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Resveratrol high-molecular bonding drug and preparation method thereof

A technology of resveratrol and high-molecular polymer, applied in the field of medicine, can solve the problems of large influence of inclusion effect, no water solubility and stability involved, etc., achieve good hydrophilicity and biocompatibility, avoid The effect of phagocytosis and efficient targeting

Active Publication Date: 2015-04-22
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patent application number CN02144831.0 (hydroxypropyl-β-cyclodextrin inclusion complex of resveratrol and glucoside and derivatives and preparation method) discloses a method for preparing hydroxypropyl-β-cyclodextrin and Conjugates composed of resveratrol compounds, the main content of which discloses the preparation method of conjugates composed of resveratrol glycosides and cyclodextrins, but the temperature that has a greater impact on the inclusion effect is not involved
The application number is CN200610038491.4 (a class of resveratrol compounds with carboxyl substituents and its preparation method) to prepare new carboxyl substituted resveratrol compounds. The higher anti-tumor, cardiovascular protection or anti-oxidation activities of retrol, but not related to its water solubility and stability

Method used

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  • Resveratrol high-molecular bonding drug and preparation method thereof
  • Resveratrol high-molecular bonding drug and preparation method thereof
  • Resveratrol high-molecular bonding drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Add 1.9g of p-toluenesulfonyl chloride into a dry reactor with a water separation device and a stirring device, replace the argon gas 3 times, azeotropically remove water with anhydrous toluene, remove most of the toluene, and change it to a decompression device to extract Toluene remained and was vacuum dried at 80°C for 6 hours. After returning to room temperature, add 3.00 g of recrystallized resveratrol and 100 ml of anhydrous acetone under the protection of an inert gas, and add a small amount of NaHCO to the reaction at the same time 3 , and reacted at 25°C for 18 hours under magnetic stirring. The product was filtered to remove NaHCO 3 , the supernatant was suspended and evaporated to a molten state to remove a large amount of acetone, the product was dissolved in appropriate dichloromethane, settled in ether, and dried in vacuo to obtain 4.10 g of a white powder product with a yield of 83.7%.

[0061] The infrared spectrum of gained resveratrol derivative sees...

Embodiment 2

[0065] Add 1.90g of p-toluenesulfonyl chloride into a dry reactor with a water separation device and a stirring device, replace the argon gas 3 times, azeotropically remove water with anhydrous toluene, remove most of the toluene, and change to a decompression device to extract Toluene remained and was vacuum dried at 80°C for 6 hours. After returning to room temperature, 3.00 g of recrystallized resveratrol and 100 ml of anhydrous acetone were added under the protection of an inert gas, and a small amount of NaHCO was added to the reaction 3 , and reacted at 25°C for 18 hours under magnetic stirring. The product was filtered to remove NaHCO 3 , the supernatant was suspended and evaporated to a molten state to remove a large amount of acetone, the product was dissolved in appropriate dichloromethane, settled in ether, and dried in vacuo to obtain 4.10 g of a white powder product with a yield of 83.7%.

[0066] The infrared test results of the obtained synthetic product show ...

Embodiment 3

[0069] Add 785 mg of acetyl chloride into a dry reactor with a water separator and a stirring device, replace the argon gas 3 times, soak the molecular sieve to remove water, remove most of the water, and change to a decompression device to extract the purified acetyl chloride. Add to 100ml of anhydrous acetone under the protection of inert gas and add recrystallized resveratrol 3.00g, add a small amount of NaHCO to the reaction at the same time 3 , and reacted at 25°C for 20 hours under magnetic stirring. The product was filtered to remove NaHCO 3 , the supernatant was suspended and evaporated to a molten state to remove a large amount of acetone, and the product was dissolved in appropriate dichloromethane, settled with ether, and dried in vacuo to obtain 2.80 g of a white powder product with a yield of 74.0%.

[0070] The infrared test results of the obtained synthetic product show that the product contains both the resveratrol structure and the characteristic absorption p...

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Abstract

The invention discloses a resveratrol high-molecular bonding drug and a preparation method of the resveratrol high-molecular bonding drug. The resveratrol high-molecular bonding drug has the general formula of P-RES'm, wherein P is a water-soluble high-molecular polymer, m is an integer ranging from 1 to 50, and RES' is resveratrol derivatives which are made from resveratrol and acyl chloride. The high-molecular bonding drug is good in hydrophilicity and biocompatibility and can avoid human body reticuloendothelial system phagocytosis in blood circulation and guarantee the situation that the drug has enough time to reach a tumor portion through the EPR effect, and therefore the drug can enter cells through endocytosis, and the efficient targeting effect of the drug is achieved.

Description

technical field [0001] The invention relates to the technical field of medicines. More specifically, it relates to a resveratrol polymer-bonded drug and a preparation method thereof. Background technique [0002] Resveratrol (resveratrol), a derivative of 1,2-stilbene, its chemical name is 3,4',5-trihydroxy-trans-stilbene (3,4',5 -trihydroxy-stilbene), is a colorless needle-like crystal, easily soluble in ether, chloroform, methanol, ethanol, acetone, ethyl acetate and other organic solvents. Resveratrol is a phytoalexin produced by plants, which has various physiological activities and pharmacological effects, and is the main active ingredient in grapes. Its structural formula is: [0003] [0004] Studies so far have shown that resveratrol has anti-tumor, anti-cardiovascular disease, anti-oxidation, antibacterial and other effects. However, resveratrol is a polyphenolic compound, which has the disadvantages of poor stability and poor solubility in water, which limit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/05A61K9/107A61P35/00A61P9/00A61P39/06A61P31/04
Inventor 乐园王文龙张亮杨小兰刘孟涛张德涛王洁欣陈建峰
Owner BEIJING UNIV OF CHEM TECH
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