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Preparation of natural active substance constructed polymer composite medicine and application thereof in inhibiting angiogenesis

A technology of natural active substances and natural macromolecules, applied in the field of biomedical materials, can solve problems such as easy bleeding and restriction, and achieve the effects of easy operation, improved efficiency and improved solubility

Inactive Publication Date: 2014-04-09
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when heparin and its derivatives are used in large quantities, they are easy to cause bleeding, which limits their clinical application.

Method used

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  • Preparation of natural active substance constructed polymer composite medicine and application thereof in inhibiting angiogenesis
  • Preparation of natural active substance constructed polymer composite medicine and application thereof in inhibiting angiogenesis
  • Preparation of natural active substance constructed polymer composite medicine and application thereof in inhibiting angiogenesis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Embodiment 1: Synthesis of ursolic acid-ethylenediamine-low molecular weight heparin compound medicine

[0064] Weigh an appropriate amount of ursolic acid (UA) and put it in an eggplant-shaped bottle, add 20 mL of tetrahydrofuran, the molar concentration of UA is 0.05 mmol / mL, ice bath, and under the protection of inert gas, add dicyclohexylcarbodiimide in turn (DCC) and hydroxysuccinimide (NHS), the molar ratio of UA, DCC, NHS was 1:1.2:1.2 in turn. The reaction was carried out in an ice bath for 30 min, and then moved to room temperature for 24 h. The precipitated dicyclohexylurea (DCU) was removed by vacuum filtration to obtain a filtrate. The filtrate was precipitated with 3 times the amount of n-hexane for 12 h, filtered and dried in vacuo to obtain succinimidyl UA. Weigh 0.23 g of succinimidyl UA, dissolve it with 15 mL of N,N-dimethylformamide (DMF), and slowly add it dropwise to 1 mL of ethylenediamine for 30 minutes. Reaction for another 6h, precipitation w...

Embodiment 2

[0065] Example 2: Synthesis of Gambogic Acid-Cystamine-N-O-Desulfated Heparin Compound Drug

[0066] Weigh an appropriate amount of gambogic acid (GA) and put it in an eggplant-shaped bottle, add 30 mL of tetrahydrofuran, the molar concentration of GA is 0.02 mmol / mL, and under the conditions of dark light, ice bath, and inert gas protection, add dicyclohexylcarbon two in turn. The molar ratio of imine (DCC) and hydroxysuccinimide (NHS), GA, DCC and NHS was 1:1.5:1.2 in turn. After 30min reaction in ice bath, move to room temperature for 36h reaction. The precipitated dicyclohexylurea (DCU) was removed by vacuum filtration to obtain a filtrate. The filtrate was precipitated with 3 times the amount of n-hexane for 8 h, filtered and dried in vacuo to obtain succinimidyl GA. 0.20 g of succinimidyl GA was weighed, dissolved in 10 mL of N,N-dimethylformamide (DMF), and slowly added dropwise to 2 mL of cystamine for 45 minutes. Reaction for another 8h, saturated brine was precipi...

Embodiment 3

[0067] Example 3: Synthesis of rhein-p-phenylenediamine-low molecular weight heparin compound drug

[0068] Weigh an appropriate amount of rhein (Rh) and put it in an eggplant-shaped bottle, add 40 mL of tetrahydrofuran, the molar concentration of Rh is 0.1 mmol / mL, protect from light, ice bath, and under the protection of inert gas, add dicyclohexylcarbodiimide in turn. The molar ratio of amine (DCC) and hydroxysuccinimide (NHS), Rh, DCC and NHS is 1:1.2:1.2 in turn. The reaction was carried out in an ice bath for 60 min, and then moved to room temperature for 24 h. The precipitated dicyclohexylurea (DCU) was removed by vacuum filtration to obtain a filtrate. The filtrate was precipitated with 3 times the amount of n-hexane for 12 h, filtered, and dried in vacuo to obtain succinimidyl Rh. Weigh 0.50 g of succinimidyl Rh, dissolve it with 30 mL of N,N-dimethylformamide (DMF), and slowly add it dropwise to 2.5 mL of p-phenylenediamine for 80 minutes. Reaction for another 12h...

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Abstract

The invention discloses a preparation method of a natural active substance constructed polymer composite medicine and application thereof in inhibiting angiogenesis. The polymer composite medicine is formed by introducing natural active small molecule substances on carboxyl of heparin or derivatives thereof by a chemical coupling method. According to the polymer composite medicine, the dissolubility of the natural active small molecule substances can be improved, the toxic and side effects are reduced, the problem of bleeding after the heparin or derivatives thereof are massively used can be improved, and the effect of inhibiting angiogenesis when the heparin or derivatives thereof are used independently can be reinforced. The polymer composite medicine is simple in preparation process, easy to operate, can reduce cost and improve efficiency, and can easily realize industrialization.

Description

technical field [0001] The invention belongs to the field of biomedical materials, in particular to the preparation of a polymer composite drug constructed from natural active substances and its application in inhibiting angiogenesis. technical background [0002] Cancer is one of the major diseases that threaten human health and life in the world. With the growth of population and changes in people's lifestyles, the incidence of cancer is increasing year by year. Cancer will become an urgent problem for mankind in the new century. [0003] The traditional treatment for tumors is surgical resection when the tumor is in its infancy, and if the tumor cells have spread, chemotherapy is used along with radiation therapy to kill tumor cells and control tumor cell metastasis. Due to the poor selectivity of these treatments, they also kill the normal tissues of the body, reduce the immunity of patients, and bring great side effects while killing tumors. With the rapid progress of ...

Claims

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Application Information

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IPC IPC(8): A61K31/727A61K31/56A61K31/585A61K31/12A61K31/05A61K31/352A61K31/192A61K9/51C08B37/10A61P35/00
Inventor 周建平姚静成文明
Owner CHINA PHARM UNIV
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