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Positron nuclide-labeled dansylamide stilbene compound, its synthesis method and application

A technology of dansylamide-based and methoxystilbenes, which is applied in the field of positronnuclide-labeled dansylamido-stilbenes, their synthesis and application, and can solve the problem of untargeted cell apoptosis and target To solve the problems of β-amyloid PET dual-mode imaging agent, achieve the effect of easy automatic labeling, high radiochemical yield, and great application prospects

Active Publication Date: 2019-10-15
GUANGDONG HUIXUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] To date, no optical and PET dual-modal imaging agents targeting apoptosis and targeting β-amyloid have been reported

Method used

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  • Positron nuclide-labeled dansylamide stilbene compound, its synthesis method and application
  • Positron nuclide-labeled dansylamide stilbene compound, its synthesis method and application
  • Positron nuclide-labeled dansylamide stilbene compound, its synthesis method and application

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Experimental program
Comparison scheme
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Embodiment 1

[0020] The structural identification of embodiment 1 precursor compound and standard product compound

[0021] 1.1 Preparation of cells, animal sources and animal models

[0022] This study was approved by the Animal Experiment Ethics Committee of the First Affiliated Hospital of Sun Yat-sen University (batch number no.2012.001). S-180 fibrosarcoma cells and liver cancer cell lines were purchased from the Animal Experiment Center of Sun Yat-sen University, Jurkat cells were purchased from the Chinese Academy of Sciences (Shanghai), and A549 cells were donated by the research group of Professor Zang Linquan of Guangzhou School of Pharmacy. Kunming mice: female, clean grade, weighing 18-22 g; nude mice: clean grade, four to five weeks old, all purchased from the Animal Experiment Center of Sun Yat-sen University, license number SYXK (Guangdong) 2007-0081. All experimental mice were raised in the general-grade animal laboratory of Sun Yat-sen Medical University, 5 mice / cage, und...

Embodiment 211

[0036] Example 2 11 Radiosynthesis of C-DSB

[0037] Cyclotron via nuclear reaction 14 N(p,α) 11 C production 11 CO 2 , and then transferred to the PET-CS-II-IT-I 11 C iodide synthesis module. 11 CO 2 Trapped by the Loop (liquid nitrogen cooled to -160°C). Remove the liquid nitrogen cooling ring, pass He gas (20mL / min) and release 11 CO 2 , via P 2 o 5 After drying, the column enters the reaction tube. Accessible 11 CO 2 with LiAlH 4 A reduction reaction occurs 11 CH 3 OH, and then undergoes a substitution reaction with HI to generate 11 CH 3 I. Under the action of He gas, 11 CH 3 I passes through the Ag-triflate column of high temperature, obtains 11 CH 3 -triflate( 11 C-CH 3 OTf). Before the experiment, dissolve 1 mg of the precursor 4-dansylamido-4'-hydroxystilbene (1) in 0.2 mL of DMSO and 0.8 mL of acetone solution, add 20 μL of 2.5 M NaOH solution, and take 0.3 mL into the reaction Tube. 11 C-CH 3 OTf through N 2 carried into the reaction tu...

Embodiment 318

[0043] Example 3 18 Radiosynthesis of F-DFESB

[0044] Cyclotron through 18 O(p,n) 18 F nuclear reaction produces 18 f - Ions, after being captured by the QMA column, use K 222 Solution (K 2 CO 3 2.7mg dissolved in 0.1mL water, 12mg K 222 Dissolved in 0.9mL MeCN) eluting 18 f - to the reaction bottle. Nitrogen gas (80 mL / min) was passed, and the solvent was removed under heating at 116°C. Anhydrous acetonitrile (1.5 mL) was added, nitrogen gas was passed and heated to 116° C., and water was removed again. A solution of the precursor 4-dansylamido-4'-methanesulfonyltriethoxystilbene (3) (5 mg of the precursor dissolved in 1 mL of acetonitrile) was added to a solution containing radioactive [K / K222] +18 f - In a reaction vial, heat to 100°C in a sealed reaction tube and keep for 10 min. After cooling the reaction tube, add 10mL of water to dilute and pass through the SEP PAK plus C18 column. 18 F-DFESB was adsorbed on the SEP PAK plus C18 column, and the SEP PAK ...

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Abstract

The invention relates to an optics and positron emission tomography (PET) dual-mode developer (formula 1) targeted to apoptotic cells and beta-amyloid protein, namely, a positron-nuclide-labeled 4-dansyl amido-4'-diphenylethylene compound. A synthesis method of the compound includes the steps that dansyl targeted to apoptotic cells and 1,2-diphenylvinyl-amino targeted to beta-amyloid protein are bound together, and then labeling is conducted. The compound is simple in radiosynthesis method, high in radiochemical yield and convenient to synthesize automatically, has broad application prospects and can be applied to anti-tumor therapy monitoring and differential diagnosis and scientific research on neurological and psychotic disorders like Alzheimer disease (AD). The formula 1 is defined in the description.

Description

【Technical field】 [0001] The invention relates to an optical and PET dual-mode imaging agent targeting apoptotic cells and targeting β-amyloid protein: a positron nuclide-labeled 4-dansylamide-4'-distyryl compound, and a synthesis method thereof Its application in the preparation of anti-tumor treatment monitoring, differential diagnosis and scientific research drugs of neuropsychiatric diseases such as senile dementia (AD). 【Background technique】 [0002] Apoptosis is the autonomous and orderly death of cells controlled by genes, and it is a special form of death of eukaryotic cells. Apoptosis has important biological significance and can be seen in many physiological processes such as embryonic development, tissue differentiation, and immune regulation. closely related to development [1] . After the apoptosis program is initiated through different pathways, apoptotic cells themselves will produce a series of pathophysiological changes. Apoptotic cells will produce a va...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04G01N21/84
Inventor 唐刚华
Owner GUANGDONG HUIXUAN PHARMA TECH
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