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Synthetic method of active BX/Nar-g-HPMA/DEAM/DMDAAC acetylsalicylate

A technology of acetylsalicylate and synthesis method, applied in the direction of organic active ingredients, drug combination, pharmaceutical formula, etc., can solve the problems of gastric mucosal damage and stimulation of gastric mucosa, etc.

Inactive Publication Date: 2021-12-24
GUILIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, long-term oral administration of aspirin can stimulate the gastric mucosa, causing damage to the gastric mucosa, causing gastric ulcer and gastric bleeding

Method used

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  • Synthetic method of active BX/Nar-g-HPMA/DEAM/DMDAAC acetylsalicylate
  • Synthetic method of active BX/Nar-g-HPMA/DEAM/DMDAAC acetylsalicylate
  • Synthetic method of active BX/Nar-g-HPMA/DEAM/DMDAAC acetylsalicylate

Examples

Experimental program
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Effect test

Embodiment

[0040] (1) 4.0 g of bagasse xylan was dried in a constant-temperature vacuum oven at 60° C. for 24 hours to obtain dry-based bagasse xylan.

[0041] (2) Put 0.3 g of naringin sugar in a vacuum constant-temperature drying oven at 60° C. for 24 hours to obtain dry naringin.

[0042] (3) Weigh 0.6g of ammonium persulfate into a 50mL beaker, add 15mL of distilled water to make an initiator solution, stir at room temperature for 10 minutes, pour into a 100mL constant pressure dropping funnel, and set aside.

[0043] (4) Measure 4.0mL of analytically pure hydroxypropyl methacrylate, 4.5mL of analytically pure diethylaminoethyl methacrylate and 4.3mL of analytically pure dimethyldiallylammonium chloride in a 50mL beaker, stir After mixing evenly, the monomer mixture was obtained and poured into another 100mL constant pressure dropping funnel for later use.

[0044] (5) Weigh 3.75g of bagasse xylan obtained in step (1) and 0.25g of dry base naringin obtained in step (2) into a 250mL ...

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Abstract

The invention discloses a synthesis method of active BX / Nar-g-HPMA / DEAM / DMDAAC acetylsalicylate. The method comprises the following steps: by taking bagasse xylan and naringin as raw materials, hydroxypropyl methacrylate, diethylaminoethyl methacrylate and dimethyl diallyl ammonium chloride as mixed grafting monomers and ammonium persulfate as an initiator, synthesizing a bagasse xylan / naringin-g-HPMA / DEAM / DMDAAC grafted copolymer through free radical reaction in a water solvent; on the basis of the intermediate, using ionic liquid 1-butyl-2, 3-dimethylimidazolium as a solvent, using acetylsalicylic acid as an esterifying agent, and synthesizing a product BX / Nar-g-HPMA / DEAM / DMDAAC acetylsalicylate with anticancer activity through catalytic esterification reaction. Effective combination of the product and various amino acid residues of the receptor protein is realized, and the method has wide anticancer and biological medicinal research prospects.

Description

technical field [0001] The invention relates to the fields of fine chemical industry and biomass materials, in particular to a synthesis method of active BX / Nar-g-HPMA / DEAM / DMDAAC acetylsalicylate. Background technique [0002] As a high-quality biomass material, biomass naringin has multiple functions such as antibacterial, anticancer, antispasmodic and choleretic. Among them, the anti-gastric cancer and colon cancer effects are the most prominent. Naringin can up-regulate p18, p19, p21, caspases-3,7, 8,9 Regulate the expression of cell cycle genes with Bak, AIF and Bax, make the cell cycle stay in S phase or G2 / M phase, and induce apoptosis of colorectal cancer cells (SW1116, sw837). However, its clinical application is limited due to its poor absorption in vivo and low oral bioavailability. At the same time, studies have proved that drugs containing carboxymethyl xylan can stimulate nerve reactions with immune cells in the body, that is, through the action of carboxymet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F251/00C08F222/28C08F220/34C08F226/02A61K31/7048A61K31/616A61K47/55A61K47/61A61P35/00
CPCC08F251/00A61K31/7048A61K31/616A61K47/55A61K47/61A61P35/00C08F220/20C08F220/34C08F226/02
Inventor 李和平田可欣赵斌苏越邹志明吕奕菊谢超煜刘红丽郑光禄杨莹莹
Owner GUILIN UNIVERSITY OF TECHNOLOGY
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