Ferrocene-berberine/indomethacin@glucose oxidase@hyaluronic acid nanomedicine, preparation method and application

A technology of glucose oxidase and indomethacin, applied in biochemical equipment and methods, oxidoreductase, drug combination and other directions, can solve problems such as limiting the further use of CDT, achieve easy reproducibility and characterization, good therapeutic effect, inhibiting transfer effect

Active Publication Date: 2022-04-26
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, CDT generated by the Fenton reaction requires high levels of acid and H in the tumor microenvironment 2 o 2 , which limits the further use of CDT

Method used

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  • Ferrocene-berberine/indomethacin@glucose oxidase@hyaluronic acid nanomedicine, preparation method and application
  • Ferrocene-berberine/indomethacin@glucose oxidase@hyaluronic acid nanomedicine, preparation method and application
  • Ferrocene-berberine/indomethacin@glucose oxidase@hyaluronic acid nanomedicine, preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1 synthesis demethylberberine

[0039] Under conditions of solvent-free and vacuum and 190°C, 5g of berberine was placed in a 100mL clean round-bottomed flask and stirred for 45min, and the obtained berberine crude product was passed through column chromatography (elution machine volume ratio: chloroform / methanol=20 / 1) Demethylberberine (3.75 g, yield 79%) was isolated.

Embodiment 2

[0040] Embodiment 2 synthetic hydroxyethyl substituted berberine

[0041] With acetonitrile (20mL) as the solvent and potassium carbonate as the base (1.29g), place the demethylberberine (3g) prepared in Example 1 in a 100mL round-bottomed flask and stir for 25min, then add bromine in batches Ethanol (2.33g), continue reflux reaction 12h, remove reaction solvent and separate by column chromatography (elution machine volume ratio: chloroform / methanol=20 / 1), obtain hydroxyethyl berberine (3.53g, yield 85% ).

Embodiment 3

[0042] The hydroxyethyl berberine of embodiment 3 synthetic reduction

[0043] Under the condition of methanol (20mL) as solvent, the hydroxyethylberberine (2g, 4.49 mmol) prepared in Example 2 was placed in a 250mL round bottom flask and stirred, then sodium borohydride (0.34g, 8.98 mmol), continue to react for 12h, remove the reaction solvent and separate by column chromatography (elution machine volume ratio: chloroform / methanol=30 / 1) to obtain reduced hydroxyethylberberine (1.54g, yield 93%).

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Abstract

The invention discloses a method for ferrocene-berberine / indomethacin@glucose oxidase@hyaluronic acid self-assembly targeting anti-cancer nano-medicine, by designing ferrocene-berberine-coupled drug molecules, and Indomethacin together induces the self-assembly of glucose oxidase, which is then encapsulated by hyaluronic acid to obtain anticancer nano-drugs. The present invention provides a preparation method of the ferrocene-berberine / indomethacin@glucose oxidase@hyaluronic acid nanomedicine and its application in cancer treatment. The nano-medicine provided by the invention can be delivered in a targeted manner, and exhibits significant inhibitory effects on growth and metastasis of liver cancer cells.

Description

technical field [0001] The invention relates to drug synthesis technology, in particular to a targeted ferrocene-berberine / indomethacin@glucose oxidase@hyaluronic acid nanomedicine and its preparation method and application. Background technique [0002] With the rapid development of nanotechnology, traditional cancer chemotherapy has made more and more progress, greatly improving the bioavailability and targeting ability of drugs, but most nanomedicine monotherapy still has drug resistance. Frequent sexual and repeated recurrence and transfer of the disease and other deficiencies. Combination therapy combining two or more therapeutic strategies is a promising approach with the potential to improve the effects of monotherapy and overcome their shortcomings. [0003] with singlet oxygen ( 1 o 2 ) compared with hydroxy radical ( OH) is another reactive oxygen species (ROS) with higher oxidative capacity, and a large amount of OH can cause irreversible damage to biological m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/55A61K38/44A61K33/26A61K31/4375A61P35/00A61P35/04
CPCA61K9/5161A61K47/55A61K38/443C12Y101/03004A61K33/26A61K31/4375A61P35/00A61P35/04A61K2300/00
Inventor 吉远辉程宇
Owner SOUTHEAST UNIV
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