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Extraction method of hyperin and application thereof in medicament preparation

A technology of hyperin and extraction method, which is applied in the direction of drug combination, preparation of sugar derivatives, chemical instruments and methods, etc., and can solve the problems of undiscovered inhibition of influenza virus infection, replication, undiscovered, etc.

Active Publication Date: 2010-11-24
JIANGXI SHANXIANG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has not been found that it has the effect of inhibiting influenza virus infection and replication, nor has it been found that it has the effect of inhibiting neuraminidase, and hyperin is extracted from the traditional Chinese medicine hollyhock flower, as mentioned in the application number 200810195922.7

Method used

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  • Extraction method of hyperin and application thereof in medicament preparation
  • Extraction method of hyperin and application thereof in medicament preparation
  • Extraction method of hyperin and application thereof in medicament preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Take 1000g of the round leaves of Shanxiang, add 12 times the amount of 70% ethanol for reflux extraction for 2 hours, filter, add 10 times the amount of 70% ethanol for reflux extraction for 1.5 hours, filter, combine the two extracts, recover the ethanol, and pass the aqueous solution through the The treated D101 macroporous resin column was eluted with water, 10% ethanol, 45% ethanol, and 1% sodium hydroxide solution respectively, and the eluted part of 45% ethanol was collected, concentrated under reduced pressure, and dried to obtain more than 30% Hypericum The mixed total glycosides of glycosides were separated by silica gel column chromatography and Sephadex LH-20 column chromatography, and the hyperin fractions were combined and crystallized to obtain pure hyperin (0.75g, purity: 98.5%). UV, IR, ESI-MS, 1 H-NMR, 13 C-NMR comparison confirmed the structure of hyperin.

Embodiment 2

[0031]Take 1000g of the round leaves of Shanxiang, add 15 times the amount of 60% ethanol for reflux extraction for 2 hours, filter, add 9 times the amount of 60% ethanol for reflux extraction for 2 hours, filter, combine the two extracts, recover the ethanol, and pass the aqueous solution through the The treated D101 macroporous resin column was eluted with water, 8% ethanol, 40% ethanol, and 1.2% sodium hydroxide solution, and the 40% ethanol eluted part was collected, concentrated under reduced pressure, and dried to obtain more than 30% Hypericum The mixed total glycosides of glycosides were separated by silica gel column chromatography and Sephadex LH-20 column chromatography, and the hyperin fractions were combined and crystallized to obtain pure hyperin (0.82g, purity: 98.7%). UV, IR, ESI-MS, 1 H-NMR, 13 C-NMR comparison confirmed the structure of hyperin.

Embodiment 3

[0033] Take 1000g of the round leaves of Shanxiang, add 9 times the amount of 65% ethanol for reflux extraction for 2 hours, filter, add 9 times the amount of 65% ethanol for reflux extraction for 1.5 hours, filter, combine the two extracts, recover the ethanol, and pass the aqueous solution through the The treated D101 macroporous resin column was eluted with water, 5% ethanol, 35% ethanol, and 0.8% sodium hydroxide solution respectively, and the eluted part with 35% ethanol was collected, concentrated under reduced pressure, and dried to obtain more than 30% Hypericum The mixed total glycosides of glycosides were separated by silica gel column chromatography and Sephadex LH-20 column chromatography, and the hyperin fractions were combined and crystallized to obtain pure hyperin (0.73g, purity: 98.4%). UV, IR, ESI-MS, 1 H-NMR, 13 C-NMR comparison confirmed the structure of hyperin.

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Abstract

The invention relates to an extraction method of hyperin and application thereof in medicament preparation. The extraction method of the hyperin comprises the following steps: placing Turpinia formosana leaves or Hypericum perforatum in 30%-90% ethanol of 5-15 times, carrying out reflux extraction for 1-3 times, and filtering, wherein the reflux extraction of each time is carried out for 1-3 hours; merging the filtrates, recovering the ethanol, eluting the aqueous solution with a macroporous adsorption resin column, collecting eluted parts, carrying out depressurized concentration, and drying to obtain mixed total glycoside of the hyperin; and carrying silicagel column chromatography and Sephadex LH-20 column chromatography separation, merging hyperin fractions, and crystallizing to obtain the pure hyperin product. The hyperin can be used as a neuraminidase inhibitor for preventing and treating flu, and can be prepared into pharmaceutically acceptable dosage forms.

Description

technical field [0001] The invention relates to a method for extracting hyperin and its application for preparing medicine. Background technique [0002] At present, influenza virus is becoming more and more serious, and influenza virus is closely related to respiratory diseases and systemic diseases caused by it. my country is one of the countries with high incidence of influenza. Not only has a large population, but also living habits are conducive to the transmission of influenza virus. The average number of episodes ranged from 0.3 to 0.7, and 2 to 4 in key groups. Influenza poses a serious threat to human beings, especially the emerging strains of influenza virus, which not only cause secondary infections of other microorganisms, but also directly lead to organ damage and allergic reactions leading to death. But there is no effective method and treatment means for treating influenza virus and its disease (influenza) at present, such as treating the inflammatory response...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H1/08A61K31/7048A61P31/16A61P13/12A61P1/00A61P11/00
Inventor 杨小玲谢宁叶劲英李志勇吕武清刘地发程帆蔡永红
Owner JIANGXI SHANXIANG PHARMA
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