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Polypeptide, polypeptide derivative, medicinal salt of polypeptide and pharmaceutical composition

A technology of peptide derivatives and compositions, applied in the direction of drug combinations, microorganisms, biochemical equipment and methods, etc., can solve the problems of short plasma half-life, achieve long plasma half-life, good stability, and improve the function of islets of pancreas

Active Publication Date: 2014-09-17
SHENZHEN HIGHTIDE BIOPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a polypeptide for the short plasma half-life of INGAP-PP in the prior art

Method used

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  • Polypeptide, polypeptide derivative, medicinal salt of polypeptide and pharmaceutical composition
  • Polypeptide, polypeptide derivative, medicinal salt of polypeptide and pharmaceutical composition
  • Polypeptide, polypeptide derivative, medicinal salt of polypeptide and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0128] Example 1 Production of Polypeptides

[0129] This example describes the production of polypeptides

[0130] All peptides used in this study were synthesized using 9-fluorenylmethyl chloroformate (Fmoc) solid-phase synthesis. Simply put: Dissolve a weighed amount of 2-chlorotrityl chloride resin (1.6mmol / g) in dichloromethane (DCM). For C-terminally amidated peptides of interest, use Rink amide resin instead of 2-chlorotrityl chloride resin. For coupling reactions in the presence of hydroxybenzotriazole (Sigma Chemicals, Inc., St. Louis, MO, USA) in dimethylformamide (DMF), preactivated Fmoc-amino acids were used. The entire synthesis process uses an excess of amino acids. Deprotection of the Fmoc group in 20% piperidine in DMF leads to chain extension reactions. When the chain extension reaction was completed, the Fmoc protecting group was removed from the N-terminus of the polypeptide using DMF containing 25% piperidine, and then washed four times with DMF solutio...

Embodiment 2

[0134] Example 2 The promoting effect of polypeptide on cell proliferation

[0135] This example describes the effects of polypeptides on the growth of pancreatic cells.

[0136] Cell proliferation was measured by bromodeoxyuridine (BrdU)-labeled ELISA. Briefly, a rat pancreatic ductal ARIP cell (ATCC (American Type Culture Collection), Manassas, VA, USA) was cultured in 10% fetal bovine serum (FBS, Fetal Bovine Serum, Thermo Fisher Inc., Waltham, MA, USA), in F-12K medium (GIBCO-BRL, Gaithersburg, MD, USA) with 100 μg / ml streptomycin and 100 μg / ml penicillin. ARIP cells were inoculated into 96-well culture plates at a density of 8000 or 0 (blank control) cells / well, and 50 μl of cell culture medium was added to culture overnight for use in experiments. The next day, use serum-free medium to replace the original medium, and 50 μl of serum-free cell culture medium containing a series of concentrations of the test polypeptide (final concentrations are 10 μM, 5 μM, 1 μM, 500 nM...

Embodiment 3

[0142] Example 3 Peptide Stability Experiment

[0143] This example describes stability experiments of peptides under various conditions.

[0144]Accurately weigh a certain amount of the selected peptide, dissolve it in distilled water to a concentration of 5 mg / mL, and use it as a stock solution to examine the stability of the peptide in the culture medium. Use F-12K medium (GIBCO-BRL, Gaithersburg, MD, USA) to dilute the stock solution to 0.25 mg / mL as a working solution. Transfer each 100 µL of working solution to a separate vial. After the vials were placed in a 37°C incubator for 0, 24, 48 and 72 hours, quantitative analysis was performed using HPLC.

[0145] figure 2 and Table 6 shows the stability of the compounds in the medium. figure 2 In particular, a comparison of the stability in culture medium of INGAP-PP (peptide 1) and selected peptides, peptides 7 and 8 (see Table 2) is shown.

[0146] Table 6

[0147] polypeptide

0h

24h

48h

72h...

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Abstract

The invention provides a polypeptide. The polypeptide solves the problem that the existing polypeptide for promoting islet neogenesis has a short plasma half-life and low activity. The invention also discloses a derivative of the polypeptide, a medicinal salt of the polypeptide and a pharmaceutical composition. The polypeptide has high stability in blood and a long half life.

Description

[0001] This application is based on, and claims priority from, an earlier PCT international application (application number PCT / CN2013 / 072771) filed on March 15, 2013, the entire content of which is hereby incorporated by reference into this application. technical field [0002] The present invention mainly relates to the fields of medicine and pharmacy, especially a polypeptide, derivatives of the polypeptide, pharmaceutically acceptable salts and pharmaceutical compositions. Background technique [0003] More than 300 million people worldwide suffer from and suffer from diabetes mellitus (DM). There are two main types of diabetes: type 1 diabetes (T1D) and type 2 diabetes (T2D). Type 1 diabetes is caused by the body's inability to produce insulin and the patient needs to be treated with daily insulin. Type 2 diabetes is caused by insulin resistance, which means that the body's cells cannot use insulin properly. At present, there are many proven and effective non-insulin t...

Claims

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Application Information

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IPC IPC(8): C07K14/47A61K38/17A61P3/10C12N5/071C12N5/079
CPCA61K38/00C07K14/4733C07K14/474C12N5/0618C12N5/067C12N5/0676C12N2501/998
Inventor 刘利平白茹
Owner SHENZHEN HIGHTIDE BIOPHARM
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