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Application of rhein compound or its salt in preparing drugs preventing and curing hypofunction of islet beta cell

A technology of rhein and compounds, applied in the field of application in the preparation of drugs for the prevention and treatment of islet beta cell function decline

Active Publication Date: 2013-07-10
KIDNEY DISEASES INST P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no effective clinical treatment to protect and restore the function of pancreatic β cells

Method used

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  • Application of rhein compound or its salt in preparing drugs preventing and curing hypofunction of islet beta cell
  • Application of rhein compound or its salt in preparing drugs preventing and curing hypofunction of islet beta cell
  • Application of rhein compound or its salt in preparing drugs preventing and curing hypofunction of islet beta cell

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Effect of Rhein on Improving Glucose Tolerance

[0024] Drugs: rhein, 0.1% sodium cellulose dissolved.

[0025] Administration of experimental animals: 30 4-week-old db / db diabetic mice were randomly divided into a treatment group and a control group, and another 15 4-week-old db / m healthy mice were used as a normal control group. Among them, the db / db diabetes treatment group was given rhein gavage intervention (120mg / Kg, dissolved in 0.1% cellulose sodium) for 8 consecutive weeks, and the db / db diabetes control group and the db / m normal control group were administered with 0.1% cellulose sodium. Stomach.

[0026] Experimental method: After 8 weeks of administration, the mice were subjected to an intraperitoneal glucose tolerance test (IPGTT). After fasting overnight, give 0.5g / kg body weight glucose by intraperitoneal injection, collect blood from the tail of the rat at 0, 30, 60 and 120 minutes, measure whole blood glucose and insulin levels, and calculat...

Embodiment 2

[0028] Example 2 Effect of rhein on first phase insulin secretion in type 2 diabetes db / db mice

[0029] Drugs and experimental animals in the same example 1

[0030] Experimental method: After 8 weeks of drug administration, 5 animals were randomly selected from each group, and the islets were isolated for perfusion. After anesthesia, the opening of the duodenal papilla of the common bile duct was clamped in vivo, the common bile duct was punctured under a solid microscope, and 2ml of type IV collagenase at a concentration of 1 mg / ml was injected, retrograde into the pancreatic duct to expand the pancreas, and the pancreas was quickly separated, and the pancreas was placed in a Type IV collagenase 1mg / ml of Hank's balance solution was digested for 40 minutes, the collagen components were removed and washed with multiple oscillations, and the islets were successfully isolated under the microscope. A group of 50 islets was incubated in a carbon dioxide incubator for 2 hours, an...

Embodiment 3

[0032] Example 3 The effect of rhein on the content of pancreatic islet β cells

[0033] Drugs and experimental animals in the same example 1

[0034] Experimental method: Immunohistochemical assay. After the mice were anesthetized with phenobarbital sodium, the heart was perfused with normal saline and 4% paraformaldehyde (pH7.4) to fix, the pancreas was removed and placed in 4% paraformaldehyde for 4-6 hours, embedded in paraffin, and sectioned with a thickness of 5 μm. Sections were dewaxed with xylene, rehydrated with different concentrations of ethanol, blocked endogenous peroxidase activity with 0.3% hydrogen peroxide for 20 minutes at room temperature, and repaired antigens with high-pressure steam at 121°C for 10 minutes, and blocked non-specific antigens with 10% goat serum After adding rabbit anti-mouse insulin antibody, react overnight at 4°C for 14h, add biotinylated goat anti-rabbit secondary antibody and react at room temperature for 30min, develop color with di...

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Abstract

This invention provides a method for inhibiting pancreatic islet &bgr;-cell dysfunction, comprising administering to a subject in need thereof an inhibitory effective amount of a rhein compound having the general formula (I) or a pharmaceutically acceptable salt thereof,

Description

technical field [0001] The invention relates to the application of a rhein compound or a salt thereof in the preparation of a drug for preventing and treating function decline of pancreatic beta cells. Background technique [0002] Insulin resistance and the decline of pancreatic β-cell function are the main pathogenesis of type 2 diabetes. The results of the UK Prospective Diabetes Study (UKPDS) show that the β-cell function of people with newly diagnosed type 2 diabetes is only 50% of that of normal people, and thereafter declines at a rate of 4.5% per year. At present, there is no effective treatment to protect and restore the function of islet β cells clinically. [0003] Rhein (Rhein) compound or its salt is a kind of structurally definite compound, and its structural formula is as follows: [0004] [0005] Among them, M is H, alkali metal, alkaline earth metal or organic base residue, R 1 , R 2 are each independently H or acetyl. [0006] At present, the repre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/192A61K31/222A61P3/10
CPCA61K31/192A61K31/222A61P1/18A61P3/04A61P3/10
Inventor 刘志红
Owner KIDNEY DISEASES INST P L A
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