A recombinant human endostatin imaging agent and its preparation method

A technology of vascular endothelium and imaging agent, which is applied in the medical field and can solve the problems of low imaging resolution and limited clinical application

Inactive Publication Date: 2018-02-02
SHANDONG RES INST OF TUMOUR PREVENTION TREATMENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

but 131 I can only be used for SPECT imaging, and its imaging resolution is low, which limits its clinical application

Method used

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  • A recombinant human endostatin imaging agent and its preparation method
  • A recombinant human endostatin imaging agent and its preparation method
  • A recombinant human endostatin imaging agent and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: 18 F-FB-Endostar labeling synthesis experiment

[0033] The synthesis steps are as follows:

[0034] 1. 800mCi synthesized by accelerator 18 F ion and 20mg K2.2.2, 5mg K 2 CO 3 React with 5 mg of ethyl 4-trimethylamine benzoate trifluoromethanesulfonate at 120°C for 20 min, then add 1 ml of 0.5 mmol / L NaOH solution for hydrolysis, then add 15 ml of 0.1 mmol / L HCL solution to generate 4- [ 18 F]fluorobenzoic acid ( 18 F-FBA);

[0035] 2. The foregoing 18 F-FBA was heated with 17mg TSTU (2-succinimidyl-1,1,3,3-tetramethyluronium tetrafluoroborate) for 15min, then added 3ml 5% acetic acid and 10mlHO 2 The acetic acid solution obtained by mixing O was acidified and purified by C-18 column to obtain 18 F-SFB ( 18 F-N-succinimide-4-fluorobenzoate).

[0036] 3. The above reaction obtained 18 F-SFB was eluted with acetonitrile, dried with nitrogen, and then 1mg Endostar dissolved in 0.5ml phosphate buffer (pH8.2) was added to the reaction tube, and reacte...

Embodiment 2

[0037] Example 2. Stability of markers in human serum

[0038] 500µCi will be obtained 18 F-FB-Endostar was mixed with 1ml of normal human serum and placed at 37°C. Samples were taken at 1h and 2h for R-TLC analysis (radioactive chromatography analysis) to observe the stability of the marker in human serum.

[0039] see results figure 2 Analysis, when mixed with normal human serum for 1 hour and 2 hours, the position of the radiation peak of the marker did not change, and no other radioactive peaks appeared. It shows that the marker has good stability in serum, and there is no obvious degradation in serum at 37°C for 2 hours.

Embodiment 3

[0040] Embodiment 3. Different pH values ​​carry out 19 F-SFB labeled Endostar experiment and detection of Endostar activity after labeling

[0041] In order to verify whether Endostar is still active after labeling, we carried out experiments under different pH conditions. 19 F-SFB labeled Endostar experiment and detection of Endostar activity after labeling. In order to avoid radioactive contamination when detecting activity, non-radioactive 19 F instead 18 F is marked, while 19 F and 18 F has exactly the same chemical properties. 19 F-SFB was synthesized by Changshu Huayi Chemical Co., Ltd.

[0042] Under the conditions of pH 6.5, 7.0 and 8.0 respectively, carry out 19 F-SFB with marking of Endostar, 19 The molar ratio of F-SFB to Endostar was 20:1, the reaction temperature was 37°C, and the reaction time was 30min. After the reaction was completed, the reaction product was eluted and separated by a desalting column, and two peaks were obtained during the eluted se...

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PUM

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Abstract

The invention relates to the technical field of recombinant human endostatin preparation prepared molecular targeting developers, and concretely provides a novel positron-emitting radionuclide or gadolinium labeled recombinant human endostatin developer and its application in the evaluation and the predication of the curative effective of the antiangiogenetic therapy through the noninvasive and dynamic observation of the conditions of new vessels of a plurality of tumors. The invention also provides a preparation method of the developer. The positron-emitting radionuclide or gadolinium can be combined with human endostatin through a bifunctional chelating agent.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a novel angiogenesis imaging agent prepared by recombinant human vascular endostatin and its application in tumor angiogenesis imaging diagnosis. Background technique [0002] Tumor angiogenesis plays an important role in tumor growth and metastasis. As early as the 1970s, Professor Folkman put forward the theory that "tumor growth and metastasis depend on the formation of new blood vessels". According to this theory, the anti-tumor angiogenesis therapy—dormancy therapy (dormancy therapy) has become one of the hot research fields of tumor therapy today. Some anti-angiogenic targeted drugs have been used clinically, such as bevacizumab, endostar, etc. A large number of clinical studies have confirmed that these drugs combined with chemotherapy or radiotherapy have brought higher treatment efficiency to patients. According to the mechanism of drug action, anti-angiogenesis th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/08A61K49/14A61K101/02A61K103/00A61K103/32
Inventor 于金明胡旭东邢力刚岳德胜张弢林欢
Owner SHANDONG RES INST OF TUMOUR PREVENTION TREATMENT
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