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Preparing method and application of peroxy-ergosterol compound

A technology of peroxyergosterol and compounds, which is applied in the field of medicine, can solve the problems of high price and large drug side effects, and achieve the effects of large preparation volume, high separation precision of fillers, and light environmental pollution

Inactive Publication Date: 2018-03-06
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, acyclovir and its derivatives are the most widely used drugs for the treatment of herpes simplex virus at home and abroad, but these drugs have the disadvantages of large toxic and side effects and relatively expensive prices.

Method used

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  • Preparing method and application of peroxy-ergosterol compound
  • Preparing method and application of peroxy-ergosterol compound
  • Preparing method and application of peroxy-ergosterol compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Take the poria cocos block and grind it into 50 mesh powder, add 80% ethanol (that is, the weight volume ratio of poria cocos coarse powder and 80% ethanol is 1:10 / kg:L) of 10 times the weight volume, and reflux extraction 3 times, each extraction 1 hour. Filtrate, combine the extracts, reclaim ethanol under reduced pressure until there is no alcohol smell, and concentrate to an extract with a relative density of 1.10; the extract is dispersed with water at a weight-to-volume ratio of 1:15 (kg:L) to obtain an aqueous dispersion of the extract, and then used Extracted five times with ethyl acetate equal to the volume of the extract aqueous dispersion; the ethyl acetate extraction layer was concentrated under reduced pressure to obtain a crude extract.

[0032] The crude extract and 60-80 mesh silica gel are mixed according to the weight ratio of 1:1.5, and the sample silica gel is obtained after drying; the 200-300 mesh silica gel is pre-dried into the compressed chromat...

Embodiment 2

[0037] Take Poria cocos block and grind it into 80 mesh powder, add 7 times the weight volume of 85% ethanol, and reflux extraction 4 times, each extraction is 2 hours. Filtrate, combine the extracts, recover ethanol under reduced pressure until there is no alcohol smell, concentrate to an extract with a relative density of 1.30; add water to the extract at a weight-to-volume ratio of 1:15 to obtain an aqueous dispersion of extract, and then disperse with extract water The same volume of ethyl acetate was extracted 8 times; the ethyl acetate extract layer was concentrated under reduced pressure to obtain a crude extract.

[0038] The crude extract and 60-80 mesh silica gel are mixed according to the weight ratio of 1:1.5, and the sample silica gel is obtained after drying; the 200-300 mesh silica gel is pre-dried into the compressed chromatographic column of the dynamic axial industrial preparation chromatograph, Then add the sample silica gel to the sample cavity in the front...

Embodiment 3

[0041] Take the Poria cocos block and grind it into a 60-mesh powder, add 6 times the weight volume of 95% ethanol, heat and reflux for extraction 5 times, and extract for 3 hours each time. Filtrate, combine the extracts, recover ethanol under reduced pressure until there is no alcohol smell, and concentrate to an extract with a relative density of 1.20. The extract was dispersed with water at a weight-to-volume ratio of 1:15 to obtain an aqueous dispersion of the extract, and then extracted 6 times with ethyl acetate equal in volume to the aqueous dispersion of the extract; the ethyl acetate extraction layer was concentrated under reduced pressure to obtain a crude extract.

[0042] The crude extract and 60-80 mesh silica gel are mixed according to the weight ratio of 1:1.5, dried and ground to obtain the sample silica gel; 200-300 mesh silica gel is pre-dried into the compressed column of the dynamic axial industrial preparation chromatograph , and then add the sample silic...

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PUM

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Abstract

The invention discloses a preparing method of a peroxy-ergosterol compound. The preparing method comprises the steps of smashing blocks of poria cocos, conducting reflux extraction 3-5 times, recycling an extracting solution to obtain extract, adding water to disperse the extract, and using ethyl acetate to conduct extraction 5-10 times to obtain a crude extract; using dynamic axial industrially-prepared chromatography to separate the crude extract to obtain a relatively pure product of peroxy-ergosterol; recrystallizing the obtained relatively pure product of peroxy-ergosterol to obtain peroxy-ergosterol of which the purity is larger than 98%. The invention further discloses application of the peroxy-ergosterol compound in preparing a drug for resisting herpes simple virus I. The multiplication of HSV-I in cells can be inhibited, the multiplication of the virus can be 100% inhibited when the concentration of peroxy-ergosterol is 40.12Mug / mL, and the selection index of peroxy-ergosterol in HSV-I is 7.5. As is shown, peroxy-ergosterol can be applied to preparing the drug for resisting the herpes simplex virus-I(HSV-I).

Description

technical field [0001] The invention belongs to the field of medical science and technology, and relates to a peroxyergosterol compound and its preparation method and application. Background technique [0002] Poria, also known as Yuling, Fuling, Wanlinggui, and Poria, is the sclerotia of Poria cocos (Schw.) Wolf, a fungus of the family Polybacteriaceae. It is used for edema, oliguria, phlegm and retention, dizziness and palpitations, spleen deficiency, lack of food, loose stools and diarrhea, restlessness, palpitation and insomnia. [0003] At present, a variety of chemical components have been isolated from Poria cocos, mainly including polysaccharides and terpenoids. In addition, it also contains steroids, fatty acids, proteins, adenine, amino acids and various inorganic elements. Modern pharmacological studies have shown that Poria cocos has the functions of enhancing immunity, delaying aging, anti-tumor, anti-virus, regulating immunity, and anti-inflammation. [0004]...

Claims

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Application Information

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IPC IPC(8): C07J71/00A61K31/58A61P31/22
CPCC07J71/0005
Inventor 萧伟李石平谢雪常秀娟宋亚玲王雪晶赵祎武杨林勇黄文哲王振中
Owner JIANGSU KANION PHARMA CO LTD
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