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Supermolecule precursor, supermolecule assembly and method for regulating and controlling macrophage polarization

A technology of supramolecular assemblies and macrophages, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and drug combinations, etc. effect of effect

Pending Publication Date: 2021-03-23
WUHAN ENG SCI & TECH RESINST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is difficult for miRNA to exist stably in body fluids, and it can only achieve low-level expression in all major organs, which in turn leads to its poor ability to regulate the polarization of macrophages

Method used

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  • Supermolecule precursor, supermolecule assembly and method for regulating and controlling macrophage polarization
  • Supermolecule precursor, supermolecule assembly and method for regulating and controlling macrophage polarization
  • Supermolecule precursor, supermolecule assembly and method for regulating and controlling macrophage polarization

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preparation example Construction

[0048] The embodiment of the present invention also provides a preparation method of the aforementioned supramolecular precursor for regulating macrophage polarization, including:

[0049] S1. Synthesis of mono-[6-deoxy-p-toluenesulfonyl]-cyclodextrin (number: 6-OTs-CD)

[0050] First, recrystallize cyclodextrin (abbreviation: CD) with boiling water, take CD and disperse it in water to form a dispersion liquid, dissolve alkaline substances, such as sodium hydroxide, etc. in water and slowly drop them into the above dispersion liquid. Weigh p-toluenesulfonyl chloride and dissolve it in acetonitrile. After the above dispersion becomes clear, add it dropwise to the dispersion in an ice-water mixing bath (around 0°C), and keep this process for more than 30 minutes. Afterwards, continue to react at room temperature (about 25°C) for 2 hours, remove the insoluble matter after the reaction by suction filtration, then place at 0-4°C overnight, filter with suction, wash with a small amo...

Embodiment 1

[0068] An embodiment of the present invention provides a supramolecular precursor that regulates the polarization of macrophages, which includes polyethyleneimine-β-cyclodextrin and adamantane-polyethylene glycol-adiponectin, the two of which interact through host-guest carry out the load.

[0069] This embodiment also provides a preparation method of a supramolecular precursor that regulates macrophage polarization, including:

[0070] S1. Synthesis of mono-[6-deoxy-p-toluenesulfonyl]-β-cyclodextrin (number: 6-OTs-β-CD)

[0071] First, use boiling water to recrystallize β-CD twice, take 15.00g (13.2mmol) β-CD and disperse evenly in 125mL water to form a dispersion liquid, dissolve 1.64g (41mmol) sodium hydroxide in 5mL water and slowly add it dropwise to the above dispersion in the liquid. Weigh 2.52g (13.2mmol) of p-toluenesulfonyl chloride and dissolve it in 7.5mL of acetonitrile. After the above dispersion becomes clear, add it dropwise to the β-CD solution in an ice-wat...

Embodiment 2

[0084] This embodiment also provides a supramolecular assembly for regulating macrophage polarization, which includes miRNA and the supramolecular precursor for regulating macrophage polarization provided in Example 1. The supramolecular precursor is wrapped by positive and negative charges outside the miRNA.

[0085] The embodiment also provides a method for preparing a supramolecular assembly that regulates macrophage polarization, including:

[0086] The mixed solution prepared in Example 1 was mixed with an equal volume of miRNA, and N / P=10, and incubated at 4° C. for 2 hours to obtain a supramolecular assembly (coded as PEI-CD / AD-SS-PEG-GAD / miRNA).

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Abstract

The invention relates to the technical field of chemical medicines, in particular to a supermolecule precursor, a supermolecule assembly and a method for regulating and controlling macrophage polarization. The supermolecule precursor comprises polycation modified by cyclodextrin, and adamantine-polyethylene glycol-active polypeptide loaded to the polycation modified by cyclodextrin, wherein an active peptide raw material for forming the adamantine-polyethylene glycol-active polypeptide can be the polypeptide capable of regulating and controlling the macrophage polarization. The supermolecule precursor can effectively regulate and control polarization from macrophage to M2 macrophage, meanwhile, the supermolecule precursor can load RNA, and therefore, the supermolecule assembly can furtherregulate and control the macrophage polarization so as to accelerate the macrophage to be converted into the M2 macrophage.

Description

technical field [0001] The invention relates to the technical field of chemical medicines, in particular to a supramolecular precursor, a supramolecular assembly and a method for regulating macrophage polarization. Background technique [0002] Cardiovascular disease (CVD) is a serious disease that seriously endangers human health and life. Worldwide, about 16.7 million people die from CVD every year, accounting for the first in the global mortality rate, and atherosclerosis (AS) is an important pathological basis for the occurrence and development of CVD. Medical research shows that the change in function of macrophages plays an important role in the occurrence of AS, becoming the first inflammatory cell associated with AS. Monocytes and macrophages have become the focus of researchers because of their strong plasticity in function. Macrophages can differentiate into M1 and M2 phenotype macrophages under different in vivo and in vitro local microenvironments. M1 macropha...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/7088A61K38/17A61K47/54A61K47/60A61K47/61A61P9/10A61P29/00B82Y5/00
CPCA61K38/1709A61K31/7088A61K47/60A61K47/54A61K47/61A61K47/6935A61P9/10A61P29/00B82Y5/00A61K2300/00
Inventor 李文宇
Owner WUHAN ENG SCI & TECH RESINST
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