Preparation method of colon cancer nuclear magnetic resonance multifunctional contrast agent

A nuclear magnetic resonance, multi-functional technology, which is applied in the field of preparation of multi-functional contrast agents for colon cancer nuclear magnetic resonance, can solve the problems of difficulty in early diagnosis of tumors, low sensitivity, and non-specificity of contrast agents.

Active Publication Date: 2015-12-09
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the inherent low sensitivity of magnetic resonance imaging and the non-specificity of contrast agents, early diagnosis of tumors is difficult.

Method used

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  • Preparation method of colon cancer nuclear magnetic resonance multifunctional contrast agent
  • Preparation method of colon cancer nuclear magnetic resonance multifunctional contrast agent
  • Preparation method of colon cancer nuclear magnetic resonance multifunctional contrast agent

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Example 1 Synthesis of multifunctional contrast agent SPIO-TCP-1-Cy5.5

[0024] (1) Synthesis of Alkyne-modified TCP-1-Cy5.5

[0025] a) Using Fmoc chemical solid-phase peptide synthesis, the swelling property is very good Resin, complete the peptide sequence with a 5-fold excess of Fmoc-protected amino acids and condensation reagent (HBTU / HOBt).

[0026] b) The side chain Mtt-protected lysine (K) was selectively deprotected with 1% trifluoroacetic acid (TFA), Cy5.5freeacid, EDC and HOBt were added as condensation reagents, and Cy5.5 was reacted overnight at room temperature.

[0027] c) Deprotect the N-terminus of the polypeptide with 20% piperidine, add propiolic acid, and use N,N'-diisopropylcarbodiimide (DIC) as a condensation reagent to modify the N-terminus as Alkynes.

[0028] d) Cleave the peptide from the resin with 95% TFA (and a free radical scavenger), precipitate with ether, and analyze and purify the crude peptide obtained by C18 reverse-phase high-p...

Embodiment 2

[0037] Example 2 Synthesis of multifunctional contrast agent SPIO-TCP-1-ATTO590

[0038] The synthesis steps were the same as in Example 1, the fluorescent dye was ATTO590, and a new multifunctional contrast agent SPIO-TCP-1-ATTO590 was obtained.

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Abstract

The invention discloses a preparation method of a colon cancer nuclear magnetic resonance multifunctional contrast agent. Colon cancer tumor targeting peptides (TCP-1) marked with dyes are combined with magnetic nanometer carriers; on one hand, the TCP-1 is specifically marked with the organic dyes Cy5.5, the N terminal is decorated with alkynyl, and then the TCP-1-Cy5.5 marked with alkynyl is synthesized; on the other hand, uniform ferric oxide nanometer particles (Azide-SPIO) decorated with azide are synthesized; finally, the multifunctional contrast agent (SPIO-TCP-1-Cy5.5) is prepared by coupling the TCP-1-Cy5.5 with the Azide-SPIO through click chemistry. The novel contrast agent for early diagnosis of colon cancer is developed, the nanometer particles are introduced to be specifically combined with and enter new blood vessel cells of tumor through the TCP-1, and the early tumor detection on the scale of few millimeters can be achieved by combining magnetic resonance imaging with far infrared fluorescence imaging.

Description

technical field [0001] The invention belongs to the technical field of nano-biomedicine, and relates to the preparation of a colon cancer nuclear magnetic resonance multifunctional contrast agent, in particular to a combination of a TCP-1 polypeptide with colon cancer tumor recognition function and magnetic iron oxide nanoparticles to prepare a A novel multifunctional tumor molecular imaging probe aimed at providing a non-invasive and sensitive T2 contrast agent for early diagnosis of colon cancer. Background technique [0002] In recent years, contrast agent-assisted magnetic resonance imaging is currently one of the best methods for tumor diagnosis. However, due to the inherent low sensitivity of MRI and the non-specificity of contrast agents, early diagnosis of tumors is difficult. Over the past 20 years, various inorganic materials have been developed as contrast agents. Among many nanomaterials, magnetic nanoparticles have become one of the most successful nanomateria...

Claims

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Application Information

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IPC IPC(8): A61K49/14
Inventor 王建浩李进晨柳丽蒋鹏举邱琳杨丽樊杰程永江吴昊董冰玉孙凯谢雨佳蒋雨
Owner CHANGZHOU UNIV
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