Preparation method for amycin pro drug and application thereof

A prodrug, doxorubicin technology, applied in the field of preparation of doxorubicin prodrug, can solve the problems of tumor cell drug resistance, cytotoxicity limitation, etc.

Inactive Publication Date: 2010-01-13
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

Clinical studies in recent years have found that in the clinical application of doxorubicin, drug resistance against tumor cells has emerged, and its cytotoxicity to normal tissues limits its further application

Method used

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  • Preparation method for amycin pro drug and application thereof
  • Preparation method for amycin pro drug and application thereof
  • Preparation method for amycin pro drug and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0017] Study on Antitumor Activity of Doxorubicin Prodrugs in Vitro

[0018] 1. Purpose:

[0019] The anti-tumor activity of the prodrug was evaluated by in vivo and in vitro experiments with doxorubicin as a positive control.

[0020] 2 Research methods:

[0021] 2.1 In vitro cytotoxicity evaluation of prodrugs

[0022] Dissolve various drugs to be tested in serum-free culture medium (DMSO less than 0.1%) according to the set concentration, and use 0.25% trypsin to digest the liver cancer cells HepG-2 and breast cancer cells that have grown to the logarithmic growth phase. Cells MCF-7 and breast cancer cells MDA-MB-231 were seeded in 96-well plates at a density of 1×10 4 After culturing for 24 hours, DOX, DOX-LNA, PEG-DOX amid, PEG-DOX hydrazone (the serum-free culture medium) were added respectively at 0.001, 0.01, 0.1, 1, 10, and 100 μM (concentrations of doxorubicin) After 48 hours of incubation, add 20 μL MTT and continue to incubate for 4 hours, discard the culture m...

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Abstract

The invention provides a preparation method for amycin pro drug and application thereof; the method is as follows: potassium permanganate and polyethylene glycol are oxidized and reacted to generate polyethylene glycol diacid; by EDCI catalyzing effect, polyethylene glycol diacid and hydrazinoformic acid butyl ester are reacted and then BOC protective group is drawn off to generate polyethylene glycol maleic hydrazide intermediate product; by EDCI catalyzing effect, the intermediate product is drawn into 13-carbonyl of amycin to obtain target compound amycin-polyethylene glycol diacid hydrazone bond linker. The pro drug can strength anti-tumor effect of amycine, reduces toxic and side effect of medicine, increases targeting effect, and provides new idea for the development of anti-tumor medicines.

Description

technical field [0001] The invention relates to a preparation method and application of doxorubicin prodrug. Background technique [0002] Malignant tumors seriously endanger human health and survival, and are one of the main causes of death. In 2000, the World Health Organization reported that the number of cancer deaths worldwide has exceeded 7 million, of which 21% were in developed countries and 9% in developing countries, and the number of deaths caused by tumors accounted for 12% of the global death toll. Malignant tumors have become the leading cause of death among urban and rural residents in my country, with about 2 million new cases and 1.7 million deaths each year. [0003] Anthracycline antibiotics are one of the most commonly used and effective anti-tumor drugs in clinical practice. Adriamycin is a representative drug of this type of anti-tumor drug. It was first obtained from the pigment metabolites of Streptococcus in the 1960s. Doxorubicin is a broad-spectr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48A61K47/48A61K31/704A61P35/00
Inventor 周四元张邦乐宦梦蕾滕增辉梅其炳
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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