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Preparation method and application of folacin mediated tumor targeting adriamycin prodrugs

The technology of a prodrug, doxorubicin, is applied in the preparation and application of folic acid-mediated tumor-targeting doxorubicin prodrug, which can solve the problems of cytotoxicity limitation, tumor cell drug resistance, etc.

Inactive Publication Date: 2012-02-08
FOURTH MILITARY MEDICAL UNIVERSITY
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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 and application of folacin mediated tumor targeting adriamycin prodrugs
  • Preparation method and application of folacin mediated tumor targeting adriamycin prodrugs
  • Preparation method and application of folacin mediated tumor targeting adriamycin prodrugs

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0036] Study on Antitumor Activity of Doxorubicin Prodrugs in Vitro

[0037] 1. Purpose:

[0038] The antitumor activity of the prodrug was evaluated by in vitro experiments with doxorubicin as a positive control.

[0039] 2 Research methods:

[0040] 2.1 In vitro cytotoxicity evaluation of prodrugs

[0041] Dissolve the 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 KB cells with high expression of folic acid and folic acid in the logarithmic growth phase. Negatively expressed A549 cells were seeded in 96-well plates at a density of 1×10 4 After culturing for 24 hours, DOX, FA-AMA-DOX, and DOX-hyd-PEG-FA were added at 0.001, 0.01, 0.1, 1, and 10 μM (concentrations of doxorubicin) respectively (the culture medium without serum was blank Control), after incubation for 24h / 48h, add 20μL MTT and continue to incubate for 4h, discard the culture medium, redissolve the purple crys...

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Abstract

The invention provides a preparation method and application of two types of adriamycin prodrugs. The two types of prodrugs with tumor active targeting and acid-sensitive initial burst release properties can be prepared by virtue of connection of hydrazone bonds and introduction of folacin. By utilizing the two types of prodrugs, the tumor resistance of adriamycin can be reinforced, the toxic and side effects of the medicament can be reduced, and the targeting property can be improved. Therefore, the preparation method provides a novel idea for the development of anti-tumor medicaments.

Description

technical field [0001] The invention relates to the preparation method and application of two doxorubicin prodrugs. 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61P35/00
Inventor 周四元叶威良宦梦蕾滕增辉张邦乐梅其炳
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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