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Cell apoptosis imaging medicament 68Ga-NOTA-Duramycin and preparation method thereof

A 68ga, drug-based technology, applied in the field of imaging drugs with phosphatidylethanolamine as the binding target and its preparation, can solve the problems of imaging agent limitation, poor early imaging image quality, slow blood clearance, etc.

Active Publication Date: 2013-01-30
NANJING FIRST HOSPITAL +1
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  • Application Information

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Problems solved by technology

but 99m Tc-AnnexinV still has obvious deficiencies. One is that AnnexinV has a larger molecular weight (36kDa) and blood clearance is slower, and the quality of early imaging images is not good; the other is that it is used for single-photon nuclide imaging, and the resolution is limited; the third is production cost high and expensive
Therefore, the practical application of this imaging agent has been greatly restricted, and the current market performance is not satisfactory.

Method used

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  • Cell apoptosis imaging medicament 68Ga-NOTA-Duramycin and preparation method thereof
  • Cell apoptosis imaging medicament 68Ga-NOTA-Duramycin and preparation method thereof
  • Cell apoptosis imaging medicament 68Ga-NOTA-Duramycin and preparation method thereof

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Embodiment Construction

[0015] one. 68 The preparation method of Ga-NODA-Duramycin

[0016] 1. Expression and purification of Duramycin

[0017] Streptomyces cinnamomycin DSM40005 expression and post-translation stage modified into thioether antibiotics with special amino acid residues, modified cinnamycin structural gene (cinA) to produce Duramycin.

[0018] 2. Synthesis of NOTA-Duramycin

[0019] Duramycin was dissolved in dimethylamide solution, the pH value of triethylamine solution was adjusted to 9.0, p-SCN-Bn-NOTA was added to the reaction system, reacted at room temperature for 2 hours, and the protective group was removed after adding trifluoroacetic acid. After the reaction, NOTA-Duramycin was separated and purified by column, confirmed by mass spectrometry, and then freeze-dried for future use.

[0020] 3. 68 Ga leaching

[0021] Use a 5ml syringe to extract 5mL of 0.05M HCl to rinse the germanium-gallium generator at a flow rate of 1mL / min, and collect the effluent at the same time, ...

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Abstract

The invention relates to a cell apoptosis imaging medicament 68Ga-NOTA-Duramycin which is mainly characterized in that the focused combined target spot is phosphatidyl ethanolamine on the surface of the apoptosis cell, and the main structure Duramycin consists of 19 amino acids and is coupled with a two-functional chelating agent named 1, 4, 7- (triazacyclononane-1, 4-7-triacetic acid, NOTA), and nuclide 68Ga marking is carried out by a direct marking method. The radioactive medicament is a colorless transparent liquid injection solution, and is used for checking cardiac muscle apoptosis after myocardial ischemia injury and tumor cell apoptosis after chemotherapy.

Description

technical field [0001] The invention relates to an imaging drug for detecting cell apoptosis, in particular to an imaging drug with phosphatidylethanolamine as a binding target and a preparation method thereof. Background technique [0002] Apoptosis is an active cell death phenomenon closely regulated by genes, which plays an important role in the occurrence, development and prognosis of many diseases, such as cardiovascular diseases and tumors. [0003] Apoptosis is the main death form of cardiomyocytes in the early stage of myocardial infarction, and it is also an independent prognostic factor for the expansion of infarction; the continuous existence of cardiomyocyte apoptosis and the continuous loss of active cells are the main mechanism for the progressive development of heart failure; cardiomyocytes Increased apoptosis is also one of the important mechanisms for myocarditis to develop into dilated cardiomyopathy and then to heart failure. [0004] The occurrence of tu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/08A61K103/00
Inventor 王峰汪蕾方纬华子春
Owner NANJING FIRST HOSPITAL
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