Application of chitooligosaccharide biguanide derivative in preparation of drug for treating pancreatic insulin defects

A biguanide derivative and sugar biguanide technology, applied in the field of pharmacy, can solve the problems of accelerated diabetes process, high metabolic demand, metabolic disorder and the like, and achieve the effects of repairing pancreatic β-cell defects, simple operation process, and promoting secretion

Pending Publication Date: 2020-03-31
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Functional deficits in islet β-cells after adaptation are primarily caused by high metabolic demands and are associated with high mortality, leading to metabolic disturbances and accelerated diabetes progression

Method used

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  • Application of chitooligosaccharide biguanide derivative in preparation of drug for treating pancreatic insulin defects
  • Application of chitooligosaccharide biguanide derivative in preparation of drug for treating pancreatic insulin defects
  • Application of chitooligosaccharide biguanide derivative in preparation of drug for treating pancreatic insulin defects

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] (1) Take by weighing 10g deacetylation degree 97%, the chitosan oligosaccharide of weight-average molecular weight 1500Da is dissolved in 0.2mol / L hydrochloric acid solution and preparation concentration is the chitosan oligosaccharide hydrochloric acid solution of 0.25g / mL, regulates with the hydrochloric acid of 1mol / L The pH value of the solution reaches 1, and then according to 0.5 times the number of moles of chitosan oligosaccharide amino groups, weigh the corresponding mass of dicyandiamide, stir and dissolve it in distilled water at 45-60 °C;

[0028] (2) Mix the aqueous solution of dicyandiamide with the hydrochloric acid solution of chitosan oligosaccharide, adjust the pH value to 1, then carry out microwave liquid phase synthesis, control the reaction time for 20min, the microwave reaction power is 400w, the reaction temperature is 100°C, and the stirring speed 100r / min;

[0029] (3) After the reaction, the reaction solution was left to cool down to room temp...

Embodiment 2

[0031] (1) Take by weighing 10g deacetylation degree 97%, the chitosan oligosaccharide of weight-average molecular weight 3000Da is dissolved in 0.2mol / L hydrochloric acid solution and preparation concentration is the chitosan oligosaccharide hydrochloric acid solution of 0.25g / mL, regulates with the hydrochloric acid of 1mol / L The pH value of the solution reaches 1, and then according to 0.5 times the number of moles of chitosan oligosaccharide amino groups, weigh the corresponding mass of dicyandiamide, stir and dissolve it in distilled water at 45-60 °C;

[0032] (2) Mix the aqueous solution of dicyandiamide with the hydrochloric acid solution of chitosan oligosaccharide, adjust the pH value to 1, then carry out microwave liquid phase synthesis, control the reaction time for 20min, the microwave reaction power is 400w, the reaction temperature is 100°C, and the stirring speed 150r / min;

[0033] (3) After the reaction, the reaction solution was allowed to stand and cooled to...

Embodiment 3

[0035] (1) Take by weighing 10g deacetylation degree 97%, the chitosan oligosaccharide of weight-average molecular weight 1500Da is dissolved in 0.2mol / L hydrochloric acid solution and preparation concentration is the chitosan oligosaccharide hydrochloric acid solution of 0.25g / mL, regulates with the hydrochloric acid of 1mol / L The pH value of the solution is 1, and then according to 1 times the number of moles of chitosan oligosaccharide amino groups, weigh the corresponding mass of dicyandiamide, stir and dissolve it in distilled water at 45-60 °C;

[0036] (2) Mix the aqueous solution of dicyandiamide with the hydrochloric acid solution of chitosan oligosaccharide, adjust the pH value to 1, then carry out microwave liquid phase synthesis, control the reaction time for 20min, the microwave reaction power is 400w, the reaction temperature is 100°C, and the stirring speed 100r / min;

[0037] (3) After the reaction, the reaction solution was left to cool down to room temperature...

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Abstract

The invention discloses an application of a chitooligosaccharide biguanide derivative in preparation of a drug for treating pancreatic insulin defects. The chitooligosaccharide biguanide derivative is prepared by the following steps: weighing chitooligosaccharide and hydrochloric acid in a four-necked bottle, performing a reaction under stirring in a microwave device, adding a dicyandiamide aqueous solution according to the ratio of raw materials, adjusting the pH of the solution by using hydrochloric acid, and continuing a reaction under stirring in the microwave device; and after the reaction is completed, performing alcohol precipitation on the mixed solution, performing drying, and performing grinding to obtain the chitooligosaccharide biguanide derivative. The production efficiency is high, the operation process is simple, the reaction process is clean and environmentally friendly, and the product performance is good; and the chitooligosaccharide biguanide derivative is administered in an intragastric administration manner, after the derivative treatment, IRS2 protein expression is increased, so that a PI3K-Akt signal transduction pathway is activated, FoxO1 nuclear output ispromoted, and downstream insulin is stimulated to secrete related signaling pathway PDX-1-GLUT2 / GCK to promote insulin secretion and repair the insulin beta cell defects.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a microwave synthesis preparation method of chitosan oligosaccharide biguanide derivatives and its application in the preparation of drugs for treating islet defects. Background technique [0002] Diabetes mellitus is a common metabolic disorder characterized by chronic hyperglycemia, carbohydrate, lipid, and protein metabolism that may be strongly associated with genetic or environmental influences (Murphy R, Ellard S, Hattersley AT. Clinical implication of a molecular genetic classification of monogenic beta-cell diabetes[J].Nat Clin Pract Endocrinol Metab,2008,4(4):200-213.), wherein non-islet-dependent diabetes (type 2 diabetes, T2DM) includes 90%~95 % of diabetic patients (Liu C W, WangY C, Hsieh C C, et al. Guava (Psidium guajava, Linn.) leaf extract promotes glucoseuptake and glycogen accumulation by modulating the insulin signaling pathway in high-glucose-induced insul...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K31/155A61P3/10
CPCA61K47/61A61K31/155A61P3/10
Inventor刘晓非邹雅露王园园赵励彦郑淇方刘宇星
OwnerTIANJIN UNIV