Hyaluronidase inhibitor as well as preparation method and use thereof

A hyaluronidase and inhibitor technology, applied in the field of chemistry, can solve the problems of cumbersome separation and purification process, high polarity and high cost, and achieve the effects of no solvent residue, prevention and improvement of inflammation, and low cost.

Inactive Publication Date: 2009-07-15
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the high cost of mass production
So far, there are no reports of the inhibitory effect of 1,2,3,4,6-penta-O-galloyl-β-D-glucose (PGG) on hyaluronidase activity; currently, PGG is mainly isolated from plant extracts Purification, but because PGG is a hydrolyzed tannin with good water solubility, there are problems such as large polarity, complicated separation and purification process, and low yield. So far, there is no preparation process for industrialized batch production of PGG with tannic acid as raw material

Method used

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  • Hyaluronidase inhibitor as well as preparation method and use thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The specific steps for the preparation of 1,2,3,4,6-penta-O-galloyl-β-D-glucose and its activity determination in the present invention are as follows:

[0044] (1) Dissolve tannic acid in methanol-water solution containing HAc-NaAc buffer solution (PH=6), and hydrolyze in a water bath at 50° C. for 12 hours in a sealed manner.

[0045] (2) The above hydrolyzate was evaporated to dryness under reduced pressure at 48°C, dissolved in methanol, and then slowly poured into the upper end of a Sephadex column (such as: Sephadex LH-20, etc.) chromatography column. About 100g of tannic acid is loaded on a 41×6.4cm column material. Use methanol for elution, and the elution flow rate is controlled at about 2 mL / min. The eluate enriched in 1,2,3,4,6-penta-O-galloyl-β-D-glucose was collected, concentrated, and dried to obtain crude PGG, whose purity was greater than 85% as determined by HPLC.

[0046] (3) Dissolve the above-mentioned 1,2,3,4,6-penta-O-galloyl-β-D-glucose crude pr...

Embodiment 2

[0069] (1) Weigh 90g of industrial tannic acid, prepare a solution with 135mL of HAc-NaAc buffer solution with pH=6.0, and 1.2L of methanol, and hydrolyze it in a water bath at 50°C for 12 hours.

[0070] (2) The hydrolyzate was evaporated to dryness under reduced pressure at 48°C, dissolved in a small volume of methanol, and then slowly poured into the upper end of a Sephadex LH-20 chromatography column. Use methanol for elution, and the elution flow rate is controlled at about 2 mL / min. The eluate enriched in 1,2,3,4,6-penta-O-galloyl-β-D-glucose was collected, concentrated, and dried to obtain crude PGG, whose purity was greater than 85% as determined by HPLC.

[0071] (3) Dissolve the above-mentioned 1,2,3,4,6-penta-O-galloyl-β-D-glucose crude product in a small volume of aqueous solution and slowly pour it into a macroporous adsorption resin (such as: Diaion HP20, D- 101, KB-8, etc.) the upper end of the chromatography column. First, gradient elution with water, 10%, 20...

Embodiment 3

[0076] Tablet: 10 mg of the compound 1,2,3,4,6-penta-O-galloyl-β-D-glucose obtained in Example 2, 180 mg of lactose, 55 mg of starch, and 5 mg of magnesium stearate;

[0077] Preparation method: mix the compound, lactose and starch, moisten it evenly with water, sieve the wetted mixture and dry it, then sieve it, add magnesium stearate, then press the mixture into tablets, each tablet weighs 250mg, and the compound content is 10mg .

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Abstract

The invention provides a new method for preparing 1, 2, 3, 4, 6-five-O-galloyl-Beta-D- glucose (PGG) by using tannin and the new use thereof. The tannin is hydrolyzed by acid to prepare a PGG crude product, and chromatographic separation and purification are then carried out on the PGG crude product by macroporous absorbent resin and hyskon gel columns to obtain PGG with the purity quotient more than 90 percent. The PGG prepared by the method has good colour and lustre, high purity quotient, simple, safe and easy preparation process, low cost, short production period and easy batch preparation and commercial process. The activity rating shows that the inhibited effect (IC50 0.01mM) of the PGG for the activity of hyaluronate lyase is obviously higher than that of positive control cromolyn sodium (IC50 6.99mM), and the PGG can be directly used as a raw material or the additive of medicine, health food and cosmetics.

Description

Technical field: [0001] The present invention relates to the field of chemistry, in particular to hyaluronidase inhibitors or cosmetics or health products or medicines with 1,2,3,4,6-penta-O-galloyl-β-D-glucose as active ingredients , and its preparation method and its application in the preparation of hyaluronidase inhibitors or cosmetics or health care products or medicines. Background technique: [0002] 1,2,3,4,6-penta-O-galloyl-β-D-glucose (1,2,3,4,6-penta-O-galloyl-β-D-glucose, PGG) is hydrolyzed mono Ning, a gallic acid tannin formed by linking glucose and 5 gallic acids through ester bonds. Pharmacological studies have shown that the compound has various physiological activities, such as anti-tumor, anti-virus, anti-oxidation, antagonism of endotoxin / lipopolysaccharide, hypoglycemic and fat-removing, etc. However, there is no report on the inhibitory effect on hyaluronidase so far. [0003] Hyaluronidase is a specific lyase of hyaluronic acid, and hyaluronic acid ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7024C07H13/08A61P35/00A61P31/12A61P39/06A61P3/10A61P3/00A61P37/08A61P29/00A61Q19/00A23L1/30
Inventor 张颖君刘青乔春玲许敏杨崇仁
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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