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Polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anti-cancer drug, preparation method thereof and application of drug

A technology of benzaldehyde nitrogen mustard and polyvinyl alcohol, which is applied in the direction of antineoplastic drugs, drug combinations, and pharmaceutical formulations, can solve the problems of poor selectivity, large toxic and side effects, and low treatment efficiency, and achieve reduced toxicity, water-soluble biocidal Good degradation and water solubility

Active Publication Date: 2018-11-13
GANSU AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nitrogen mustard drugs have the advantages of broad anti-tumor spectrum and strong lethality to tumor cells, but they have disadvantages such as poor selectivity, low therapeutic efficiency, and large toxic and side effects.

Method used

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  • Polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anti-cancer drug, preparation method thereof and application of drug
  • Polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anti-cancer drug, preparation method thereof and application of drug
  • Polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anti-cancer drug, preparation method thereof and application of drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 The preparation method of the polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anticancer drug refers to: dissolving PVA (0.30 g, 6.70 mmol) and PTSA (0.0250 g, 0.15 mmol) in 4 mL DMSO at 70°C , then add benzaldehyde nitrogen mustard (0.165g, 0.67 mmol), stir until dissolved, vacuumize and nitrogen cycle 3~5 times, seal and react at 70°C for 24 h under nitrogen protection, and then precipitate with saturated sodium bicarbonate solution , filtered to obtain precipitate A; precipitate A was air-dried overnight to obtain dry precipitate A; dried precipitate A was dissolved in 10 mL DMSO and stirred overnight, precipitated by saturated sodium bicarbonate solution, and filtered to remove unreacted PVA and nitrogen mustard to obtain precipitate B, which was washed three times with distilled water to remove small molecules, and dried in vacuum at 40°C for 24 h to obtain polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anticancer drug.

[0040] Mn=2.2×10...

Embodiment 2

[0041] Example 2 The preparation method of the polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anticancer drug refers to: dissolving PVA (0.20 g, 4.50 mmol) and PTSA (0.0250 g, 0.15 mmol mmol) in 4 mL DMSO at 70 ° C , then add benzaldehyde nitrogen mustard (0.55g, 2.25mmol), stir until dissolved, vacuumize and nitrogen cycle 3~5 times, seal and react at 70°C for 24 h under nitrogen protection, and then precipitate with saturated sodium bicarbonate solution , filtered to obtain precipitate A; precipitate A was air-dried overnight to obtain dry precipitate A; dried precipitate A was dissolved in 10 mL DMSO and stirred overnight, precipitated by saturated sodium bicarbonate solution, and filtered to remove unreacted PVA and nitrogen mustard to obtain precipitate B, which was washed three times with distilled water to remove small molecules, and dried in vacuum at 40°C for 24 h to obtain polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anticancer drug.

[0042] Mn=2...

Embodiment 3

[0043] Example 3 The preparation method of the polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anticancer drug refers to: dissolving PVA (0.10 g, 2.20 mmol) and PTSA (0.0250 g, 0.15 mmol) in 4 mL DMSO at 70°C , then add benzaldehyde nitrogen mustard (0.55g, 2.20 mmol), stir until dissolved, vacuumize and nitrogen cycle 3~5 times, seal and react at 70°C for 24 h under nitrogen protection, and then precipitate with saturated sodium bicarbonate solution , filtered to obtain precipitate A; precipitate A was air-dried overnight to obtain dry precipitate A; dried precipitate A was dissolved in DMSO and stirred overnight, precipitated by saturated sodium bicarbonate solution, filtered to remove unreacted PVA and nitrogen mustard to obtain precipitate B, which was washed three times with distilled water to remove small molecules, and dried in vacuum at 40°C for 24 h to obtain polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anticancer drug.

[0044] Mn=2.9×10 4 , Mw / Mn...

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Abstract

The invention relates to a polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anti-cancer drug. The average molecular weight of the anti-cancer drug is 20-40kDa, and the structural formula of theanti-cancer drug is as shown in the specification, wherein x=10-100mol%, and y=0-90mol%. The invention further discloses a preparation method and an application of the anti-cancer drug. The staying time of the anti-cancer drug in a tumor can be prolonged, and harm to a normal tissue is reduced.

Description

technical field [0001] The invention relates to the technical field of polymer anticancer drugs, in particular to polyvinyl alcohol-benzaldehyde nitrogen mustard polymer anticancer drugs and its preparation and application. Background technique [0002] Nitrogen mustard was first used to treat tumors in 1940, which ushered in a new era of chemotherapy for tumors. Nitrogen mustard is still a very important class of drugs for clinical treatment of malignant tumors. The mechanism of action of nitrogen mustard antineoplastic drugs is to form electron-deficient ethyleneimine ions in the human body, and then react with electron-rich groups in biomacromolecules (such as DNA, RNA, or some important enzymes). Covalently combined to make DNA molecules break or lose activity, so as to achieve the purpose of anti-tumor. Nitrogen mustard drugs have the advantages of broad anti-tumor spectrum and strong lethality to tumor cells, but they have disadvantages such as poor selectivity, low ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/58A61K31/136A61P35/00
CPCA61K31/136A61K47/58A61P35/00
Inventor 许卫兵闫东强龙海涛蒲陆梅
Owner GANSU AGRI UNIV
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