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Ginsenoside R10, extraction method and pharmaceutical use thereof

A technology of ginsenoside and extraction method, applied in the field of ginsenoside R10 and its extraction, can solve the problems of short half-life, systemic internal bleeding of patients, and high production cost, and can reduce the generation of MDA, slow down energy metabolism, and improve hypoxia tolerance. Effect

Active Publication Date: 2012-08-15
吉林圣亚医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In practical application, they are all injectable drugs, which may cause systemic internal bleeding in patients, and have a short half-life in vivo and high production costs

Method used

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  • Ginsenoside R10, extraction method and pharmaceutical use thereof
  • Ginsenoside R10, extraction method and pharmaceutical use thereof
  • Ginsenoside R10, extraction method and pharmaceutical use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Take American ginseng stems and leaves, add 3 times the amount of water, extract 5 times, 6 hours each time, combine the extracts, concentrate under reduced pressure, add CHCl 3 Extract 5 times, take the water layer, continue to add n-BuOH to extract 5 times, combine the n-BuOH layers, concentrate under reduced pressure, to dryness, dissolve in 10 times the volume of propylene glycol, and hydrolyze at 180 degrees under 15% alkaline conditions After 12 hours, the hydrolyzate was diluted with an equal volume of water, and neutralized to pH 7; then added to D101 macroporous adsorption resin, rinsed with water first, and then eluted with 70% EtOH, collected the EtOH eluate, and recovered the solvent until dry, the part was subjected to repeated silica gel column chromatography, eluent: CHCl 3 -MeOH (100:1), the eluent was subjected to RP-HPLC, and the mobile phase was MeOH-H 2 O (55:45), the compound with a retention time of 45 min was retained, which was ginsenoside R10. ...

Embodiment 2

[0030] Take American ginseng stems and leaves, add 4 times the amount of water, extract 5 times, 4 hours each time, combine the extracts, concentrate under reduced pressure, add CHCl 3 Extract 4 times, take the water layer, continue to add n-BuOH to extract 3 times, combine the n-BuOH layers, concentrate under reduced pressure, until dry, dissolve in 10 times the volume of propylene glycol, and hydrolyze at 180 degrees under 15% alkaline conditions After 12 hours, the hydrolyzate was diluted with an equal volume of water and neutralized to Ph7. Then add D101 macroporous adsorption resin, first wash with water, then add 85% EtOH to elute, collect the EtOH eluate, recover the solvent, until dry, and repeat silica gel column chromatography for this part, eluent: CHCl 3 -MeOH 110:1, the eluent was subjected to RP-HPLC, and the mobile phase was MeOH-H 2 O (65:30), the compound with a retention time of 35 min was retained, which was ginsenoside R10.

Embodiment 3

[0032] Take American ginseng stems and leaves, add 5 times the amount of water, extract twice, 3 hours each time, combine the extracts, concentrate under reduced pressure, add CHCl 3 Extract 2 times, take the water layer, continue to add n-BuOH to extract 2 times, combine the n-BuOH layers, concentrate under reduced pressure, until dry, dissolve in 10 times the volume of propylene glycol, and hydrolyze at 180 degrees under 15% alkaline conditions After 12 hours, the hydrolyzate was diluted with an equal volume of water and neutralized to pH7. Then add D101 macroporous adsorption resin, rinse with water first, then elute with 95% EtOH, collect the EtOH eluate, recover the solvent, and dry it, and then perform repeated silica gel column chromatography on this part, eluent: CHCl 3 -MeOH 120:1, the eluent was subjected to RP-HPLC, and the mobile phase was MeOH-H 2 O (75:20), the compound with a retention time of 28 min was retained, which was ginsenoside R10.

[0033] Table 1 Gi...

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Abstract

The invention relates to ginsenoside R10, an extraction method and pharmaceutical use thereof, and belongs to a new compound and the pharmaceutical use thereof. The extraction method comprises the following steps: taking stems and leaves of American ginseng, adding 3-5-fold water, extracting for 2-5 times (3-6 hours each time), merging extracting solutions, decompressing and concentrating, addingCHC13, extracting for 2-5 times, taking a water layer, continuously adding n-BuOH, extracting for 2-5 times, merging a n-BuOH layer, decompressing and concentrating until being dried, dissolving the obtained concentrated solution in propylene glycol with 10-fold volume, hydrolyzing for 12 hours under an alkaline condition (15%) at 180 DEC G, diluting hydrolysate with isometric water, and neutralizing until pH is 7; and adding D101 macroporous adsorbing resin, washing with water, eluting with 70-95% of EtOH, collecting EtOH eluent, recovering a solvent until being dried, carrying out repeated silica gel column chromatography on the recovered solvent with an eluting agent of CHC13-MeOH (100-120:1), carrying out RP-HPLC on the eluent with a mobile phase of MeOH-H2O (55-75:20-45), and preserving a compound retention time of which is 28-45min to obtain the ginsenoside R10. The ginsenoside R10 can be applied to preparing an anti-stroke drug.

Description

technical field [0001] The invention relates to ginsenoside R10, its extraction method, and its application in the preparation of anti-stroke drugs. Background technique [0002] Cerebrovascular disease (CVD) refers to brain lesions caused by various cerebrovascular diseases. It is one of the three major diseases that cause human death. Globally, it kills 4.6 million people every year, of which 1 / 3 occurs in industrialized countries and the rest occurs in developing countries. The disease and death mainly occur in people over 65 years old. Japan is one of the countries with the highest morbidity and mortality rate of stroke, and the mortality rate of cerebrovascular disease has always been the top cause of death. my country is also an area with a high incidence of stroke mortality. It is estimated that 6 million residents suffer from cerebrovascular diseases, 1.3 million new cerebrovascular diseases occur each year, and nearly 1 million people die. Among the survivors, abou...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J17/00A61K31/704A61P9/10
Inventor 李平亚刘金平卢丹刘传贵杜秀娟李丰
Owner 吉林圣亚医药科技有限公司
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