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Polypeptide, derivative of polypeptide, pharmaceutical salt of polypeptide, pharmaceutical composition and application of polypeptide or derivative of polypeptide

A technology of peptide derivatives and compositions, applied in the field of polypeptides and derivatives of the polypeptides, can solve the problems of short plasma half-life and the like, and achieve the effects of long plasma half-life, good stability, and improvement of islet function

Inactive Publication Date: 2015-05-06
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, derivative of polypeptide, pharmaceutical salt of polypeptide, pharmaceutical composition and application of polypeptide or derivative of polypeptide
  • Polypeptide, derivative of polypeptide, pharmaceutical salt of polypeptide, pharmaceutical composition and application of polypeptide or derivative of polypeptide
  • Polypeptide, derivative of polypeptide, pharmaceutical salt of polypeptide, pharmaceutical composition and application of polypeptide or derivative of polypeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0142] The production of embodiment 1 polypeptide

[0143] This example describes the production of polypeptides

[0144] All peptides used in this study were synthesized using 9-fluorenylmethyl chloroformate (Fmoc) solid-phase synthesis. Briefly, a weighed amount of 2-chlorotrityl chloride resin (1.6 mmol / g) was dissolved 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 DM...

Embodiment 2

[0148] Stability experiment of embodiment 2 peptide

[0149] This example describes stability experiments of peptides under various conditions.

[0150] 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. The stock solution was diluted to 0.25 mg / mL using F-12K medium (GIBCO-BRL, Gaithersburg, Maryland, USA) 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.

[0151] Table 5 shows the stability of the compounds in the medium. Table 5 shows the stability comparison in culture medium of INGAP-PP (peptide 1) and selected polypeptides, peptide 12 and peptide 16 (see Table 2). in particular, figure 1 Stability comparisons of the INGAP peptide (peptide 1) and sele...

Embodiment 3

[0183] Example 3 Effects of Peptides on Glucose-Stimulated Insulin Secretion

[0184] This example describes the effect of peptides on glucose-stimulated insulin secretion (GSIS).

[0185] 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, islets were stored 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 the medium of RPMI 1640 (Carlsbad, California, USA) and divided into the following groups: without adding any compound (control group), adding 100 nM glucagon-like peptide-1 (GLP-1 group) , adding 10 μg / mL peptide 1 group, peptide 12 group, peptide 16 group, see Table 11 below.

[0186] Table 11

[0187]

[0188]

[0189] in CO 2 / O 2 (5 / 95%), 37 ℃ enviro...

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Abstract

The invention provides a polypeptide and aims to solve the problems of short half life of plasma and low activity of insulinotropic nascent polypeptides in the prior art. The polypeptide has a sequence of Ac-IGLHDPSHGTLPNGS-OH (No.16), Ac-IGLHDPSHGTLPNGS-NH2 (No.31) or Ac-IGLHDPSHGTLPNGSC-OH (No.34). In addition, the invention further discloses a derivative of the polypeptide, a pharmaceutical salt of the polypeptide, a pharmaceutical composition and application of the polypeptide or the derivative of the polypeptide. The polypeptide provided by the invention is highly stable in blood and has long half life.

Description

[0001] This application is based on the Chinese patent application (application number CN201410096370.X, titled a polypeptide, a polypeptide derivative, a pharmaceutically acceptable salt of a polypeptide, and a pharmaceutical composition) submitted on March 14, 2014 as the parent case. Divisional application. The parent case is based on an earlier PCT international application (application number PCT / CN2013 / 072771) filed on March 15, 2013, and claims priority from it. 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, pharmaceutical compositions and applications thereof. 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 pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/47A61K38/17A61P3/10A61P1/16A61P25/00A61P29/00C12N5/071C12N5/079
CPCC07K14/47A61K38/00C12N5/0613C12N5/0618C12N5/067
Inventor 刘利平白茹
Owner SHENZHEN HIGHTIDE BIOPHARM
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