Application of sakuranetin and derivatives thereof in preparation of anti-H5N1 virus medicament

The technology of a derivative, sakuratin, is applied in the application field of sakuratin and its derivatives in the preparation of anti-H5N1 virus drugs, can solve the problems such as the undiscovered anti-H5N1 virus of sakuratin and its derivatives, and achieves strong pharmacological effects, The effect of high yield and rich source of raw materials

Inactive Publication Date: 2013-07-10
中国人民解放军防化学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Through literature search, etc., no report on the use of sakurain and its derivatives for anti-H5N1 virus has been found so far.

Method used

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  • Application of sakuranetin and derivatives thereof in preparation of anti-H5N1 virus medicament
  • Application of sakuranetin and derivatives thereof in preparation of anti-H5N1 virus medicament
  • Application of sakuranetin and derivatives thereof in preparation of anti-H5N1 virus medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1, cherry blossom element extraction and purification

[0031] Hydrangea (Galium aparine L) whole herb 60kg, cold soaked with 480kg of 60% ethanol and extracted 3 times (3 days / time), the extracts were combined, the ethanol was recovered until there was no alcohol smell, and petroleum ether, chloroform, ethyl acetate were used successively Ester, n-butanol extraction, decompression recovery solvent to obtain n-butanol extract 210g, n-butanol extract 1.2L deionized water dissolved and filtered, through macroporous resin AB-8 type column chromatography, followed by water, 25% ethanol , 50% ethanol, 95% ethanol for elution, and the eluents of the above parts were concentrated under reduced pressure respectively to obtain 80 g of water eluate, 22 g of 25% ethanol eluate, 67 g of 50% ethanol eluate, and 95% ethanol eluate. Desiccant 35g. Wherein 25% ethanol eluate (22g) is carried out silica gel column chromatography separation, separates 14 components through th...

Embodiment 2

[0032] Embodiment 2, synthesis and purification of sakurain

[0033]

[0034] Dissolve 20.0g naringenin in 200mL acetone, add K 2 CO 3 15.0g, add (CH 3 ) 2 SO 4 10.0g, heated to reflux for 24h. Filter and spin dry. Purified by 200-300 mesh silica gel column chromatography, eluting with petroleum ether: ethyl acetate = 5:1, to obtain 19.2 g of sakurain with a yield of 91%. See attached for hydrogen spectrum figure 1 .

Embodiment 3

[0035] Synthesis and purification of embodiment 3,7-benzylnaringenin

[0036]

[0037] Dissolve 25.0g naringenin in 500mL acetone, add K 2 CO 3 35.0g, plus 31.0g benzyl bromide, heated to reflux for 24h. Filter and spin dry. Purified by 200-300 mesh silica gel column chromatography, eluting with petroleum ether: ethyl acetate = 2:1, to obtain 23.4 g of sakurain with a yield of 69%. See attached for hydrogen spectrum figure 2 .

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Abstract

The invention relates to a new application of sakuranetin and derivatives thereof in preparation of an anti-highly pathogenic avian influenza (HPAI) H5N1 virus medicament. Experiments prove that the sakuranetin and the derivatives thereof have a good inhibiting and inactivating effect. The anti-H5N1 virus medicament can be prepared by using the compounds as an active ingredient. The anti-virus medicament can be used for clinically preventing and treating influenza viruses, particularly diseases caused by HPAI H5N1 viruses. The compounds are safe, low in toxicity and strong in pharmacologic action; and the raw material sources are rich, wide and cheap, the preparation cost is low, the process is simple, and the yield is high. In order to prevent and treat the influenza viruses, particularly the HPAI H5N1 viruses, the invention provides a new medicament source, which has great practical significance and a broad application prospect in the fields of medicine and bio-pharmaceuticals, particularly in the field of preparation of anti-H5N1 virus medicaments.

Description

technical field [0001] The present invention relates to the new application of the compound, in particular to the application of sakurain and its derivatives in the preparation of anti-H5N1 virus drugs. Background technique [0002] Since the first outbreak of highly pathogenic avian influenza in Italy in 1878, it has occurred more than 20 times around the world, and each outbreak has caused serious economic losses and social panic. In 1997, the Hong Kong region of my country reported for the first time that the highly pathogenic avian influenza H5N1 virus broke through the interspecies barrier and directly infected humans and caused death. At present, cases of human infection with H5N1 virus have occurred in countries such as Asia, Europe, and Africa, and there is a trend of continuous expansion. H5N1 virus is more pathogenic than common influenza virus, showing typical fulminant viral pneumonia, which can quickly lead to acute respiratory distress syndrome. [0003] Drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/7048A61P31/16
Inventor 李建董俊军王相承
Owner 中国人民解放军防化学院
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