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Folic acid targeting carrier loaded with epigallocatechin gallate, preparation method and application thereof

A technology of epigallocatechin and gallate, which is applied in the field of folic acid targeting carrier loaded with epigallocatechin gallate and its preparation, and can solve the problem of the utilization rate of tea polyphenol epigallocatechin gallate Low-level problems, to achieve the effect of reducing the level of active oxygen, prolonging the time of high purity, and simple synthesis method

Active Publication Date: 2020-09-18
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to address the deficiencies in the prior art, to provide a folic acid targeting carrier loaded with epigallocatechin gallate, which improves the antioxidant effect of epigallocatechin gallate, and solves the The problem of low utilization rate of phenolic epigallocatechin gallate reduces the toxic and side effects of cancer treatment and makes the drug treatment targeted

Method used

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  • Folic acid targeting carrier loaded with epigallocatechin gallate, preparation method and application thereof
  • Folic acid targeting carrier loaded with epigallocatechin gallate, preparation method and application thereof
  • Folic acid targeting carrier loaded with epigallocatechin gallate, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1: Preparation of FA-PEG / EGCG@ZIF-8

[0055] (1) Dissolve 40mg of epigallocatechin gallate in 4ml of methanol and 0.2g of zinc nitrate hexahydrate in 0.8ml of methanol solution, mix them at room temperature for 5 minutes, and use the zinc ions of zinc nitrate and epigallocatechin Vegetarian gallate forms a coordination bond;

[0056] (2) Add 10ml of anhydrous methanol and 2g of 2-methylimidazole, and continue to stir at room temperature for 15min, 2-methylimidazole and the zinc ion of the coordination compound form ZIF-8;

[0057] (3) Centrifuge at a rotational speed of 11000rmp for 20min, then wash three times with absolute ethanol and a deionized mixed solution to remove unreacted reagents, and dry in vacuum to obtain the EGCG@ZIF-8 carrier;

[0058] (4) Dissolve 50mg of folic acid-polyethylene glycol into 5ml of deionized water;

[0059] (5) Add 50 mg of EGCG@ZIF-8 carrier, ultrasonically shake evenly, and stir at room temperature for 36 hours;

[0060] (6...

Embodiment 2

[0061] Example 2: Preparation of FA-PEG / EGCG@ZIF-8

[0062] (1) Dissolve 10 mg of epigallocatechin gallate in 4 ml of methanol and 0.2 g of zinc nitrate hexahydrate in 0.8 ml of methanol solution, mix them at room temperature for 5 minutes, and utilize the zinc ions of zinc nitrate and epigallocatechin Vegetarian gallate forms a coordination bond;

[0063] (2) Add 10ml of anhydrous methanol and 2g of 2-methylimidazole, and continue to stir at room temperature for 15min, 2-methylimidazole and the zinc ion of the coordination compound form ZIF-8;

[0064] (3) Centrifuge at a rotational speed of 11000rmp for 20min, then wash three times with absolute ethanol and a deionized mixed solution to remove unreacted reagents, and dry in vacuum to obtain the EGCG@ZIF-8 carrier;

[0065] (4) Dissolve 50mg of folic acid-polyethylene glycol into 5ml of deionized water;

[0066] (5) Add 50 mg of EGCG@ZIF-8 carrier, ultrasonically shake evenly, and stir at room temperature for 36 hours;

[...

Embodiment 3

[0068] Example 3: Preparation of FA-PEG / EGCG@ZIF-8

[0069] (1) Dissolve 40mg of epigallocatechin gallate in 4ml of methanol and 0.2g of zinc nitrate hexahydrate in 0.8ml of methanol solution, mix them at room temperature for 5 minutes, and use the zinc ions of zinc nitrate and epigallocatechin Vegetarian gallate forms a coordination bond;

[0070] (2) Add 10ml of anhydrous methanol and 4g of 2-methylimidazole, and continue to stir at room temperature for 15min, 2-methylimidazole and the zinc ion of the coordination compound form ZIF-8;

[0071] (3) Centrifuge at a rotational speed of 11000rmp for 20min, then wash three times with absolute ethanol and a deionized mixed solution to remove unreacted reagents, and dry in vacuum to obtain the EGCG@ZIF-8 carrier;

[0072] (4) Dissolve 50mg of folic acid-polyethylene glycol into 5ml of deionized water;

[0073] (5) Add 50 mg of EGCG@ZIF-8 carrier, ultrasonically shake evenly, and stir at room temperature for 36 hours;

[0074] (6...

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Abstract

The invention relates to an epigallocatechin gallate-loaded folate-targeted carrier, which is prepared from zeolite imidazole skeleton, epigallocatechin gallate embedded in the zeolite imidazole skeleton, and folic acid-polyethylene glycol modified on the zeolite imidazole skeleton by means of an amido bond. The invention also relates to a preparation method and application of the epigallocatechingallate-loaded folate-targeted carrier. The folate-targeted carrier enhances the antioxidant effect of the epigallocatechin gallate, not only solves the problem of low utilization rate of the tea polyphenol epigallocatechin gallate, but also reduces the toxic and side effects of cancer treatment, and enables medical therapy to have targeting ability.

Description

technical field [0001] The invention relates to a targeting carrier, in particular to a folic acid targeting carrier loaded with epigallocatechin gallate and a preparation method and application thereof. Background technique [0002] The harm of cancer is increasing worldwide, and it has become the number one "killer" that threatens human health. Regardless of age, gender, social status, etc., cancer directly or indirectly affects human life. It is not only a personal health issue, but also a social issue that has been closely watched by families and society. Therefore, research on cancer cells has always been a hot spot in recent scientific research. Some essential characteristics of cancer cells, such as uncontrolled reproduction, high reactive oxygen species, and strong environmental adaptability, have been discovered one after another. In cancer research, treating cancer according to the characteristics of cancer cells has gradually become a research direction. [000...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K47/60A61K47/69A61K47/22A61K47/02A61K31/353A61P35/00
CPCA61K31/353A61K47/02A61K47/22
Inventor 陈雪瑞施浙琪吴健雷群芳方文军
Owner ZHEJIANG UNIV
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