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Anti-inflammatory hexapeptide

An anti-inflammatory drug and inflammatory technology, applied in the field of preparation and application of anti-inflammatory hexapeptide, can solve problems such as physiological dysfunction

Inactive Publication Date: 2011-02-16
THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as we all know, the application of NF-κB antagonists must face the following unavoidable problems: ①Safety: Since NF-κB is distributed in all cells in the body, indiscriminate inhibition of its activity will lead to extensive physiological dysfunction

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The operating steps of embodiment 1, Lys Val Cit Lys Pro Val preparation method

[0023]The main operation steps of solid-phase peptide synthesis are as follows: 1. Resin swelling: Put Wang-Resin resin into a reaction tube, add DMF (15ml / g) for 30min. 2. Deprotection: remove DMF, add 20% piperidine DMF solution (15ml / g) for 5min, remove and add 20% piperidine DMF solution (15ml / g) for 15min. 3. Detection: Take out the piperidine solution, take more than a dozen resins, wash them three times with ethanol, add ninhydrin, KCN, and phenol solution one drop each, heat at 105°C-110°C for 5 minutes, and turn dark blue to indicate a positive reaction. 4. Washing: DMF (10ml / g) twice, methanol (10ml / g) twice, DMF (10ml / g) twice. 5. Condensation: Add a three-fold excess of protected amino acids and a three-fold excess of activator HBTU, dissolve them with as little DMF as possible, add to a reaction tube, immediately add a ten-fold excess of NMM, and react for 30 minutes. 6. W...

Embodiment 2

[0024] Example 2, the effect of anti-inflammatory hexapeptide on the secretion of inflammatory factors in mouse peritoneal macrophages

[0025] Take about 20 grams of female C57BL / 6 mice, routinely lavage out peritoneal macrophages, and use 1×10 6 The amount of cells per well is added to a 24-well culture plate, and endotoxin (LPS) 1 μg / ml is added to act for 24 hours. At the same time, peptides of different concentrations in different groups are added, and the supernatant is collected to measure inflammatory factors such as tumor necrosis with ELISA kits. factor (TNF-α), interleukin Level.

[0026] The results show that the polypeptide of the present invention (positive peptide 1) can inhibit the secretion of inflammatory factors stimulated by endotoxin in peritoneal macrophages, and the inhibitory effect has a dose-effect relationship, and the intensity of this action is significantly higher than that of the positive peptide 2 group (sequence: Lys(D-Pro)ValCit); while t...

Embodiment 3

[0027] Example 3, Zymosan A-induced mouse foot plantar inflammation and therapeutic effect of anti-inflammatory hexapeptide

[0028] About 20 grams of female C57BL / 6 mice were taken and randomly divided into control group, inflammatory group and different treatment groups, with 5 mice in each group. Zymosan A (15 mg / ml) was injected into the 50 μl of both hindlimbs of the inflammation group and the treatment group, and the same dose of saline was injected into the corresponding parts of the control group. The day of injection was defined as day 0, and on the second day, dexamethasone injection (750 μmol / L) and polypeptide injection (75 μmol / L) were applied to the treatment group once, 50 μl / foot, and the mouse paws were dynamically measured during the observation period. volume.

[0029] The results show that inflammation and swelling of the sole of the foot occurs in the inflammatory group, and the polypeptide of the present invention (positive peptide 1) can effectively r...

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Abstract

The invention relates to anti-inflammatory hexapeptide Lys, Val, Cit Lys Pro Val as well as preparation and application thereof. The invention also comprises a method for preparing the polypeptide. The method is selected from the conventional solid phase synthesis method, a synthesis method in a solution, a gene recombination method or a chemical synthesis method. The medicament is used for treating inflammatory immune relevant diseases, wherein the inflammatory relevant diseases comprise sepsis, septic shock, rheumatoid (rheumatoid) arthritis, asthma, acute and chronic glomerulonephritis, systemic lupus erythematosus, and the like.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a hexapeptide molecule Lys Val Cit Lys Pro Val capable of inhibiting the secretion of inflammatory factors, and also relates to the preparation and application of the anti-inflammatory hexapeptide. Background technique [0002] Since nuclear factor-κB (nuclear factor-κB, NF-κB) was accidentally discovered in 1986, its importance has been increasingly concerned and has become one of the most active research fields. Typical NF-κB is a heterodimer formed by two subunits of polypeptide chain p50 and p65. When cells are in a resting state, NF-κB mainly combines with κB inhibitory proteins (IκBs, of which IκBα and IκBβ play an important role) to form a trimer, which exists in the cytoplasm in an inactive manner; when cells are subjected to various When external signals (such as inflammatory stimuli, carcinogens, ionizing radiation, growth factors and other stressors, etc.) are stimulated to ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61P13/12A61P29/00A61P19/02A61P19/04A61P11/06A61P31/00C07K7/06A61P37/02
Inventor 梁华平范霞张醇王希杨雪
Owner THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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