does not depend on the effect on AMPK. inhibition. It has been reported that compound C can inhibit the che...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P1/16
CPCA61K31/519
Inventor 王芳莫朝晖项荣陈科杨文君陈柯竹
Owner THE THIRD XIANGYA HOSPITAL OF CENT SOUTH UNIV
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