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Peptide, peptide derivatives, medicinal salts of peptide, medicine composition and application of peptide and peptide derivatives

A technology of peptide derivatives and compositions, which is applied in the field of polypeptides and their derivatives, pharmaceutically acceptable salts and pharmaceutical compositions, can solve the problems of short plasma half-life, achieve long plasma half-life, good stability, and improve pancreatic islet The effect of the function

Inactive Publication Date: 2015-05-27
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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  • Peptide, peptide derivatives, medicinal salts of peptide, medicine composition and application of peptide and peptide derivatives
  • Peptide, peptide derivatives, medicinal salts of peptide, medicine composition and application of peptide and peptide derivatives
  • Peptide, peptide derivatives, medicinal salts of peptide, medicine composition and application of peptide and peptide derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0132] Example 1 Production of Polypeptides

[0133] This example describes the production of polypeptides

[0134] 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 DMF solu...

Embodiment 2

[0138] Embodiment 2 Stability experiment of peptide

[0139] This example describes stability experiments of peptides under various conditions.

[0140] 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.

[0141] 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

[0168] Example 3 Effect of Peptides on Glucose-Stimulated Insulin Secretion

[0169] This example describes the effect of peptides on glucose-stimulated insulin secretion (GSIS).

[0170] 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% (vol / vol) 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 10 below.

[0171] Table 10

[0172]

[0173]

[0174] in CO 2 / O 2 (5 / 95%), 37 ℃ envi...

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Abstract

The invention provides a peptide to solve the problems of shorter plasma half-lives and lower activities of insulinotropic nascent peptides in the prior art. The peptide has a sequence as follows: Ac-IGLHDPSHGTLPAGS-OH (No.12), Ac-IGLHDPSHGTLPAGS-NH2 (No.29) or Ac-IGLHDPSHGTLPAGSC-OH (No.43). Meanwhile, the invention also discloses peptide derivatives, medicinal salts of the peptide, a medicine composition and an application of the peptide and the peptide derivatives. The peptide provided by the invention has high stability and long half-life in blood.

Description

[0001] This application is based on the Chinese patent application (application number CN201410096363.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 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 p...

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
CPCC07K14/4713A61K38/00C12N5/0619C12N5/067C12N5/0676
Inventor 刘利平白茹
Owner SHENZHEN HIGHTIDE BIOPHARM
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