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Folic acid targeting vector loading single-substituted epigallocatechin gallate palmitate as well as preparation method and application of folic acid targeting vector

A technology of gallocatechin and gallate, applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc. The time of purity, the effect of improving the efficacy and improving the utilization rate

Active Publication Date: 2018-06-12
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to address the deficiencies in the prior art, to provide a folic acid targeting carrier loaded with mono-substituted epigallocatechin gallate palmitate, which improves the efficiency of single-substituted epigallocatechin gallate palmitate Antioxidant effect, which not only solves the problem of low utilization rate of monogallocatechin gallate palmitate, but also reduces the toxic and side effects of cancer treatment, and makes the drug treatment targeted

Method used

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  • Folic acid targeting vector loading single-substituted epigallocatechin gallate palmitate as well as preparation method and application of folic acid targeting vector
  • Folic acid targeting vector loading single-substituted epigallocatechin gallate palmitate as well as preparation method and application of folic acid targeting vector
  • Folic acid targeting vector loading single-substituted epigallocatechin gallate palmitate as well as preparation method and application of folic acid targeting vector

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1: Preparation of PEGCG

[0054] (1) 10 mmol of EGCG (4.58 g) was added to 100 ml of acetone, and heated in a water bath at 40°C.

[0055] (2) After complete dissolution, 2.46 g of sodium carbonate was added to the solution.

[0056] (3) Add 20 mmol of palmitoyl chloride dropwise to the solution under stirring, and the mixture is carried out in a stoppered flask under water bath conditions.

[0057] (4) After reacting for 6 hours, the reaction mixture was filtered and washed with 100 ml of deionized water, and 100 ml of ethyl acetate was added to extract the mixture.

[0058] (5) Wash the organic phase twice with deionized water. Afterwards, the upper organic phase was dried over anhydrous sodium sulfate and concentrated under reduced pressure to obtain the product PEGCG as a yellow powder.

[0059] The resulting PEGCG has the following structural formula:

[0060]

Embodiment 2

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

[0062] (1) Dissolve 40mg of monogallocatechin gallate palmitate in 4ml of methanol, mix with 0.8mL of 0.25g / mL zinc nitrate hexahydrate methanol solution, stir at room temperature for 5min, and utilize the zinc ions of zinc nitrate Form a coordination bond with monosubstituted epigallocatechin gallate palmitate;

[0063] (2) Add 10ml of 2-methylimidazole in methanol (0.2g / mL), continue stirring 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 PEGCG@ZIF-8 carrier;

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

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

Embodiment 3

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

[0069] (1) Dissolve 10 mg of monogallocatechin gallate palmitate in 4 ml of methanol, mix with 0.8 mL of 0.25 g / mL zinc nitrate hexahydrate methanol solution, stir at room temperature for 5 min, and utilize the zinc ions of zinc nitrate Form a coordination bond with monosubstituted epigallocatechin gallate palmitate;

[0070] (2) Add 10ml of 2-methylimidazole in methanol (0.2g / mL), continue stirring 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 PEGCG@ZIF-8 carrier;

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

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

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Abstract

The invention relates to a folic acid targeting vector loading the single-substituted epigallocatechin gallate palmitate. The folic acid targeting vector comprises a zeolite imidazole skeleton, single-substituted epigallocatechin gallate palmitate embedded in the zeolite imidazole skeleton as well as folic acid-polyethyleneglycol modified on the zeolite imidazole skeleton by virtue of an amido bond. The invention also relates to a preparation method and application of the folic acid targeting vector loading the single-substituted epigallocatechin gallate palmitate. By adopting the folic acid targeting vector, the antioxidant effect of the single-substituted epigallocatechin gallate palmitate is improved, not only can the problem that the utilization rate of the single-substituted epigallocatechin gallate palmitate is low be solved, but also the toxic and side effect in treating the cancer can be reduced, and the treatment of a drug has targeting performance.

Description

technical field [0001] The invention relates to a targeting carrier, in particular to a folic acid targeting carrier loaded with monogallocatechin gallate palmitate and a preparation method and application thereof. Background technique [0002] Tea contains a large amount of polyphenolic compounds, these compounds are collectively called tea polyphenols (tea polyphenol, TP), accounting for about 18-36% of the dry weight of tea. The research on the chemical composition of tea polyphenols shows that the main components of tea polyphenols are catechin compounds, accounting for about 70% to 80% of the total amount of tea polyphenols, mainly containing catechin (C), epicatechin Epigallocatechin (EC), epicatechin gallate (ECG), epigallocatechin gallate (EGC) and epigallocatechin gallate (EGCG) and other active substances, among which EGCG has the highest content, about It accounts for 50% to 60% of the total catechins. At present, a large number of studies have shown that EGCG h...

Claims

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Application Information

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