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A kind of polypeptide, polypeptide derivative, pharmaceutically acceptable 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: 2019-04-16
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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  • A kind of polypeptide, polypeptide derivative, pharmaceutically acceptable salt of polypeptide and pharmaceutical composition
  • A kind of polypeptide, polypeptide derivative, pharmaceutically acceptable salt of polypeptide and pharmaceutical composition
  • A kind of polypeptide, polypeptide derivative, pharmaceutically acceptable salt of polypeptide and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] The production of embodiment 1 polypeptide

[0141] This example describes the production of polypeptides

[0142] 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

[0146] Stability experiment of embodiment 2 peptide

[0147] This example describes stability experiments of peptides under various conditions.

[0148] 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.

[0149] 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

[0177] Example 3 Effects of Peptides on Glucose-Stimulated Insulin Secretion

[0178] This example describes the effect of peptides on glucose stimulated insulin secretion (GSIS).

[0179] 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), Peptide 1, Peptide 12, and Peptide 16 were added at 10 μg / mL, see Table 10 below.

[0180] Table 10

[0181]

[0182] in CO 2 / O 2 (5 / 95%), 37 ℃ environment, in 1.0ml containing 0.5% (...

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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 Patents(China)
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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