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3MH (3-mercapto-1-hexanol)-EGCG (epigallocatechin gallate) nanoparticle solution system and preparation method thereof

A 3MH-EGCG, 3MH-EGCG- technology, applied in the field of medicine, can solve problems such as liver toxicity

Active Publication Date: 2017-05-31
ZHEJIANG FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] China Patent Authorization Notice No. CN103877588B is our research result in 2014, which discloses the preparation method of EGCG-β-LG nanoparticle solution system by assembling EGCG and β-LG. However, high concentrations of EGCG can cause liver toxicity

Method used

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  • 3MH (3-mercapto-1-hexanol)-EGCG (epigallocatechin gallate) nanoparticle solution system and preparation method thereof
  • 3MH (3-mercapto-1-hexanol)-EGCG (epigallocatechin gallate) nanoparticle solution system and preparation method thereof
  • 3MH (3-mercapto-1-hexanol)-EGCG (epigallocatechin gallate) nanoparticle solution system and preparation method thereof

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Experimental program
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Effect test

Embodiment 1、3

[0032] The preparation method of embodiment 1, 3MH-EGCG-β-LG nanoparticle solution system, carries out the following steps successively:

[0033] 1), 2g of β-LG and 0.1g of 3MH were dissolved in 1L of pH 6.5 phosphate buffer solution, and the shaker was shaken at 200rpm / min at room temperature overnight to fully dissolve to obtain β-LG+3MH solution.

[0034] 2) 1.5 g of EGCG was dissolved in 1 L of pH 6.5 phosphate buffer to obtain an EGCG solution.

[0035] 3) Heat the β-LG+3MH solution obtained in step 1) to 75°C, then add the EGCG solution obtained in step 2) and oscillate ultrasonically (FS-2000T ultrasonic processor, Shanghai Shengxi Ultrasonic Instrument Co., Ltd.) and mix for 20 seconds Minutes to obtain a well-mixed solution;

[0036] 4) Cool the above well-mixed solution to 25° C. with a water bath to obtain a 3MH-EGCG-β-LG nanoparticle solution system.

[0037] Example 1 obtained nanoparticles with an average particle size of 35.2nm, an inhibition rate of 60-80% to...

Embodiment 2、3

[0038] The preparation method of embodiment 2, 3MH-EGCG-β-LG nanoparticle solution system, carries out the following steps successively:

[0039] 1), 2g of β-LG and 0.2g of 3MH were dissolved in 1L of pH 6.5 phosphate buffer solution, and shaken at room temperature at 200rpm / min overnight to fully dissolve; β-LG+3MH solution was obtained.

[0040] 2) Dissolve 2 g of EGCG in 1 L of pH 6.5 phosphate buffer to obtain an EGCG solution.

[0041] 3), heat the β-LG+3MH solution obtained in step 1) to 75°C, then add the EGCG solution obtained in step 2), and mix with ultrasonic vibration (FS-2000T ultrasonic processor, Shanghai Shengxi Ultrasonic Instrument Co., Ltd.) for 20 seconds, must be thoroughly mixed;

[0042] 4) Cool the above well-mixed mixture to 25° C. with a water bath to obtain 3MH-EGCG-β-LG nanoparticles.

[0043] The average particle diameter of this nanoparticle is 33.6nm, and the inhibition rate to the proliferation of three cancer cells is 55-70%. Without adding 3...

Embodiment 3、3

[0044] The preparation method of embodiment 3, 3MH-EGCG-β-LG nanoparticles, carries out the following steps successively:

[0045] 1), 2g of β-LG and 0.05g of 3MH were dissolved in 1L of pH 6.5 phosphate buffer solution, and shaken at room temperature at 200rpm / min overnight to fully dissolve; β-LG+3MH solution was obtained.

[0046] 2) Dissolve 1 g of EGCG in 1 L of pH 6.5 phosphate buffer to obtain an EGCG solution.

[0047] 3) Heat the β-LG+3MH solution obtained in step 1) to 75°C, then add the EGCG solution obtained in step 2) and oscillate ultrasonically (FS-2000T ultrasonic processor, Shanghai Shengxi Ultrasonic Instrument Co., Ltd.) and mix for 20 seconds clock, must be thoroughly mixed;

[0048] 4) Cool the above well-mixed mixture to 20°C with a water bath to obtain 3MH-EGCG-β-LG nanoparticles.

[0049]The average particle diameter of this nanoparticle is 30.1nm, and the inhibition rate to the proliferation of three cancer cells is 53-65%. Without adding 3MH, the co...

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Abstract

The invention provides a 3MH (3-mercapto-1-hexanol)-EGCG (epigallocatechin gallate) nanoparticle solution system capable of improving the EGCG stability and bioavailability, and a preparation method of the solution system. The 3MH-EGCG nanoparticle solution system contains 3MH-EGCG-beta-LG nanoparticles formed by EGCG, 3MH and beta-lactoglobulin; the solution is a buffer solution with the pH being 6.5 to 7.0; the concentration of the EGCG is 0.5 to 1g / L; the concentration of the 3MH is 0.025 to 0.1g / L; the concentration of the beta-lactoglobulin is 1g / L. 3MH is added into a nanometer system formed by the beta-LG and the EGCG; the characteristics that the 3MH has high reducibility, and the structure body of the 3MH is similar to the amino acid structure are utilized for protecting the EGCG from oxidative degradation, so that the action efficiency of the EGCG is improved; the antitumor activity of the EGCG in vitro and in vivo is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an EGCG nanoparticle solution system and a preparation method thereof. Background technique [0002] The structural formula of EGCG is as follows: [0003] [0004] EGCG (epigallocatechin gallate) is a widely studied chemical component with potential anticancer activity and has tumor suppressor activity in all stages of tumor formation. Most in vitro studies have found that EGCG can act on related molecular targets and affect disease-related cellular processes only at relatively high concentrations. In the in vitro study, the concentration of EGCG is quite high, 1-2 orders of magnitude higher than the concentration of EGCG in the blood after oral administration into the human body; secondly, EGCG is easy to oxidize itself, for example, the loss of EGCG can reach 10% in one day at 37°C. Therefore, improving the stability and bioavailability of EGCG is one of the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/20A61K47/42A61K9/08A61K31/353A61P35/00
Inventor 杜琪珍祁洁徐颖磊王凯吴敏
Owner ZHEJIANG FORESTRY UNIVERSITY
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