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Oral hypoglycemic peptide as well as fatty acid derivative and application thereof

A fatty acid and derivative technology, applied in the field of medicine and biology, can solve problems such as low oral availability, difficulty in absorption, and inability to maintain drug concentration, and achieve the effect of avoiding enzymatic hydrolysis failure

Active Publication Date: 2019-11-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low oral availability of peptides and protein drugs, no practical results have been obtained. At present, there are still no related peptides and protein drugs that can be administered orally. The main reasons are two aspects: 1. Peptides, Protein drugs are mostly macromolecules with large molecular weight and poor fat solubility, making them difficult to absorb in the intestinal tract; 2. There are a large number of proteases in the intestinal tract, which will quickly degrade the biomacromolecules entering the intestinal tract, so that the drugs in the intestinal tract cannot maintain Concentrations required for treatment

Method used

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  • Oral hypoglycemic peptide as well as fatty acid derivative and application thereof
  • Oral hypoglycemic peptide as well as fatty acid derivative and application thereof
  • Oral hypoglycemic peptide as well as fatty acid derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1 Determination of resistance to enzymolysis of OHP1-OHP6

[0070] Step 1: Prepare trypsin, protease, and elastase solutions with a concentration of 0.005 mg / mL, and incubate each protease solution at 37°C for 15 minutes.

[0071] Step 2: Mix 500 μL of 0.5 mg / mL OHPX solution (OHPX is one of OHP1-OHP6, the same below) with an equal volume of protease solution, that is, each protease: OHPX=1:100 (w / w), Incubate at 37°C for 60 min. After the reaction, take out 50 μL of the reaction solution, add 50 μL of 1% (v / v) TFA solution to stop the reaction, centrifuge at room temperature at 12000 rpm for 5 min, collect the supernatant, and use RP-HPLC to analyze the supernatant. detection. At the same time, Exendin-4 (i.e. exenatide), TSME1, and TSME2 were used as control samples, which were treated and detected with the same volume and concentration.

[0072] The third step: use RP-HPLC to detect: the chromatographic column is a Zorbax Eclipse Plus C18 reversed-phase chr...

Embodiment 2

[0079] Example 2 Determination of the ability of OHP1-OHP6 to activate the glucagon-like peptide-1 receptor

[0080] Step 1: Using the CHO cell line that can stably express the glucagon-like peptide-1 receptor on the cell membrane surface and connect the luciferase reporter gene constructed earlier in our laboratory, at 37°C, 5% CO 2 The in vitro activity assay was performed using the luciferase reporter gene method after cultured to the third passage in a cell culture incubator.

[0081] Step 2: For experimental determination, the cells were first digested with 0.25% trypsin, and then the complete medium containing 0.25% fetal bovine serum was added. Take 2×10 5 Inoculate the cell solution in a 96-well plate at a concentration of 1 cell / mL, inoculate 100 μL per well, and inoculate at 37°C, 5% CO 2 cultured in a cell culture incubator for 4 h.

[0082] Step 3: Take out the 96-well plate, and add 20 μL of OHPX solution, TSME1 solution, TSME2 solution, or Exendin-4 positive con...

Embodiment 3

[0091] Example 3 OHP1 and OHP2 activate the content of the second messenger cAMP downstream of the glucagon-like peptide-1 receptor

[0092] The first step: use the CHO cell line constructed in our laboratory that can stably express the GLP-1 receptor on the cell membrane surface and connect the luciferase reporter gene to carry out the second messenger molecule cAMP downstream of the glucagon-like peptide-1 receptor Determination of activation content, cell culture conditions as previously described.

[0093] Step 2: For experimental determination, the cells were first digested with 0.25% trypsin, and then a complete medium containing 0.25% fetal bovine serum and 0.5mmol / L IBMX was added. Take 2×10 5 Inoculate the cell solution in a 96-well plate at a concentration of 1 cell / mL, inoculate 100 μL per well, and inoculate at 37°C, 5% CO 2 cultured in a cell culture incubator for 4 h.

[0094] Step 3: Take out the 96-well plate, and add a certain amount of OHP1 / OHP2 solution o...

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Abstract

The invention relates to oral hypoglycemic peptide as well as a fatty acid derivative and application thereof. The sequence of the polypeptide is shown in SEQ ID NO.1. The polypeptide or the fatty acid derivative can be used for preparing a drug or a drug composition for preventing or treating diabetes or preparing a hypoglycemic drug or drug composition. Compared with the prior art, the polypeptide can well prevent enzymolysis ineffectiveness in gastrointestinal tracts for enzymolysis resistance of protease and is more suitable to be used as an oral hypoglycemic drug.

Description

technical field [0001] The invention relates to an oral hypoglycemic peptide, its fatty acid derivatives and uses, and belongs to the field of medical biotechnology. Background technique [0002] Diabetes is a metabolic disease characterized by persistent hyperglycemia caused by multiple etiologies. Its complications involve cardiovascular and cerebrovascular tissues, kidney tissues, eyes, feet and other tissues and organs. Once it occurs, it is difficult to reverse . With the improvement of living standards and the aggravation of aging, its incidence has a tendency to increase year by year. According to WHO statistics, the current incidence of diabetes is 2.8%, and it is expected to increase to 4.8% by 2030. Nearly 10% of adults in my country suffer from diabetes. According to authoritative data, the number of diabetic patients in my country will rank first in the world by 2030, and the annual consumption of diabetes and its complications will reach 43.2 billion US dollar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/575C07K1/107A61K38/22A61P3/10
CPCA61K38/00A61P3/10C07K14/57563
Inventor 高向东田浤陆玮晟姚文兵赛文博
Owner CHINA PHARM UNIV
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