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A conjugate capable of passing through the blood labyrinth barrier and its preparation method

A conjugate and conjugation technology, applied in the field of conjugates that can pass through the blood labyrinth barrier and its preparation, can solve the problems of surgical prophylactic administration, inconvenience and high risk of multiple medications, and achieve a good inner ear target Effect of direction and enrichment function, treatment of neurological deafness

Active Publication Date: 2022-06-03
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this barrier system necessary to ensure the special functions of the inner ear has also become an important obstacle to restrict the entry of drug molecules into the inner ear and treat related diseases. Therefore, a series of inner ear diseases related to hearing and balance medicine, including deafness, tinnitus, and vertigo, are worldwide. Difficult diseases, currently there is no practical and effective inner ear drug delivery method except surgery, and surgery has many inconveniences in preventive drug administration and multiple drug use, and the risk is relatively high

Method used

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  • A conjugate capable of passing through the blood labyrinth barrier and its preparation method
  • A conjugate capable of passing through the blood labyrinth barrier and its preparation method
  • A conjugate capable of passing through the blood labyrinth barrier and its preparation method

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] X is a random amino acid.

[0078] Library1

[0081] The restriction sites are underlined, and the capital letters are the nucleic acid sequences encoding the peptide library.

[0084] The primer cross-primer synthesis company synthesized.

[0087]

[0089]

[0090] The expansion target fragment is about 100bp, and the Tiangen PCR purification and recovery kit reclaims the PCR product. Determination of recovered products

[0092] Enzymatic digestion reclaimed the PMESY 4-plasmid, the PCR target fragment.

[0094]

[0095] Run 1% agarose gel, and cut the gel to recover the plasmid fragment cut by the enzyme.

[0099]

[0100] At 16°C overnight, the ligation product was recovered according to the product recovery kit, and eluted with ultrapure water at 70°C.

[0104] (2) The Escherichia coli liquid was centrifuged at 4° C. and 4000 rpm for 10 min, and the supernatant was discarded.

[0106] (4) Repeat step (3) 1 time.

[0110] The electric rotor cup was pre-cooled on ice for ...

Embodiment 3

[0127] The detection results of label-free polypeptide mass spectrometry are shown in Figure 3. The molecular weight of the peptide is 1027.86*2‑2=2053.6, the molecular weight

[0128] The detection result of CY5.5 fluorescent polypeptide mass spectrometry is shown in Figure 4. CY5.5 labeled with fluorescent molecular weight 873.22*3‑

[0130] Linked fluorescent molecular peptides were used for subsequent in vivo detection in mice. Accurately weigh the short peptide, dissolve it with normal saline,

[0131] At 4 h of tail vein injection, M1-CY5.5 was clearly observed to be enriched in the brain. Take the mouse, the speed of 5ml / min

Embodiment 4

[0134]

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PUM

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Abstract

The invention relates to a conjugate capable of passing through the blood labyrinth barrier and a preparation method thereof. The conjugate is formed by coupling a peptide and an active molecule having inner ear diagnostic or therapeutic activity. The peptide has the following general structural formula TFYGGRX1KRNNFX2X3X4X5X6X7 . The conjugate can be administered through intravenous infusion, and can carry active molecules into the inner ear non-invasively, breaking through the technical bottleneck that drugs are difficult to enter the inner ear in the prior art. The present invention also specifically provides a peptide-curcumin compound, whose inner ear targeting function has been verified at the animal experiment level, which can effectively cross the labyrinth barrier of the inner ear of mice, treat neurological deafness, and protect hearing after noise exposure effect.

Description

A conjugate that can pass through the blood labyrinth barrier and its preparation method technical field The present invention relates to bioengineering and medical technology field, be specifically related to a kind of conjugate that can pass through blood labyrinth barrier and its preparation method. Background technique Human ear anatomy is mainly divided into outer ear, middle ear and inner ear, wherein inner ear is relatively closed and the structure is extremely complex It is one of the most sophisticated sensory organs in the human body, and its internal complex membrane labyrinth system It is filled with two kinds of lymph fluids with different ion concentrations, inside and outside, which circulate independently in order to perform acoustoelectric conversion for hair cells. The necessary potential difference is provided to generate an action potential. In order to ensure the normal operation of this mechanism, the inner ear lymphatic system and peripheral b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/64A61K31/12A61K45/00A61K49/14A61P27/16C07K7/08C07K14/00C07K1/107
CPCA61K47/64A61K31/12A61K45/00A61K49/14A61P27/16C07K7/08C07K14/001
Inventor 林坚时晰陈龙
Owner PEKING UNIV