CN1546054A - Application of wolfberry polyose in the preparation process of gastric ulcer treating medicine - Google Patents
Application of wolfberry polyose in the preparation process of gastric ulcer treating medicine Download PDFInfo
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- CN1546054A CN1546054A CNA2003101094277A CN200310109427A CN1546054A CN 1546054 A CN1546054 A CN 1546054A CN A2003101094277 A CNA2003101094277 A CN A2003101094277A CN 200310109427 A CN200310109427 A CN 200310109427A CN 1546054 A CN1546054 A CN 1546054A
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- lbp
- polysaccharide
- lycium barbarum
- barbarum polysaccharide
- gastric ulcer
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Abstract
The invention relates to the use of matrimony vine polysaccharides in preparing medicament for treating gastric ulcer, wherein said matrimony vine polysaccharides are LBP-2 and LBP-4 extracted from matrimony vine, which exhibit substantial inhibitory action to mouse gastric ulcer.
Description
Technical field:
The present invention relates to technical field of pharmaceuticals, be specifically related to the application of lycium barbarum polysaccharide in preparation treatment gastric ulcer medicine.
Background technology:
Fructus Lycii is the dry mature fruit of plant of Solanaceae lycium barbarum Lyeium barbarum.L, is the traditional tonic Chinese medicine of China, and the beginning is stated from Shennong's Herbal.Has nourishing the liver and kidney, the effect of replenishing vital essence to improve eyesight.Find after deliberation, contain polysaccharide, albumen, fat, V in the Fructus Lycii
A, V
B1With trace element and mineral such as aminoacid and calcium, ferrum, germanium.Assist medium report the Meng, identifying has free amino acid in 10 in the lycium barbarum fruit, as aspartic acid, glutamic acid, alanine etc.Contain alkaloids such as atropina, hyoscyamine in the Harsh M I report Fructus Lycii.Report such as Wang Qiang adopts organic solvent and water alcohol method to extract lycium barbarum polysaccharide.Storage is drilled the dream report and is got lycium barbarum polysaccharide I and II, identifies through component and learns the heteropolysaccharide that they are made up of arabinose, glucose, mannose, galactose, xylose and rhamnose, and contain a certain amount of aminoacid.Report lycium barbarum polysaccharide such as Xu Shichen also contain galacturonic acid and protein.Have in recent years many researchs report lycium barbarum polysaccharide have enhancing immunity, anticancer, anti-aging, increase hemopoietic function, prevent multiple biological activity such as genetic damage, but the anti-gastric-ulcer effect does not appear in the newspapers.
Summary of the invention:
Technical problem to be solved by this invention is to develop the new purposes of lycium barbarum polysaccharide, provides the Fructus Lycii acidic polysaccharose to use in preparation treatment gastric ulcer medicine.
Lycium barbarum polysaccharide disclosed by the invention is meant separates LBP-2 and the LBP-4 that obtains from lycium barbarum polysaccharide.Zoopery shows, LBP-2 all has significant inhibitory effect to the mouse gastric ulcer that the mouse gastric ulcer that caused by dehydrated alcohol and indometacin cause, and LBP-4 has significant inhibitory effect to the mouse gastric ulcer that dehydrated alcohol causes.
The present invention at first carries out rat dehydrated alcohol ulcer model to two kinds of dosage groups of two kinds of dosage groups of lycium barbarum polysaccharide macromolecule and lycium barbarum polysaccharide small-molecular weight and suppresses effect relatively, finds that the macromolecule lycium barbarum polysaccharide has the gastric ulcer effect that significant anti-dehydrated alcohol causes.The present invention separates lycium barbarum polysaccharide macromolecule part water, variable concentrations NaCl solution or NaOH solution again then, and obtaining four kinds of polysaccharide components is LBP-1, LBP-2, LBP-3, LBP-4.Further evidence LBP-2 and LBP-4 have significant inhibitory effect to the mouse gastric ulcer that is caused by dehydrated alcohol.Polysaccharide LBP-2 has significant inhibitory effect to the mouse gastric ulcer that is caused by indometacin.The embodiment of the invention 1 is described in detail this.
The existing open report of the separation method of lycium barbarum polysaccharide LBP-2 and LBP-4, " Hua Zhong Agriculture University's journal " 1996; 15 (6): Sun Zhi such as reaches at extraction, separation and the Study on Physico-chemical of having reported lycium barbarum polysaccharide among the 603-607.Wherein lycium barbarum polysaccharide LBP-2 and separating of LBP-4 are: get the dried wolfberry fruit, add extraction solvent and extract, extract concentrates, and adds a certain amount of precipitant, and standing over night is got precipitation and is dissolved in water redeposition once; Precipitation adds a certain amount of water dissolution, and the Sevag method is removed floating preteins; Lyophilization gets the Fructus Lycii crude polysaccharides, yield about 5%.The Fructus Lycii total sugar packed into dialyses in the bag filter, after the dialyzed solution drying macromolecular polysaccharide.With chromatographic column on the large molecular weight polysaccharides, with the eluant gradient elution of variable concentrations, every pipe 8ml collects with automatic collector, sulphuric acid-anthrone method pipe detects, and makes elution curve, merges mountain portions, concentrate drying is got wherein two polysaccharide partial L BP-2, LBP-4, promptly.
Extraction solvent described in the said method is water or 50% following ethanol; Described precipitant is 65-95% alcoholic solution or 65-95% methanol solution; Described chromatographic column inner stuffing can be active carbon, macroporous resin, DEAE-cellulose, silica gel; Described eluant is water, 50-95% ethanol, 0.01-1mol/l NaCL or 0.01-1mol/l NaOH solution.
As the medicine of treatment gastric ulcer, lycium barbarum polysaccharide LBP-2 of the present invention, LBP-4 can be made into various forms of oral formulations and comprise tablet (containing intra-gastric floating tablet), capsule, granule or oral liquid etc.
Described pharmaceutical preparation is that 20-30% Lycium barbarum polysaccharide extract and 80-70% pharmaceutic adjuvant or additives are formed by percentage by weight preferably.
The specific embodiment:
Embodiment 1, the screening of lycium barbarum polysaccharide anti-gastric-ulcer active site
(1) effect of lycium barbarum polysaccharide anti-gastric-ulcer, result
Adopting the method for dialysis earlier, lycium barbarum polysaccharide is divided into macromolecule part and small-molecular weight part, is that index is screened with the inhibition effect to rat dehydrated alcohol ulcer model.Select body weight 160-200gSD rat for use, male and female half and half, be divided into 6 groups at random: normal saline group (NS group), positive controls (sucralfate group, 250mg/kg), large molecular weight polysaccharides (greater than 8000 molecular weight) dosage I group (500mg/kg) and dosage II group (250mg/kg), small-molecular weight sugar (less than 8000 molecular weight) dosage I group (500mg/kg) and dosage II group (250mg/kg).Successive administration seven days, the mouse fasting is 24 hours before the last administration, freely drinks water during the fasting, and last administration was irritated stomach with dehydrated alcohol after 1 hour, and dosage is every 1ml/200g.After 1 hour, rat is taken off neck put to death.Cut open the belly, cardia is imprisoned in ligation, injects the formalin solution of 10ml4% from pylorus.Get stomach, immerse in the formalin solution fixedly 30min after, cut along greater gastric curvature, can be observed strand and flaky hemorrhage zone.
Take with digital camera under fixed light source, the ipwin32 image analysis software that image adopts Shanghai Univ. of Traditional Chinese Medicine pharmacological toxicology center to provide is calculated its ulcer area index.
Table 1 Fructus Lycii total polysaccharides component is to the inhibition effect of dehydrated alcohol gastric ulcer
Group dosage (mg/kg) N ulcer index suppression ratio (%)
NS group-10 20.84 ± 11.09
Positive controls 250 10 6.64 ± 8.66
*68.10%
Large molecular weight polysaccharides dosage I organizes 500 10 9.08 ± 12.93
*56.40%
Large molecular weight polysaccharides dosage II organizes 250 10 11.68 ± 5.70
*43.90%
Small-molecular weight polysaccharide dosage I organizes 500 10 23.20 ± 12.47
Small-molecular weight polysaccharide dosage II organizes 250 10 23.08 ± 19.38
Compare * * P＜0.01 with the NS group; * P＜0.05
From table data as can be seen, the macromolecule lycium barbarum polysaccharide has the effect of the gastric ulcer that significant antagonism dehydrated alcohol causes.
(2) lycium barbarum polysaccharide macromolecule part antiulcer action The selection result
Adopt chromatographic column to macromolecule part in the lycium barbarum polysaccharide respectively the NaCL solution or the NaOH solution of water, variable concentrations separate, obtain four kinds of polysaccharide component: LPB-1, LBP-2, LBP-3, LBP-4.Inhibition effect with mice dehydrated alcohol ulcer model is an index, investigates each component antiulcer effect.Get Kunming mouse, male, body weight 25-40g is divided into 6 groups at random: normal saline group (NS group), positive controls (sucralfate group, 100mg/kg), LPB-1 organizes (250mg/kg), and LBP-2 organizes (250mg/kg), LBP-3 organizes (250mg/kg), LBP-4 organizes (250mg/kg), and modeling method is the same substantially, and the dosage of dehydrated alcohol is 0.1ml/20g.Index evaluation adopts scoring method.1) the long note of every 1mm is 1 minute; 2) width surpasses 1mm, then will be at the score value of the corresponding superior width of score value; 3) length is no more than the note 0.5 minute of 1mm; 4) last score value is added up by each ulcer zone score value and obtains
Table 2 polysaccharide component is to the inhibition effect of dehydrated alcohol gastric ulcer
Group dosage (mg/kg) N ulcer index suppression ratio (%)
NS group-10 62.70 ± 50.07
Positive controls 100 8 22.31 ± 17.36
*64.4%
LBP-1 250 10 35.05±27.33 44.1％
LBP-2 250 10 14.00±10.22
* 77.7％
LBP-3 250 10 26.85±27.90 57.2％
LBP-4 250 10 12.50±11.82
* 80.1％
Compare * P＜0.05 with the NS group
From table data as can be seen, the mouse gastric ulcer that four kinds of polysaccharide components all cause dehydrated alcohol has certain inhibitory action, but compares with the normal saline group, has only LBP-2 and LBP-4 that significant difference is arranged.
With the inhibition effect that indometacin is caused mouse gastric ulcer is index, continues to investigate three kinds of polysaccharide: LBP-2 that dehydrated alcohol ulcer model had certain inhibition effect, LBP-3, LBP-4.Positive controls is a ranitidine, and by preceding method administration, fasting, 30min after the last administration to mouse peritoneal injection indometacin 20mg/kg, puts to death behind the 6h, gets stomach, and is fixing, estimates the ulcer index with scoring method.
Three kinds of polysaccharide components of table 3 are to the inhibition effect of indometacin gastric ulcer
Group dosage (mg/kg) N ulcer index suppression ratio (%)
NS group-15 9.07 ± 9.07
Ranitidine group 100 15 1.77 ± 3.67
*80.5%
LBP2 250 15 3.20±3.80
* 64.7％
LBP3 250 15 9.17±7.05
LBP4 250 15 4.77±4.14
* 47.4％
Compare * P＜0.05 with the NS group
From the table data as can be seen, the mouse gastric ulcer that LBP-2 and LBP-4 cause indometacin has certain inhibition effect, but compares with the normal saline group, has only LBP-2 that significant difference is arranged.
The preparation of embodiment 2, Lycium barbarum polysaccharide extract
Get the dried wolfberry fruit, extracting in water, twice totally; Merge the water extract, concentrate; Add 4 times of amount 80% ethanol, standing over night is got precipitation and is dissolved in water precipitate with ethanol once again; Precipitation adds a certain amount of water dissolution, and the Sevag method is removed floating preteins; Lyophilization gets the Fructus Lycii crude polysaccharides, yield about 5%.The Fructus Lycii total sugar packed into dialyses in the bag filter, after the dialyzed solution drying macromolecular polysaccharide.With activated-charcoal column on the large molecular weight polysaccharides, with 0.01-1mol/l NaCL gradient elution, every pipe 8ml collects with automatic collector, sulphuric acid-anthrone method pipe detects, and makes elution curve, merges mountain portions, concentrate drying is got wherein two polysaccharide partial L BP-2, LBP-4, promptly.
The preparation of embodiment 3 lycium barbarum polysaccharide intra-gastric floating tablet
Lycium barbarum polysaccharide LBP-2 and LBP-4 10 grams, HPMC, octadecanol, magnesium stearate, totally 40 grams.Preparation: with principal agent and the abundant mix homogeneously of adjuvant, cross 100 mesh sieves, add binding agent and make soft material, cross 16 mesh sieves and granulate 40 ℃ of dryings, granulate.Add magnesium stearate and make lubricant, mix the back tabletting, make 100 altogether, every 0.5 gram.
The capsular preparation of embodiment 4 lycium barbarum polysaccharide
Lycium barbarum polysaccharide LBP-2 10 grams, totally 40 grams such as starch, dextrin, calcium carbonate etc.; Preparation: principal agent and the abundant mix homogeneously of adjuvant is encapsulated, make 100 every 0.5 gram altogether, get final product.The preparation of embodiment 5 lycium barbarum polysaccharide granules
Lycium barbarum polysaccharide LBP-4 10 grams, starch, dextrin, Icing Sugar etc., totally 90 grams; Preparation: with principal agent and the abundant mix homogeneously of adjuvant, make soft material in right amount, granulate with the ethanol of debita spissitudo, drying, granulate, packing, every bag 1 gram is made 100 bags altogether, gets final product.
The preparation of embodiment 6 lycium barbarum polysaccharide oral liquids
Lycium barbarum polysaccharide LBP-2 and LBP-4 10 grams; Other gets sucrose 500 and restrains into syrup, adds fully dissolving such as principal agent, antiseptic, filter, and fill, every 5ml, totally 100 get final product.
Claims (4)
1, lycium barbarum polysaccharide is used in preparation treatment gastric ulcer medicine.
2, application according to claim 1 is characterized in that wherein said lycium barbarum polysaccharide is LBP-2 or LBP-4.
3, application according to claim 2 is characterized in that wherein said LBP-2 or LBP-4 are obtained by following step: get the dried wolfberry fruit, add extraction solvent and extract, extracting solution concentrates, add a certain amount of precipitant, standing over night is got precipitation and is dissolved in water redeposition once; Precipitation adds a certain amount of water dissolution, and the Sevag method is removed floating preteins; Lyophilization gets the Fructus Lycii crude polysaccharides; The Fructus Lycii total sugar packed into dialyses in the bag filter, after the dialyzed solution drying macromolecular polysaccharide.With chromatographic column on the large molecular weight polysaccharides, with the eluant gradient elution of variable concentrations, every pipe 8ml collects with automatic collector, sulphuric acid-anthrone method pipe detects, and makes elution curve, merges mountain portions, concentrate drying is got wherein two polysaccharide partial L BP-2, LBP-4, promptly;
Wherein extraction solvent is water or 50% following ethanol; Precipitant is 65-95% alcoholic solution or 65-95% methanol solution; The chromatographic column inner stuffing can be active carbon, macroporous resin, DEAE-cellulose or silica gel; Described eluant is water, 50-95% ethanol, 0.01-1mol/lNaCL or 0.01-1mol/l NaOH solution.
4, application according to claim 1 is characterized in that wherein said medicine is the oral formulations that 20-30% Lycium barbarum polysaccharide extract and 80-70% pharmaceutic adjuvant or additives are formed by percentage by weight.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102949409A (en) * | 2012-11-08 | 2013-03-06 | 合肥工业大学 | Application of using lachnum exopolysaccharide to prepare medicine for preventing gastric ulcer |
| CN103030708A (en) * | 2012-12-13 | 2013-04-10 | 大兴安岭林格贝有机食品有限责任公司 | Novel purification method of lycium chinense polysaccharide |
| CN103044569A (en) * | 2013-01-15 | 2013-04-17 | 上海诺德生物实业有限公司 | Wolfberry extract containing wolfberry acid and preparation method thereof |
-
2003
- 2003-12-15 CN CN 200310109427 patent/CN1257716C/en not_active Expired - Fee Related
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102949409A (en) * | 2012-11-08 | 2013-03-06 | 合肥工业大学 | Application of using lachnum exopolysaccharide to prepare medicine for preventing gastric ulcer |
| CN102949409B (en) * | 2012-11-08 | 2014-10-08 | 合肥工业大学 | Application of using lachnum exopolysaccharide to prepare medicine for preventing gastric ulcer |
| CN103030708A (en) * | 2012-12-13 | 2013-04-10 | 大兴安岭林格贝有机食品有限责任公司 | Novel purification method of lycium chinense polysaccharide |
| CN103030708B (en) * | 2012-12-13 | 2016-04-13 | 大兴安岭林格贝寒带生物科技股份有限公司 | A kind of Novel purification method of lycium barbarum polysaccharide |
| CN103044569A (en) * | 2013-01-15 | 2013-04-17 | 上海诺德生物实业有限公司 | Wolfberry extract containing wolfberry acid and preparation method thereof |
| CN103044569B (en) * | 2013-01-15 | 2015-08-19 | 上海诺德生物实业有限公司 | Wolfberry fruit extract containing matrimony vine acid and preparation method thereof |
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| CN1257716C (en) | 2006-05-31 |
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