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Application of appa in preparation of medicine for treating diabetic nephropathy

A technology for diabetic nephropathy and drugs, which is applied in drug combinations, urinary system diseases, metabolic diseases, etc., can solve problems such as no related reports, and achieve good effects, good medicinal prospects, and small doses

Inactive Publication Date: 2019-05-14
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] After searching the literature, there is no relevant report on the pharmacological activity of the compound APPA

Method used

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  • Application of appa in preparation of medicine for treating diabetic nephropathy
  • Application of appa in preparation of medicine for treating diabetic nephropathy
  • Application of appa in preparation of medicine for treating diabetic nephropathy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Effect of APPA on proliferation of glomerular mesangial cells (HBZY-1)

[0035] In order to determine the effect of different concentrations of APPA on the proliferation activity of HBZY-1 cells, 6 groups were established (NS: normal control group; HG: high glucose administration model group; AL: APPA low dose (0.3 μ M) administration group; AM : APPA middle dose (0.6 μ M) administration group; AH: APPA high dose (0.9 μ M) administration group; EPS: epalrestat (10 μ M) positive control group), each group is 33mmol / L in sugar concentration and cultivates 72h , each APPA group and the EPS group were administered at the same time, and the absorbance (OD) value at 490 nm of cells in each well was detected by using the MTT method. ;

[0036] Experimental results: attached figure 1 Show: Compared with the NS group, the OD value of each experimental group decreased, HG, AL, AM, EPS group P# P## P<0.01.

Embodiment 2

[0037] Example 2 Determination of Cell Type IV Collagen and Laminin Content

[0038] By setting 6 groups (NS: normal control group; HG: high glucose administration model group; AL: APPA low dose (0.3 μM) administration group; AM: APPA medium dose (0.6 μM) administration group; AH: APPA High dose (0.9 μ M) administration group; EPS: epalrestat (10 μ M) positive control group) measure intercellular IV collagen and laminin content, the result is as attached figure 2 Shown: Compared with the normal control group, *P# P## P<0.01; By comparing the normal control group and the high-glucose-induced group, it can be found that high-glucose induction can significantly increase the generation of intercellular matrix hyperplasia, and the content of type IV collagen and laminin in the cell extract is significantly higher than that of the vehicle control group and after APPA administration, it was found that compared with the HG group, the higher the concentration of APPA administration, t...

Embodiment 3

[0039] Example 3 Determination of Cellular TGF-β1 Protein Expression

[0040] This experiment adopts the method of Western Bloot to measure 6 groups (NS: normal control group; HG: high glucose administration model group; AL: APPA low dosage (0.3 μ M) administration group; AM: APPA dosage (0.6 μ M) administration group; AH: APPA high-dose (0.9μM) administration group; EPS: epalrestat (10μM) positive control group) intracellular TGF-β1 protein, as attached image 3 The results showed: compared with the normal control group, *P# P## P<0.01; compared with the NS group, the TGF-β1 protein content in the HG and AL groups significantly increased P<0.05, and compared with the HG group, the TGF-β1 protein content in the AL and AM groups decreased significantly P <0.05, the decrease of TGF-β1 content in EPS group was the most significant P<0.01.

[0041] In conclusion, APPA has a certain inhibitory effect on the HBZY-1 cell injury model induced by high glucose, and can reduce the expre...

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Abstract

The invention discloses application of APPA (1-acetyl-5-phenyl-1H-pyrrol-3-yl acetate) in preparation of a medicine for treating the diabetic nephropathy. When serving as the medicine for treating or preventing the early diabetic nephropathy, APPA has the advantages of small dosage, low side effect, good effect and the like, and has the obvious treatment effect on the early diabetic nephropathy. The invention further discloses a preparation method of the medicine for treating or preventing the early diabetic nephropathy from APPA.

Description

technical field [0001] The invention belongs to the technical field of chemical drugs and pharmaceutical preparations, in particular to a 1-acetyl-5-phenyl-1H-pyrrol-3-yl acetate (1-acetyl-5-phenyl-1H- Application of pyrrol-3-yl acetate, APPA) in the preparation of medicine for treating type 2 diabetes. Background technique [0002] Diabetes is listed as one of the three difficult diseases by the World Health Organization. With the development of diabetes, patients often develop various forms of diabetic complications, among which diabetic nephropathy (DN) is one of the most common complications of diabetes and one of the main causes of death in diabetic patients. Diabetic nephropathy is a serious vascular complication of diabetes, which is glomerulosclerosis caused by microangiopathy caused by diabetes. Glomerular mesangial cells are very active cells in the glomerulus, which have the functions of regulating the surface area of ​​glomerular capillaries, controlling glomer...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/40A61K9/48A61K9/20A61P3/10A61P13/12
CPCA61K9/2059A61K9/4866A61K31/40
Inventor 王丽萍修志明付君徐佳
Owner JILIN UNIV
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