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Polypeptide crossing blood-brain barrier as well as derivative and application thereof

A blood-brain barrier and derivative technology, applied in the field of medical biology, can solve limited problems and achieve the effects of broad application prospects, enhanced targeting and therapeutic properties, and easy synthesis and modification.

Pending Publication Date: 2022-04-08
SHENZHEN INST OF ADVANCED TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as of now, the research on mediating ligands is still very limited, and there are few available mediating ligands.

Method used

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  • Polypeptide crossing blood-brain barrier as well as derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Preparation of polypeptide sequences across the blood-brain barrier

[0047] Synthesize the polypeptide sequence across the blood-brain barrier by artificial synthesis method,

[0048] The polypeptide sequence is as follows:

[0049] YLGASVPSPDPLEPT SEQ ID No. 1;

[0050] YLGASVPSPDPLEPTREQCELNPACDELSDQYGLKTAYKRIYGITI SEQ ID No. 2;

[0051] YLYQWLGAPVPYPDPLEPR SEQ ID No. 3;

[0052] YLYQWLGAPVPYPDPLEPREVCELNPDCDELADHIGFQEAYRRFYGPV SEQ ID No. 4.

[0053] The above-mentioned polypeptides are synthesized by conventional solid-phase synthesis or liquid-phase synthesis methods. Among them, the solid-phase synthetic peptide method is used to react from the amino acid at the C-terminal to the N-terminal. After the steps of resin activation, amino acid linkage, elution protection, and detection, the amino acid linkage is completed one by one, and then precipitated and centrifuged with excess ether, and the crude peptide is purified by HPLC. Afterwards, mass spec...

Embodiment 2

[0055] Example 2: Preparation of polypeptide probes across the blood-brain barrier

[0056] This embodiment provides a polypeptide probe, using the polypeptide prepared in Example 1, and combining it with ICG through an organic chemical reaction.

[0057] The specific method is purchase or synthesis. In this example, the probe is prepared by linking the polypeptide with ICG by click chemistry method, and the linker is the common DBCO. ICG with an activating functional group containing the amino group NH2 , carboxyl COOH, activated lipid NHS, maleimide MAL, mercapto SH, azide N 3 , alkyne ALK, and then coupled with the polypeptide prepared in Example 1 to obtain the blood-brain barrier polypeptide ICG probe.

Embodiment 3

[0058] Example 3: Detection of the ability of mice to cross the blood-brain barrier

[0059] Adult mice were used, and the cross-blood-brain barrier polypeptide ICG probe (containing SEQ ID NO.1) prepared in Example 2, ICG solution (2mM) and PBS were injected into the tail vein, and each mouse was injected with 100 microliters. After 24 hours, Detection under small animal imager.

[0060] See the experimental results figure 1 , by comparing the results of the three groups, it can be seen that only the cross-blood-brain barrier polypeptide probe group has specific signals in the brain, while the other two groups do not show fluorescent signals in the brain. From the above experimental results, it can be seen that the blood-brain barrier-crossing polypeptide probe of the present invention can realize the effect of crossing the blood-brain barrier. Promote the transport efficiency across the blood-brain barrier, and then realize the transport of other active ingredients.

[00...

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Abstract

The invention discloses a cross-blood-brain-barrier polypeptide as well as a derivative and application thereof, and belongs to the field of biological medicines. The invention specifically discloses application of polypeptide in preparation of a medicine or a detection reagent crossing a blood-brain barrier. The polypeptide is selected from metabonotin or osteocalcin. The invention also discloses a derivative, and the derivative is a product obtained by modifying the tail end or the side chain of polypeptide or a product obtained by performing isotope labeling modification. The polypeptide molecule can enter brain tissues across the blood-brain barrier, a specific blood-brain barrier crossing tool is provided for diagnosis and treatment of brain diseases, and the polypeptide molecule can be used for preparing detection reagents and blood-brain barrier crossing drugs.

Description

technical field [0001] The invention belongs to the field of medical biology, and relates to a blood-brain barrier crossing polypeptide, derivatives and applications thereof. Background technique [0002] The blood-brain barrier is an important structure to ensure the development and normal function of the nervous system. It not only protects the brain from external interference, but also restricts the delivery and transport of a large number of valuable drugs. It is known that except for some small molecules that can cross the blood-brain barrier, the transport of most macromolecules needs to be mediated by receptors. With the help of endogenous receptors, macromolecular drugs can be delivered to the brain Internally, drug delivery is achieved. However, so far, the research on mediating ligands is still very limited, and there are very few mediating ligands available. The discovery of such ligands is also something that can be encountered but not sought after, which is al...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/64A61K49/00C07K14/435C07K14/795
CPCA61K49/00A61K47/42A61K47/64C07K14/795C07K14/435
Inventor 赵华山朱雯张键任培根雷晓华
Owner SHENZHEN INST OF ADVANCED TECH
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