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Application of CGP 57380 in preparation of medicine for preventing or treating type 2 diabetes

A type 2 diabetes and drug technology, applied in the field of biomedicine, can solve the problems that the research on metabolic diseases has not been reported yet

Pending Publication Date: 2021-09-14
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In oncology research, CGP 57380 can inhibit the proliferation, migration and invasion of nasopharyngeal carcinoma cells by inhibiting the nuclear translocation of β-catenin, but the research on metabolic diseases such as type 2 diabetes has not been reported

Method used

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  • Application of CGP 57380 in preparation of medicine for preventing or treating type 2 diabetes
  • Application of CGP 57380 in preparation of medicine for preventing or treating type 2 diabetes
  • Application of CGP 57380 in preparation of medicine for preventing or treating type 2 diabetes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Experimental verification that CGP 57380 can be used as an inhibitor of the kinase BRSK2, and its enzyme activity is detected at the same time

[0028] The following experiments were entrusted to Shanghai Ruizhi Chemical Research Co., Ltd. to complete.

[0029] 1. Preparation of experimental materials:

[0030] 1) BRSK2 (Carna, Cat.No 02-116, Lot.No 08CBS-0302);

[0031] 2) Peptide10 (invitrogen, Cat. No 116583 Lot. No P130913-XP116583);

[0032] 3) ADP-Glo TM Kinase Assay (Promege, Cat.No v9102 / 3, Lot.No 314795);

[0033] 4) ATP (Sigma, Cat. No. A7699-1G, CAS No. 987-65-5);

[0034] 5) DMSO (Sigma, Cat. No. D2650, Lot. No. 474382);

[0035] 6) EDTA (Gibco, Cat. No. 15575, Lot No. 846901);

[0036] 7) 96-well plate (Corning, Cat.No.3365, Lot.No.22008026);

[0037]8) 384-well plate (Corning, Cat.No.4512, Lot.No.13315417);

[0038] 9) Staurosporine (Sellekchem, Cat. No. S1421, Lot. No. S142105).

[0039] 2. Kinase response system:

[0040] 1)1xkinase b...

Embodiment 2

[0068] Example 2 The effect of CGP 57380 on BRSK2 activity and protein level was detected at the cell level of MIN6, and the effect of CGP 57380 on the glucose-stimulated insulin secretion function was detected at the cell level and on primary pancreatic islets.

[0069] Cell line: mouse islet β cell line MIN6 ( DOI: 10.1210 / endo-127-1-126 ), human primary islets (Tianjin First Central Hospital).

[0070] Experimental drug: CGP 57380 was purchased from MCE Company, and the negative control was DMSO.

[0071] The specific steps are: 20-24 hours after the MIN6 cells were plated, the cells were treated with CGP 57380 (10uM) for 12 hours and 24 hours respectively, the control group was set as DMSO treatment, and Western Blot was used to detect the phosphorylation level of the BRSK2 substrate and the protein level of BRSK2 in the cells The change. Under the same treatment conditions, GSIS detects the function of the cells. The detailed steps are to pre-equilibrate MIN6 cells wit...

Embodiment 3

[0077] Example 3 Effect of CGP 57380 on metabolic phenotype of type 2 diabetic mice.

[0078] Experimental animals: C57BL / 6J mice of 3-4 weeks were fed with normal diet (NCD) and high-fat diet (HFD) for about 4 months, and the animals were randomly divided into cages and fed freely.

[0079] Experimental steps:

[0080] 1) Mice fed with normal feeding and high-fat feeding for about 4 months were randomly divided into 5-7 mice in each group. The HFD group was given CGP 57380 (HFD CGP 57380) and the negative control (HFD Vehicle) respectively, and the NCD group Only the negative control (NCDVehicle) was administered intragastrically, once a day, at a dose of 10 mg / kg;

[0081] 2) The blood sugar and body weight of the mice were detected every week for 4-5 weeks. The blood sugar measurement method was: take 1 drop of tail vein blood, and measure random blood sugar with blood sugar test strips and a rapid blood glucose meter;

[0082] 3) The level of glucose tolerance of the mic...

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Abstract

The invention discloses an application of CGP 57380 in preparation of a medicine for preventing and treating type 2 diabetes. CGP 57380 is a cell-permeable pyrazole-pyrimidine compound, and it is found that CGP 57380 can relieve hyperglycemia and hyperinsulinemia of high-fat-induced type 2 diabetic mice and improve the glucose tolerance level and insulin sensitivity of high-fat mice by inhibiting the kinase activity and protein expression quantity of BRSK2, and finally, the glycolipid metabolism disorder of the high-fat mice is remarkably improved, the effect of treating the type 2 diabetes is achieved, and an important reference value is provided for clinical research and development of new drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to the application of inhibitor CGP 57380 in the preparation of drugs for preventing or treating type 2 diabetes. Background technique [0002] Diabetes mellitus is a chronic metabolic disease characterized by persistently elevated blood sugar. According to the latest global diabetes report released by the International Diabetes Federation (IDF) in 2019, as of 2019, about 4.6 people worldwide suffer from diabetes, and this number is expected to reach 700 million by 2045. With the continuous progress of diabetes, diabetic retinopathy, diabetic nephropathy, and diabetes-related cardiovascular diseases are also coming one after another, which brings a huge economic burden to the family and society. Therefore, it is important to explore the pathogenesis of diabetes and develop corresponding therapeutic drugs. socioeconomic significance. [0003] Diabetes is mainly divid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P3/10A61P3/04
CPCA61K31/519A61P3/10A61P3/04
Inventor 朱云霞韩晓许茹凤王开远姚正建
Owner NANJING MEDICAL UNIV
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