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

A technology of peptide derivatives and compositions, applied in the fields of polypeptides and derivatives of the polypeptides, pharmaceutically acceptable salts and pharmaceutical compositions, can solve the problems of short plasma half-life and the like, achieve long plasma half-life, good stability, and improve pancreatic islets effect of function

Inactive 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

[0138] The production of embodiment 1 polypeptide

[0139] This example describes the production of polypeptides

[0140] 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 s...

Embodiment 2

[0144] Stability experiment of embodiment 2 peptide

[0145] This example describes stability experiments of peptides under various conditions.

[0146] 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.

[0147] Table 5 shows the stability of the compounds in the medium. Table 5 shows a comparison of the stability in culture medium of INGAP-PP (peptide 1) and selected peptides, peptide 12 and peptide 16 (see Table 2). in particular, figure 1 Stability comparisons of the INGAP peptide (peptide 1) and selected homo...

Embodiment 3

[0181] Example 3 Effects of Peptides on Glucose-Stimulated Insulin Secretion

[0182] This example describes the effect of peptides on glucose stimulated insulin secretion (GSIS).

[0183] Pancreatic tissue was extracted from male adult Sprague-Dawley (SD) rats. After 7 days of acclimatization, the animals were sacrificed by cervical dislocation, and the whole pancreas was harvested, and the islets were digested with collagenase. After digestion, store islets at 37 °C in a humidified environment at pH 7.4 containing 10% (v / v) fetal bovine serum, 1% penicillin / streptomycin, 10 mM glucose (5% CO 2 / 95%O 2 ) in RPMI1640 (Carlsbad, California, USA) medium, and divided into the following groups: without adding any compound (control group), adding 100nM glucagon-like peptide-1 (GLP-1 group), Add 10 μg / mL peptide 1 group, peptide 12 group, peptide 16 group, see Table 11 below.

[0184] Table 11

[0185]

[0186] in CO 2 / O 2 (5 / 95%), 37 ℃ environment, in 1.0ml containing 0....

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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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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/47C12N5/071C12N5/079A61K38/17A61P3/10
CPCC07K14/4733A61K38/00C07K14/474C12N5/0618C12N5/067C12N5/0676C12N2501/998
Inventor 刘利平白茹
Owner SHENZHEN HIGHTIDE BIOPHARM
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