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Screening probe of medicine for inducing tumor cell epithelial-mesenchymal transition as well as preparation method and application of screening probe

A technology of tumor cells and drugs, applied in the field of medicine, can solve problems such as inability to obtain intuitively

Pending Publication Date: 2022-04-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The aptamer SYL3C can bind to the EMT biomarker EpCAM protein with high affinity and strong specificity, but the effect of binding to the biomarker cannot be intuitively obtained only by using the aptamer

Method used

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  • Screening probe of medicine for inducing tumor cell epithelial-mesenchymal transition as well as preparation method and application of screening probe
  • Screening probe of medicine for inducing tumor cell epithelial-mesenchymal transition as well as preparation method and application of screening probe
  • Screening probe of medicine for inducing tumor cell epithelial-mesenchymal transition as well as preparation method and application of screening probe

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] The preparation method of the screening probe TPE-SYL3C-FAM for inducing tumor cell epithelial-mesenchymal transition drugs is as follows: figure 1 ,Proceed as follows:

[0068] Step (1), triphenylbromoethylene (700mg), 4-ethoxycarbonylphenylboronic acid (450mg), potassium carbonate (3.6g), tetrakis (triphenylphosphine) palladium (120mg) and tetra-n-octyl bromide Ammonium (100mg) was dissolved in toluene-ethanol-water (4:1:1, v:v:v) mixed solvent (60mL), heated to reflux at 90°C for 12h under nitrogen protection, extracted 3 times with 40mL dichloromethane, combined The dichloromethane phase was purified by flash column chromatography after rotary evaporation (eluent was petroleum ether:dichloromethane=1:4, v:v) to obtain 4-(1,2,2-triphenylvinyl) Ethyl benzoate (yield 86.1%); image 3 It is the structural characterization result of ethyl 4-(1,2,2-triphenylvinyl)benzoate, [M+Na] + Precise molecular weight theoretical value m / z 427.1674, measured value m / z 427.1675, m...

Embodiment 2

[0094] Step (1), triphenylbromoethylene (700mg), 4-ethoxycarbonylphenylboronic acid (700mg), potassium carbonate (5.4g), tetrakis (triphenylphosphine) palladium (120mg) and tetra-n-octyl bromide Ammonium (100mg) was dissolved in toluene-ethanol-water (5:1:1, v:v:v) mixed solvent (60mL), heated to reflux at 100°C for 24h under nitrogen protection, extracted 3 times with dichloromethane, and passed through rapid Purified by column chromatography (eluent: petroleum ether:dichloromethane=1:4, v:v) to obtain ethyl 4-(1,2,2-triphenylvinyl)benzoate.

[0095] Step (2), 4-(1,2,2-triphenylvinyl)ethyl benzoate (400mg), lithium hydroxide monohydrate (1.89g), water (30mL) were dissolved in tetrahydrofuran (30mL), Heating to reflux at 100°C for 24 h under nitrogen protection; cooling the reaction solution to room temperature, adjusting the pH of the reaction solution to 4.0 with 1M HCl, extracting with dichloromethane three times, and purifying by flash column chromatography (eluent: ethyl ...

Embodiment 3

[0099] Step (1), triphenylbromide (700mg), 4-ethoxycarbonylphenylboronic acid (900mg), potassium carbonate (5g), tetrakis (triphenylphosphine) palladium (240mg) and tetra-n-octyl ammonium bromide (200mg) dissolved in a mixed solvent (60mL) of toluene-ethanol-water (4:1:1, v:v:v), heated to reflux at 120°C for 48h under nitrogen protection, extracted 3 times with dichloromethane, and passed Purified by column chromatography (eluent is petroleum ether:dichloromethane=1:4, v:v) to obtain ethyl 4-(1,2,2-triphenylethenyl)benzoate;

[0100] Step (2), 4-(1,2,2-triphenylvinyl)ethyl benzoate (400mg), lithium hydroxide monohydrate (2.52g), water (40mL) were dissolved in tetrahydrofuran (40mL), Heated to reflux at 120°C for 48 h under nitrogen protection, cooled the reaction solution to room temperature, adjusted the pH of the reaction solution to 4.0 with 1M HCl, extracted 3 times with dichloromethane, and purified by flash column chromatography (eluent: ethyl acetate:petroleum ether =...

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Abstract

The invention belongs to the technical field of medicines, and discloses a screening probe of a medicine for inducing tumor cell epithelial-mesenchymal transition, which is characterized in that the screening probe is formed by modifying the 5'end of an aptamer SYL3C and modifying 6-carboxyl fluorescein at the 3 'end of the aptamer SYL3C. According to the probe disclosed by the invention, by identifying a biomarker epithelial adhesion molecule down-regulated in an epithelial-mesenchymal transition process, an epithelial-mesenchymal transition positive drug is screened according to reduction of a normalized fluorescence intensity signal of cell viability after drug administration. In addition, the chemosensitizer for blocking epithelial-mesenchymal transition and an epithelial-mesenchymal transition inducer TGF-beta are jointly administered, and the chemosensitizer is screened according to the recovery condition of a normalized fluorescence intensity signal of cell viability after the chemosensitizer is administered.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a screening probe for inducing epithelial-mesenchymal transition drugs of tumor cells, a preparation method and application thereof. Background technique [0002] Inhibition of tumor metastasis and drug resistance is a difficult problem in the clinical treatment of tumors. Epithelial-mesenchymal transition (EMT) is one of the important factors leading to tumor metastasis and drug resistance. EMT refers to the characteristics of mesenchymal cells with migration and invasion capabilities after epithelial tumor cells undergo various physiological changes. The key biochemical and morphological changes of EMT include down-regulation of epithelial cell adhesion molecule (EpCAM) protein expression and loss of intercellular contact. The activation of the EMT program is considered to be an important marker of tumor progression, which can induce and improve the metastatic ability of epithelial tumo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N15/115C07D207/46C09K11/06G01N21/64G01N33/574
Inventor 王颖铭韩承刚郑枫柳文媛冯锋
Owner CHINA PHARM UNIV
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