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A radioactive iodine-labeled protein-binding ligand and its application

A technology of radioactive iodine and protein, which is applied in the direction of radioactive carriers, in vivo radioactive preparations, preparations for in vivo experiments, etc., can solve the problems that proteins are easy to be polluted, easily affected by other factors, and complicated preparation methods, so as to improve pharmacokinetics The effects of biological properties, prolonged blood half-life, and simple labeling method

Active Publication Date: 2020-12-18
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the drugs for the diagnosis and treatment of cardiovascular diseases have the following problems: such as short blood half-life, fast renal clearance rate, easy to be excreted from the body, making it necessary to use high doses or frequent administration, etc., which will inevitably produces a series of toxic and side effects, thus limiting its use
Although it is a relatively mature method to directly label albumin with radionuclides in vitro, it is a human extract, which is expensive and may cause immune rejection when injected into the body, and the protein is easily contaminated and denatured. Limit its application on
It can be seen that the existing relatively successful serum albumin labeling methods still have disadvantages such as complicated preparation methods, high prices, easy virus infection, and easily affected imaging effects by other factors. Radioactive markers with low cost and good effect that can effectively bind to albumin will have broad application prospects

Method used

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  • A radioactive iodine-labeled protein-binding ligand and its application
  • A radioactive iodine-labeled protein-binding ligand and its application
  • A radioactive iodine-labeled protein-binding ligand and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 1.4-[ 131 I] Synthesis of IBA-NHS

[0044] Dissolve 1 g of 4-[(4-boronic acid phenyl) butyric acid (4-BBA) in 15 mL of DMF, add 981 mg of dicyclohexylcarbodiimide and 548 mg of N-hydroxysuccinimide, and stir at room temperature overnight . By-products were removed by filtration, and the filtrate was concentrated to obtain a white solid powder, the activated ester of 4-[(4-boronic acid phenyl)butanoic acid;

[0045] Take 1 mg of the activated ester (4-BBA-NHS) of 4-[(4-boronic acid phenyl) butyric acid, and add 50 μL of the catalyst of cuprous oxide and 1,10-phenanthroline mixed uniformly; add the above solution Into the air-dried radioactive iodine, shaking and reacting at room temperature for 30min, the labeled product 4-[ 131 I] IBA-NHS; add appropriate amount of Na 2 CO 3 It is hydrolyzed to obtain the target product 4-[ 131 I] IBA. The labeled final product was identified by HPLC, and its radioactive peak time could be compared with that of the stable albumin...

Embodiment 2

[0052] The following is the marker 4-[ 131 I] IBA, 4-[ 131 I]IBA-PEG or 4-[ 131 I] The performance measurement description of IBA-FA:

[0053] 1. Analysis and identification by TLC and HPLC

[0054] 4-[ 131 I] the TLC analysis system of IBA is as follows: sherwood oil: the system of ethyl acetate=1: 1 measures TLC to analyze with silica gel aluminum plate respectively at different time points; The system of physiological saline measures with polyamide film respectively at different time points TLC for analysis. 4-[ 131 I] the labeling rate of IBA is faster, has exceeded 99% in 10min; The radiochemical purity is high, greater than 95%; Stable in nature and difficult to decompose, until 24h it still exists stably in normal saline and acetonitrile solvent, TLC shows only A single peak appears, resulting in figure 1 shown.

[0055] 4-[ 131 I] The HPLC analysis system of IBA is as follows: Perkin-Elmer Series 200LC is equipped with Waters 2784 double absorption wavelength ...

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Abstract

The invention discloses a radioactive iodine marked protein binding ligand and application thereof. A structural formula of the radioactive iodine marked protein binding ligand is shown in a followingimage, wherein the I is radioactive iodine nuclide, the R is OH or derived from PEG, folic acid, RGD, octreotide, epidermal growth factor, protein, nucleic acid or polysaccharide. The radioactive iodine marked protein binding ligand disclosed by the invention has the advantages of simple marking method, low cost and good stability. Animal live test results show that the albumin binding ligand hashigher uptake and longer-time retention in blood and further has a higher target / non-target specific value. When the radioactive iodine marked protein binding ligand is modified to a target group orother functional groups, pharmacokinetic characters of compound can be obviously improved, a blood half-life period of the compound is prolonged, and the compound is suitable for being utilized as a blood pool, lymph and tumor diagnosing and treating reagent.

Description

technical field [0001] The invention belongs to the technical field of diagnostic reagents, and in particular relates to a radioactive iodine-labeled protein-binding ligand and an application thereof. Background technique [0002] Molecular imaging is known as medical imaging in the 21st century, because it can provide a strong guarantee for early detection, early diagnosis and early treatment of diseases. On the one hand, the development of imaging equipment has promoted the realization of early diagnosis and treatment of diseases; on the other hand, the development of non-invasive probes with good targeting, strong specificity and high sensitivity has become a key element of molecular imaging. Only by obtaining probes with good performance can we better diagnose and treat diseases and evaluate the prognosis. [0003] In recent years, cardiovascular system diseases and malignant tumors have seriously affected human health, and they have ranked the top two in the world's po...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04A61K51/06C07D475/04C07C51/00C07C57/58C08G65/337A61K101/02
CPCA61K51/0459A61K51/06C07C57/58C07D475/04C08G65/337
Inventor 张现忠文雪君郭志德张蒲石昌荣李进典许多
Owner XIAMEN UNIV
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