Anticancer drug with targeting and fluorescence and preparation method thereof

An anticancer drug and fluorescent technology, which is applied in the field of targeted and fluorescent anticancer drugs and their preparation, can solve normal organ cell damage, tissue organ damage, and difficult in situ real-time evaluation of tumor changes of anticancer drugs To achieve the effect of early tumor diagnosis, reduction of toxic side effects, strong targeting and fluorescence

Inactive Publication Date: 2018-04-27
SHANGHAI UNIV
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods are only a static description of a state in the process of tumor changes, and it is difficult to evaluate the changes of anticancer drugs on the patient's tumor in situ and in real time, and to study the kinetics of the action process of anticancer drugs and cancer lesions at the molecular level
[0004] At present, chemical drugs are mainly used for the treatment of cancer patients. While inhibiting or killing tumor cancer cells, these anticancer drugs are also likely to cause serious damage to some normal organ cells in the body, and to certain tissues and organs such as the liver. , kidneys, heart, lungs, etc. also cause serious damage

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Anticancer drug with targeting and fluorescence and preparation method thereof
  • Anticancer drug with targeting and fluorescence and preparation method thereof
  • Anticancer drug with targeting and fluorescence and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Step 1, synthesis of bromoacetyl bromide dextran:

[0084] Dissolve β-glucan 20,000, pyridine and bromoacetyl bromide in dimethyl sulfoxide at a molar ratio of 1:1:0.6, and the molar concentration of β-glucan 20,000 in dimethyl sulfoxide is 0.1 ~1mol / L, react at room temperature for 1~5d, then precipitate the reaction solution with absolute ethanol, filter with suction to obtain a solid, and after drying, dissolve the product in deionized water, dialyze by secondary distillation, and dry under vacuum at 40~80°C to obtain bromine Acetyl bromide dextran.

[0085] Step 2, preparation of sodium sulfadiazine:

[0086] Dissolve sulfadiazine and sodium hydroxide in deionized water at a molar ratio of 1:1, the molar concentration of sulfadiazine and sodium hydroxide in deionized water is 0.1mol / L~1mol / L, react at room temperature for 10~48h, and then The reaction solution was poured into an appropriate amount of absolute ethanol while stirring, and a white precipitate was for...

Embodiment 2

[0098] According to the method described in Example 1, bromoacetyl bromide dextran was prepared, except that 100,000 β-glucan, pyridine and bromoacetyl bromide were used in a molar ratio of 1:1:0.5.

[0099] The synthetic process of step 4 is as follows:

[0100] Bromoacetyl bromide dextran, tetrabutylammonium hydroxide and sodium sulfadiazine were dissolved in dimethyl sulfoxide solution at a molar ratio of 1:0.1:0.3, and the bromoacetyl bromide dextran in dimethyl sulfoxide solution The molar concentration is 0.5 mol / L, react at room temperature for 1~5 days, then precipitate with absolute ethanol, filter with suction, dry, dialyze by secondary distillation, and dry in vacuum to obtain bromoacetyl bromide dextran grafted with sulfadiazine;

[0101] The bromoacetyl bromide dextran grafted with sulfadiazine and the ethylenediamine rhodamine B grafted with methanesulfonyl carbanion were mixed according to the molar ratio of 1:0.2 and dissolved in dimethyl sulfoxide solution, an...

Embodiment 3

[0103] Prepare bromoacetyl bromide dextran and sulfadiazine sodium according to the method described in Example 1, the difference is that the molar concentration of rhodamine B and ethylenediamine in step 3 in dehydrated alcohol is 0.1 mol / L ~ 0.15mol / L, the molar ratio of dimethyl sulfoxide to sodium hydride is 5:1.

[0104] The synthetic process of step 4 is as follows:

[0105] Bromoacetyl bromide dextran, tetrabutylammonium hydroxide and sulfadiazine sodium are dissolved in dimethyl sulfoxide solution according to the molar ratio of 1:0.1:0.1, and the bromoacetyl bromide dextran in dimethyl sulfoxide solution The molar concentration is 0.1mol / L, react at room temperature for 1~5 days, then precipitate with absolute ethanol, filter with suction, dry, dialyze by secondary distillation, and dry in vacuum to obtain bromoacetyl bromide dextran grafted with sulfadiazine;

[0106] The bromoacetyl bromide dextran grafted with sulfadiazine and the ethylenediamine rhodamine B graft...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
degree of graftingaaaaaaaaaa
degree of graftingaaaaaaaaaa
Login to view more

Abstract

The invention provides a targeted fluorescent anti-cancer drug and a preparation method thereof. A structural formula of the anti-cancer drug is shown as the description. The targeted fluorescent anti-cancer drug has the advantages that the anti-cancer drug is highly targeted and fluorescent, so that stability of the anti-cancer drug in vivo can be improved and use ratio of the anti-cancer drug can be increased; since an anti-cancer drug and cancer cell acting process and drug efficacy in-situ imaging evaluation are achieved, early cancer diagnosis is achieved, and further, cancer treatment efficiency is improved while side effect is reduced.

Description

technical field [0001] The invention relates to an anticancer drug and a preparation method thereof, in particular to an anticancer drug with targeting and fluorescence and a preparation method thereof. Background technique [0002] Due to certain environmental and genetic carcinogenic factors, DNA damage is caused, proto-oncogenes are activated or tumor suppressor genes are inactivated, and target cells are transformed. When these transformed target cells accumulate to a certain extent, malignant diseases, even malignant tumors, will form. This type of disease often lacks specific symptoms in the early stage, and when it is discovered, it is mostly in the middle and late stages, and the best time for treatment has been lost. Therefore, early detection, early diagnosis, and early treatment are the key to reducing the recurrence rate of malignant tumors and improving the survival rate. [0003] The traditional methods for evaluating the curative effect of anticancer drugs o...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K31/635A61K31/716A61K49/00A61P35/00
CPCA61K31/635A61K31/716A61K49/0041A61K49/0054A61K2300/00
Inventor 颜世峰刘明巧尹静波
Owner SHANGHAI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap