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Compound for inhibiting aggregation of amyloid polypeptide as well as preparation method and application thereof

A technology of amyloid polypeptide and complex, applied in the field of biomedicine

Inactive Publication Date: 2014-01-29
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Several methods for inhibiting the toxicity of amyloid peptides reported above are all from the perspective of synthesizing short peptide inhibitors to achieve the effect of regulating the aggregation of amyloid peptides and inhibiting neurotoxicity. At present, no short peptides have been prepared by using non-covalent bonds. Peptide Inhibitor Approach

Method used

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  • Compound for inhibiting aggregation of amyloid polypeptide as well as preparation method and application thereof
  • Compound for inhibiting aggregation of amyloid polypeptide as well as preparation method and application thereof
  • Compound for inhibiting aggregation of amyloid polypeptide as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] Example 1 Based on scanning probe microscopy to observe the assembly structure of short peptide inhibitors and the regulation of adjuvant 1 on the assembly structure of short peptide inhibitors

[0141] 1. The chemical structure of the substance used

[0142] Short peptide inhibitor (Aβ16-20 (SEQ ID NO:1), Shanghai Keyept Biotechnology Co., Ltd., with a purity of 98%) and adjuvant 1 (4'-chloro-2,2':6',2”-terpyridine , Acros), as shown in the following formula:

[0143]

[0144] Short Peptide Inhibitor, β-Amyloid Peptide 16-20 (Aβ16-20)

[0145]

[0146] Adjuvant 1, (4’-chloro-2,2’:6’,2”-terpyridine)

[0147] 2. Specific method

[0148] 1) Scanning tunneling microscopy was used to detect the assembly structure of the short peptide inhibitor Aβ16-20 and the regulation of adjuvant 1 on the assembly structure of the short peptide inhibitor Aβ16-20.

[0149] First, mix the short peptide inhibitor (Aβ16-20) and pyridine adjuvant 1 () in the aqueous solution, ultra...

Embodiment 2

[0165] Example 2 Detection of neurotoxicity of amyloid polypeptide Aβ1-42 and inhibition of amyloid polypeptide neurotoxicity by adjuvant 1, short peptide inhibitor, inhibitor-adjuvant 1 complex using neurocytotoxicity test method

[0166] SH-SY5Y cells (ECACC, UK) were seeded in 96-well plates (purchased from Greiner Bio-One Inc., Longwood, FL, USA), 100 μL of cell culture medium per well, and cultured in an incubator at 37°C. When about 40% of the cells adhere to the wall and are in good condition, add amyloid peptide, adjuvant 1, short peptide inhibitor, inhibitor-adjuvant 1 complex and amyloid peptide with their respective The mixed system was tested for cytotoxicity, and the cell concentration was 10,000 cells / well.

[0167] Aβ1-42, Aβ1-42 / Aβ16-20 / 4'-chloro-2,2':6',2"-tripyridine, Aβ16-20, 4'-chloro-2,2':6',2 "-tripyridine, Aβ16-20 / 4'-chloro-2,2':6',2"-tripyridine were added to the cell culture medium, and the final concentrations were as follows: Aβ1-42: 10 μM; Aβ1-42...

Embodiment 3

[0173] Example 3 Observation of short peptide inhibitors, polyphenol adjuvants, and inhibitor-polyphenol adjuvant complexes in solution based on ThT fluorescence spectrum to observe the regulation effect of amyloid polypeptide Aβ1-42 aggregation kinetics

[0174]Disperse amyloid peptide Aβ1-42 and short peptide inhibitor Aβ16-20 with hexafluoroethylenepropanol in advance to make the concentration 1mg / mL, prepare 1mM ThT solution with 10mM phosphate buffer solution, and prepare 100mM EGCG as adjuvant with DMSO. agent solution. The inhibitor-EGCG complex was prepared 1 hour in advance with a concentration ratio of 1.25mM:1.25mM. Take 79 μL of 1 mg / mL amyloid peptide Aβ1-42 dispersed in hexafluoroethylenepropanol and place them in four 0.6mL centrifuge tubes, numbered A (62.5μM Aβ1-42), B (62.5μM Aβ1-42 / 125μM short Peptide inhibitor), C (62.5 μM Aβ1-42 / 125 μM adjuvant 2), D (62.5 μM Aβ1-42 / 125 μM inhibitor-adjuvant 2 complex), vacuum-dry at room temperature for 30 min, add 0.5...

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Abstract

The invention discloses a compound for inhibiting aggregation of amyloid polypeptide as well as a preparation method and application thereof. The compound is prepared from a short peptide inhibitor and an adjuvant according to a molar ratio of (1:5) to (10:1), wherein the short peptide inhibitor is selected from segments of 3-10 amino acids of beta-amyloid polypeptide, mutants and derivatives thereof; the adjuvant is selected from a nitrogenous heterocyclic compound and derivatives thereof; according to the compound, the short peptide inhibitor and the adjuvant are dissolved into a buffer solution according to the molar ratio of (1:5) to (10:1), so as to prepare a mixed solution; the final concentration of the short peptide inhibitor is 10-100 muM; the compound is prepared in an incubation manner; the compound is used for preparing a drug for inhibiting the toxic action of the amyloid polypeptide on a cell or used for preparing a drug for treating and / or preventing a disease associated with the amyloid polypeptide. The invention discloses interaction of molecules and the amyloid polypeptide in the molecular level; an effective method is provided for research on an interaction mechanism of drug molecules and the amyloid polypeptide.

Description

[0001] This application claims the priority of the patent application for invention filed on July 16, 2012, entitled "Complex for Inhibiting Aggregation of Amyloid Polypeptide and Its Preparation Method and Application", with application number 201210246344.1. technical field [0002] The invention belongs to the technical field of biomedicine. The present invention generally relates to a compound, in particular to a compound for inhibiting aggregation of amyloid polypeptide. The invention also relates to the preparation method and application of the complex for inhibiting amyloid polypeptide aggregation. The compound for inhibiting amyloid polypeptide aggregation of the present invention can greatly improve the inhibitory effect on the aggregation and toxicity of amyloid polypeptide. Background technique [0003] The misfolding and abnormal assembly behavior of amyloid peptides are closely related to the pathogenesis of many human degenerative diseases, such as Alzheimer's...

Claims

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Application Information

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IPC IPC(8): A61K38/06A61K38/07A61K38/08A61P25/28A61P25/14A61P25/16A61P25/00A61P3/10A61K31/353A61K31/05A61K31/352A61K31/12A61K31/444
Inventor 杨延莲牛琳王琛刘磊赵琼徐萌
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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