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Labeling technique for 99Tcm-His10-AnnexinV labeling compound and application of the same as developer in detecting cell apoptosis

A technology of 99tcm-his10-annexinv and compound, which is applied in the application field of radionuclide-labeled compounds, can solve the problems of complex process of bifunctional chelating agent method, increased liver radioactive uptake, and high preparation cost

Active Publication Date: 2008-03-19
JIANGSU TARGET BIOMEDICINE RES INST
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Problems solved by technology

However, the process of the bifunctional chelating agent method is relatively complicated, the technical requirements are strict, and the preparation cost is high.
[0009] The direct reduction labeling method is a more convenient and ideal labeling method, but previous studies believe that: with SnCl 2 As a reducing agent, under neutral pH conditions, high labeling rate (>95%) and good stability (>10h) can be obtained 99 Tc m -AnnexinV labeled product, and easy to kit, but the activity will be affected, resulting in some denatured protein, resulting in increased radioactive uptake by the liver

Method used

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  • Labeling technique for 99Tcm-His10-AnnexinV labeling compound and application of the same as developer in detecting cell apoptosis
  • Labeling technique for 99Tcm-His10-AnnexinV labeling compound and application of the same as developer in detecting cell apoptosis

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example 199

[0033] example 1. 99 Tc m -His10-AnnexinV labeled compound as imaging agent to detect cardiomyocyte apoptosis

[0034] Select 6 experimental minipigs (provided by the Experimental Animal Center of Nanjing Military General Hospital), weighing 15-20Kg, anesthetized by intramuscular injection of 10 mg / Kg of ketamine hydrochloride, and maintained anesthesia by intravenous infusion of Jingan 6 mg / Kg / h. Under X-ray monitoring, the femoral artery was punctured, and a balloon was sent to the distal end of the main branch of the coronary artery through a 6F catheter. The balloon was inflated to block the coronary blood flow. After the blood flow was blocked for 20 to 30 minutes, the pressure was reduced and the catheter was removed, causing myocardial ischemia-reperfusion-acute myocardial infarction injury. ECG monitoring throughout.

[0035] 1 hour after the successful preparation of the animal model, inject into the ear vein 99 Tc m -His10-AnnexinV, the dose is 370MBq (10mCi), 3...

example 299

[0041] Example 2. 99 Tc m -His10-AnnexinV labeled compound is used as an imaging agent to detect tumor cell apoptosis after chemotherapy (taking non-small cell lung cancer as an example)

[0042] A nude mouse model bearing H460 tumor was established. Take the human non-small cell lung cancer (NSCLC) cell line H460, use the RPMI-1640 complete medium containing 15% calf serum in the mass fraction, at 37 ° C, the volume fraction 5% CO 2 Cultured under conditions, when the cells grow to 80%-90% confluence, digest with trypsin to ensure that the rate of viable cells is greater than 99%. Take 4 to 5 week old BALB / C nude mice, will contain 1×10 6 0.2 mL of cell suspension of tumor cells was injected into the axilla of the right forelimb of the mice. When the diameter of the tumor grows to about 1cm, paclitaxel is injected into the tail vein to induce chemotherapy, and the dosage is 100mg / m 2 , 24h, 48h, 72h after chemotherapy for imaging experiments.

[0043] Untreated tumor-be...

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Abstract

The invention relates to a labeling technique of 99Tcm-His10-Annexin V and the applications of the 99Tcm-His10-Annexin V as an imaging agent in terms of apoptosis under the condition of detecting diseases. By applying a direct labeling method, the invention utilizes SnCl2 . 2H2O reductant and citrate buffer to carry out 99Tcm labeling on His10-Annexin V. The method has the advantages of simple and convenient operation and low cost. Experiments on animals show that the injected 99Tcm-His10-Annexin V can clearly display the apoptosis of different tissues, such as cardiac muscle, tumor, etc., and can be applied to the diagnosis of myocardial lesions, the efficacy evaluation of tumor chemotherapy, etc.

Description

technical field [0001] The present invention relates to a radionuclide labeling technology of a compound, and the application of the radionuclide labeled compound, [0002] especially involved 99 Tc m -Application of the His10-AnnexinV labeled compound as an imaging agent. Background technique [0003] Apoptosis is a highly conserved programmed cell death (PCD), which plays an important role in many physiological and pathological processes. Excessive apoptosis can lead to loss of tissue function, such as acute myocardial infarction, chronic heart failure, transplant rejection, stroke, neurodegenerative diseases, etc. In contrast, systemic lupus erythematosus and rheumatoid arthritis are characterized by insufficient apoptosis, which allows a large number of immune cells to survive and inappropriately kill and destroy normal tissues, resulting in impaired tissue and organ functions. Inhibition of apoptosis leads to excessive cell proliferation and tumor formation, and man...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/435A61K51/08A61K103/10
Inventor 华子春王峰方纬杨翔王自正季顺东郑玉民武婕潘旭东
Owner JIANGSU TARGET BIOMEDICINE RES INST
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