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Polyethylene glycol modified GLP-1 receptor agonist peptide and application thereof

A technology of GLP-1 and polyethylene glycol, which is applied in the direction of medical preparations containing non-active ingredients, medical preparations containing active ingredients, peptides, etc., can solve the problems of short half-life of polypeptides, and achieve the effect of preventing or treating diabetes

Inactive Publication Date: 2015-12-23
SUZHOU PULUODA BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the half-life of the above-mentioned polypeptides is short, which brings pain to patients with chronic diseases of diabetes.

Method used

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  • Polyethylene glycol modified GLP-1 receptor agonist peptide and application thereof
  • Polyethylene glycol modified GLP-1 receptor agonist peptide and application thereof
  • Polyethylene glycol modified GLP-1 receptor agonist peptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] In Vitro Cell Viability Determination of Polyethylene Glycol Modified GLP-1 Receptor Agonist Polypeptide

[0015] The MTT colorimetric method was used. Insulinoma cells (INS-1 cells) with logarithmic growth were added to a 96-well culture plate at 1.0×105, and cultured for 24 hours. Different concentrations of the experimental drug polyethylene glycol-modified GLP were added to the experimental wells and positive drug control wells. -1 receptor agonistic polypeptide; add the same volume of solvent to the blank group. Set up five duplicate wells in every well, culture 48h, add MTT in every hole, after 4h of action, add DMSO, hatch 30min, measure the absorbance A value at 570nm place of microplate reader, according to the formula cell growth proliferation rate=(experimental group absorbance value / Absorbance value of control group -1)×100%. The calculated EC50 of the experimental drug was 53.41nmol / L.

Embodiment 2

[0017] In Vivo Hypoglycemic Experiment of Polyethylene Glycol Modified GLP-1 Receptor Agonist Polypeptide

[0018] Kunming mice were fed with high-fat and high-sugar to a body weight of 18-22 g, half male and half female, fasted for 24 hours before the experiment, and intraperitoneally injected with streptozotocin (STZ) 50 mg / kg (1% citrate buffer). liquid solution preparation). One week later, blood glucose (BS) was measured by blood collection from the tail vein of the mice. If the BS was higher than 16mmol / L, the modeling was successful. After modeling, the mice were divided into 3 groups, 10 in each group. Diabetes model group (DM group): subcutaneous injection of the same amount of PBS buffer; control group (exenatide): 20 μg / kg subcutaneous injection (dissolved in 0.1mol / LPBS buffer), twice a day, continuously for 15 days; sample group (polyethylene glycol-modified GLP-1 receptor agonist polypeptide): 1 mg / kg subcutaneous injection (dissolved in 0.1mol / LPBS buffer solu...

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Abstract

The invention relates to the field of medicines, and concretely relates to a polypeptide with GLP-1 receptor promotion activity and capable of preventing and treating diabetes. The sequence of the peptide is a brand sequence represented by PEG-MRLLPLLALLALWGPDPAAAFV, the molecular weight of PEG is 1000-20000, and the peptide is used for preventing or treating diabetes. The peptide can be used to treat the diabetes, and has potential new drug exploitation values.

Description

Technical field: [0001] The invention relates to the field of medicine, in particular to a GLP-1 receptor agonist polypeptide for treating diabetes. Background technique: [0002] Diabetes mellitus is a group of metabolic diseases characterized by hyperglycemia. It is a syndrome of glucose, protein and lipid metabolism disorders caused by insufficient insulin or defects in insulin cell metabolism. In recent years, the number of diabetic patients has gradually increased, and is divided into type I diabetes and type II diabetes. Among them, the number of patients with type II diabetes accounts for 85-90% of the total number of diabetes, which seriously threatens the health and life of patients. If diabetes is not well controlled, it may cause many complications, such as diabetic nephropathy, retinopathy, high blood pressure, etc. [0003] At present, most patients treat diabetes by injecting insulin or oral hypoglycemic drugs to help control blood sugar in the body, or regul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00A61K47/34A61K38/16A61P3/10
CPCA61K38/00A61K47/10
Inventor 罗瑞雪
Owner SUZHOU PULUODA BIOLOGICAL SCI & TECH
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