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PET/CT (Positron Emission Tomography/Computed Tomography) in vivo molecular imaging probe 18F-Annexin B1 for apoptosis and preparation method and purposes thereof

An 18f-annexinb1, molecular imaging technology, applied in the field of nuclear medicine and molecular imaging, can solve the problems of inability to intuitively evaluate the effectiveness of apoptosis treatment plans, sampling errors in sample processing and preservation, inability to detect, etc., and achieve good in vitro stability. Effect

Inactive Publication Date: 2013-01-09
FUNDAN UNIVERSITY SHANGHAI CANER CENTER
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  • Summary
  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

[0003] In current medical practice, in vitro apoptosis detection methods include morphological detection, TUNEL method, DNA fragmentation detection, mitochondrial membrane potential energy detection, caspase family activity detection and flow cytometry; these in vitro detection methods A certain amount of tissue samples must be obtained, and in vivo testing cannot be performed, and the role of apoptosis in the pathophysiological process of the disease and the effectiveness of the treatment plan cannot be visually evaluated, and there are artificial and uncertainties in sampling errors, sample processing and storage, etc. Factors, so there are great limitations in clinical practical application value

Method used

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  • PET/CT (Positron Emission Tomography/Computed Tomography) in vivo molecular imaging probe 18F-Annexin B1 for apoptosis and preparation method and purposes thereof
  • PET/CT (Positron Emission Tomography/Computed Tomography) in vivo molecular imaging probe 18F-Annexin B1 for apoptosis and preparation method and purposes thereof
  • PET/CT (Positron Emission Tomography/Computed Tomography) in vivo molecular imaging probe 18F-Annexin B1 for apoptosis and preparation method and purposes thereof

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Experimental program
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Embodiment 1

[0022] Embodiment 1: preparation 18 F-Annexin B1

[0023] At 40°C, [ 18 F] SFB and Annexin B1 were mixed and reacted for 20min in the borate buffer solution of pH 8.4, and the labeling rate was detected by analytical gel HPLC (mobile phase was PBS solution (pH 7.4)), and then gel column chromatography method (PD-10, eluent is PBS solution (pH 7.4)) for separation and purification 18 F-Annexin B1 with a labeling efficiency of -15% and a radiochemical purity of -95%.

Embodiment 2

[0024] Embodiment 2: preparation18 F-Annexin B1

[0025] At room temperature, [ 18 F] SFB and Annexin B1 were mixed with borate buffer solution at pH 8.6 and reacted for 60min. First, the labeling rate was detected by analytical gel HPLC (mobile phase was PBS solution (pH 7.4)), and then separated by ultrafiltration centrifugal membrane (NanoSep, the solution is PBS (pH 7.4)) for separation and purification 18 F-Annexin B1 with a labeling efficiency of -10% and a radiochemical purity of -95%.

Embodiment 3

[0026] Embodiment 3: preparation 18 F-Annexin B1

[0027] At 35°C, [ 18 F] SFB and Annexin B1 were mixed with borate buffer solution at pH 8.5 and reacted for 40min. First, the labeling rate was detected by analytical gel HPLC (mobile phase was PBS solution (pH 7.4)), and then semi-preparative gel was used. HPLC method (mobile phase is PBS solution (pH 7.4)) for separation and purification 18 F-Annexin B1 has a labeling rate of ~20% and a radiochemical purity of ~97%. The corresponding HPLC spectra are shown in Figure 1 and figure 2 .

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Abstract

The invention belongs to the technical field of nuclear medicine and molecular imaging, and relates to a PET / CT (Positron Emission Tomography / Computed Tomography) in vivo molecular imaging probe 18F-Annexin B1 for apoptosis and a preparation method and application thereof. The PET / CT in vivo molecular imaging probe 18F-Annexin B1 for apoptosis is 18F-marked annexin B1, an 18F-marked prosthetic group and an annexin B1 are coupled under certain conditions, and the 18F-annexin B1 is separated out and purified. The invention also provides the preparation method for the PET / CT in vivo molecular imaging probe 18F-Annexin B1 for apoptosis. The PET / CT in vivo molecular imaging probe 18F-Annexin B1 for apoptosis can be applied in the experiment on the in vitro association capability of the 18F-annexin B1 with apoptotic cells and PET / CT imaging in the disease diagnosis of tumours, the kidney, the liver, the thymus and other related tissues and organs, the evaluation of curative effect and the screening and evaluation of new curatives and new methods.

Description

technical field [0001] The invention belongs to the technical field of nuclear medicine and molecular imaging, and relates to a cell apoptosis PET / CT in vivo molecular imaging probe 18 F-Annexin B1 and its preparation method and use. Background technique [0002] Apoptosis is a kind of programmed death of cells with typical morphological and biochemical characteristics under the guidance of genes. Apoptosis is closely related to many human diseases, such as tumors, cardiovascular and cerebrovascular diseases, degenerative diseases, inflammation, immune system diseases, and transplant rejection. Drugs targeting apoptosis pathways are expected to bring new benefits to certain diseases. Come new treatments. For example, abnormal cell apoptosis plays an important role in the occurrence and development of tumors, and is closely related to many biological behaviors of tumors, affecting tumor metastasis and prognosis. Artificially induced apoptosis can inhibit the proliferation ...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61K101/02
Inventor 王明伟张勇平章英剑王芳孙树汉
Owner FUNDAN UNIVERSITY SHANGHAI CANER CENTER
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