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Method for rapidly marking Cys-Annexin V through <18>F and application of method

A 18f-al-nota-cys-annexinv and labeling technology, applied in the field of PET imaging, can solve the problems of low efficiency, long labeling time, and low labeling rate, so as to solve the problems of low labeling rate, improve labeling rate, and shorten labeling the effect of time

Active Publication Date: 2016-06-15
JIANGSU INST OF NUCLEAR MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Therefore, the technical problem to be solved in the present invention is to overcome the problems in the prior art 18 F positioning marker Cys-AnnexinV has the defects of low labeling rate, long labeling time and low efficiency, thus providing a high labeling rate, short labeling time and high efficiency 18 The method and application of fast labeling Cys-AnnexinV

Method used

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  • Method for rapidly marking Cys-Annexin V through &lt;18&gt;F and application of method
  • Method for rapidly marking Cys-Annexin V through &lt;18&gt;F and application of method
  • Method for rapidly marking Cys-Annexin V through &lt;18&gt;F and application of method

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Experimental program
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Embodiment 1

[0050] described in this example 18 The method for rapidly labeling Cys-AnnexinV in F, specifically comprises the following steps:

[0051] (1) 18 The preparation of F-Al-NOTA-Maleimide: get the containing 18 F target water 200μL (about 3700MBq), add 200μL containing AlCl 3 A sodium acetate-acetic acid buffer solution with a concentration of 0.5mol / L, pH=4 and 200 μL of an acetonitrile solution containing 5 mg / mL of NOTA-maleimide, wherein the AlCl 3 AlCl in the buffer solution 3 The concentration is 10mg / mL, mix well and react at 90°C for 10 minutes to get 18 F-Al-NOTA-Maleimide, prepared from 18 The F-Al-NOTA-Maleimide solution was purified by preparative HPLC, and the chromatographic conditions were: preparative reversed-phase C18 column (Phenomenex00G-4252-N0, 5 μm, 250x10mm), with a mass concentration of 0.1% trifluoroacetic acid and a mass concentration of 10% acetonitrile solution as the mobile phase for eluting, the flow rate is 2mL / min, the detection wavelength...

Embodiment 2

[0057] described in this example 18 The method for rapidly labeling Cys-AnnexinV in F, specifically comprises the following steps:

[0058] (1) 18 The preparation of F-Al-NOTA-Maleimide: get the containing 18 F target water 200μL (about 3700MBq), add 150μL AlCl containing 10mg / mL 3 The sodium acetate-acetic acid buffer solution with a concentration of 0.5 mol / L and pH=4 and 300 μL acetonitrile solution containing 5 mg / mL NOTA-maleimide were mixed evenly and reacted at 90°C for 10 minutes to obtain 18 F-Al-NOTA-Maleimide, prepared from 18 The F-Al-NOTA-Maleimide solution was purified by preparative HPLC, and the chromatographic conditions were: preparative reversed-phase C18 column (Phenomenex00G-4252-N0, 5 μm, 250x10mm), with a mass concentration of 0.01% trifluoroacetic acid and a mass concentration of 30% acetonitrile solution as the mobile phase for elution, the flow rate is 0.5mL / min, the detection wavelength is 210nm, and the peak time of collection is 13.5min. The ...

Embodiment 3

[0062] described in this example 18 The method for rapidly labeling Cys-AnnexinV in F, specifically comprises the following steps:

[0063] (1) 18 The preparation of F-Al-NOTA-Maleimide: get the containing 18 F target water 250μL (about 3700MBq), add 100μL AlCl containing 5mg / mL 3 The sodium acetate-acetic acid buffer solution with a concentration of 0.2 mol / L and pH=5 and 100 μL acetonitrile solution containing 10 mg / mL NOTA-maleimide were mixed evenly and reacted at 80°C for 20 minutes to obtain 18 F-Al-NOTA-Maleimide, prepared from 18 The F-Al-NOTA-Maleimide solution was purified by preparative HPLC, and the chromatographic conditions were: preparative reversed-phase C18 column (Phenomenex00G-4252-N0, 5 μm, 250x10mm), with a mass concentration of 1% trifluoroacetic acid and a mass concentration of 4% acetonitrile solution as the mobile phase for eluting, the flow rate is 6mL / min, the detection wavelength is 230nm, and the collected peak time is 7.5min. Components, whi...

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Abstract

The invention belongs to the technical field of positron emission computed tomography (PET) imaging, and particularly relates to a method for rapidly marking Cys-Annexin V through <18>F and application of obtained <18>F-Al-NOTA-Cys-Annexin V in the aspect of detecting cell apoptosis. According to the method for rapidly marking Cys-Annexin V through <18>F, <18>F-Al-NOTA-Maleimide is adopted to mark Cys-Annexin V for the first time, the marking time used by the marking method is short, the marking rate is high, the fact of using <18>F for positioning and marking Cys-Annexin V is achieved, and <18>F-Al-NOTA-Cys-Annexin V maintains good affinity with PS, has a good imaging effect by serving as a PET imaging agent and has the more ideal imaging specificity.

Description

technical field [0001] The invention belongs to the field of PET imaging, in particular to a 18 F The method and application of rapidly labeling Cys-AnnexinV. Background technique [0002] Apoptosis, also known as programmed cell death (PCD), is an active cell death process regulated by genes, which is different from necrosis and accidental death. As an important part of the cell life cycle, the process of apoptosis is accompanied by a series of changes in biomolecules and cell morphology. Among them, the phosphatidylserine (PS) in the lipid bilayer of the cell membrane is flipped from the inner layer of the cell membrane to the outer layer, and then exposed to the cell surface. The initial event of the death cascade. The eversion of PS, as a sign of recognition of apoptotic cells by phagocytes, will further cause the shrinkage of cytoplasm, the concentration of chromatin and the degradation of DNA in the nucleus. Therefore, as the target of apoptosis detection, the ever...

Claims

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Application Information

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IPC IPC(8): C07K14/47C07K1/13A61K51/08
CPCA61K51/087C07K14/47
Inventor 陆春雄蒋泉福俞惠新华子春胡敏进谭成
Owner JIANGSU INST OF NUCLEAR MEDICINE
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