CN104825520A - Medicinal application and preparation method of Kamaziriyousi (dcroptiol repens) acetyl cholinesterase-inhibiting active extract and composition thereof - Google Patents

Medicinal application and preparation method of Kamaziriyousi (dcroptiol repens) acetyl cholinesterase-inhibiting active extract and composition thereof Download PDF

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Publication number
CN104825520A
CN104825520A CN201510058758.5A CN201510058758A CN104825520A CN 104825520 A CN104825520 A CN 104825520A CN 201510058758 A CN201510058758 A CN 201510058758A CN 104825520 A CN104825520 A CN 104825520A
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petroleum ether
extract
ethyl acetate
diligent
eluting
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Inventor
热娜·卡斯木
王金辉
李国玉
黄健
李理
胡君萍
曹苑
张珂
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Xinjiang Medical University
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Xinjiang Medical University
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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of a kamaziriyousi (dcroptiol repens) acetyl cholinesterase-inhibiting active extract and a composition thereof, and a medical application of the extract and the composition in treatment of Alzheimer's diseases (AD) and the like. The preparation method comprises following steps: (1) performing elution with petroleum ether; (2) performing elution with a petroleum ether-ethyl acetate mixed solvent, wherein the volume ratio of petroleum ether to ethyl acetate is 100:1; (3) performing solvent recycling to the elution solution after the petroleum ether-ethyl acetate mixed solvent according to the volume ratio of 100:1 in the step (2); and (4) drying a product to obtain the acetyl cholinesterase-inhibiting active extract.

Description

Block medical usage and the preparation method of numb diligent You Si inhibiting activity of acetylcholinesterase, extract and compositions thereof
Technical field
The invention belongs to medical art, be specifically related to a kind of block numb diligent You Si inhibiting activity of acetylcholinesterase, extract and compositions thereof preparation method and its medical usage in treatment Alzheimer (AD) etc.
Background technology
This product be feverfew Herba Acroptili repentis Dcroptiol repens (L.) Dc dry fruit the present invention by a large scale, systematically screening active ingredients, be surprised to find that the Uigurs medicine card diligent You Si extract of fiber crops and partial chemical component thereof, have inhibiting activity of acetylcholinesterase, significantly, this activity extract and compositions thereof are expected to the medical usage being applied to the aspects such as treatment Alzheimer (AD).
Summary of the invention
Technical problem solved by the invention is to provide the numb diligent You Si extract of a kind of card.
Present invention also offers the compositions that the numb diligent You Si extract of card is main active.
Invention also provides the preparation of the numb diligent You Si extract of card and compositions thereof and the application in treatment Alzheimer (AD).
The present invention is achieved through the following technical solutions:
The diligent You Si of Uigurs medicine card fiber crops through methanol supersound extraction, after extracting solution is concentrated, with silica gel (SiO 2) post separation, silicagel column after loading, with petroleum ether-ethyl acetate mixed solvent gradient elution (petroleum ether-ethyl acetate, ratio is in table 1), each petroleum ether-ethyl acetate ratio mixed solvent eluent, concentrated, after drying, in-vitro screening system is utilized to test its inhibiting activity of acetylcholinesterase, be surprised to find that and first use petroleum ether eluting, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) the petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate that obtains of eluting, 100:1, volume ratio) eluent through reclaim organic solvent, dry, be inhibiting activity of acetylcholinesterase, extract.And the eluting position of other ratios, there is no the effect of inhibiting activity of acetylcholinesterase.Especially, preferably first use petroleum ether eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting 30 times of column volumes, eluent drying is the extract of inhibiting activity of acetylcholinesterase, of the present invention afterwards, and it can obtain enrichment by above method, thus separates with other impurity constituents.The diligent You Si inhibiting activity of acetylcholinesterase, extract of these card fiber crops is from having no bibliographical information, its thin layer spectrum color spectrum (TLC) analysis and characterization is as Fig. 1, TLC analysis condition: GF254 silica gel plate, development system: petroleum ether: ethyl acetate: acetone (3:1:1) coloration method: vanillin-sulfuric acid develops the color.
Specifically, discovery procedure is as follows:
1, the preparation of numb diligent You Si through methanol sonicated extract is blocked
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, obtain extract A (methanol extraction): 1.2752 g; B(macroporous resin treatment): 0.3269 g, merging keeps sample: 0.4165 g, silicagel column on remaining sample (1.1856 g).
Petroleum ether-ethyl acetate system elutions.
2, petroleum ether-ethyl acetate mixed solvent gradient elution method and result
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, obtain extract SN0050, A (methanol extraction): 1.2752 g; B(macroporous resin treatment): 0.3269 g, merging keeps sample: 0.4165 g, and on remaining sample, (1.1856 g), applied sample amount: 1.1856 g for silicagel column; Mix sample silica gel: 1.5 g; Blank silica gel 10 g; , petroleum ether-ethyl acetate system gradient elution (condition is in table 1), a column volume is 29 ml; Pillar internal diameter: 2 cm, each gradient elution 200 mL, obtain, each concentration extracts the eluate of eluent, recycling design, obtain, petroleum ether: ethyl acetate gradient extract, TLC analysis result is shown in Fig. 2, TLC analysis condition: GF254 silica gel plate, development system:, petroleum ether: ethyl acetate: acetone (3:1:1) coloration method: vanillin-concentrated sulphuric acid colour developing.
Table 1
3, acetylcholine esterase inhibition activity screening technique and result
1) experiment condition
A, material: DMSO (dimethyl sulfoxide) (Ke Miou company); KH 2pO 4, K 2hPO 43H 2o (Xi Long chemical plant, Shantou, Guangdong city); AchE enzyme (Sigma Co., USA); PNPG (Sigma Co., USA)
B, experimental apparatus: multi-functional microplate reader Bio-Rad Model 680 type (Bio-Rad Laboratories Inc.)
2) experimental technique and process
Sample treatment: 1 mg testing sample is dissolved in 20 μl dimethyl sulfoxide (DMSO), as mother solution, gets 1 μl mother solution adds 249 μl distilled water is made into 200 μgmL -1solution.
Inhibiting activity of acetylcholinesterase, assay method:
The AchE inhibit activities of working sample in 96 hole ELISA Plate.Concrete operations are as follows: in 96 hole ELISA Plate, add 20 μ L PB (100mM, pH 8. 0) successively, 25 μ L AChE (0. 033 U/mL, pH 8. 0 PB dissolved dilution), 25 μ L sample solution (40 μ gmL -1).After ice bath 5min, add 15 μ L ATCI(0.6mM) and 15 μ L DTNB(1.5mM).37 DEG C hatch 60min after, under 412 nm, measure its absorbance by microplate reader.Suppression ratio is calculated according to following formula:
Inhibition of enzyme activity rate %=[A blank-(A sample-A background)]/A blank× 100
A in formula blank: do not add the reacted absorption value of sample;
A sample: add the absorption value after example reaction;
A background: the absorption value only adding sample.
3) experimental result
Table 2
Found that:
Optimal case of the present invention is: the diligent You Si of Uigurs medicine card fiber crops is through organic solvent supersound extraction, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use petroleum ether eluting, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, with the eluent of petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting through reclaiming organic solvent, drying, is this inhibiting activity of acetylcholinesterase, extract.This inhibiting activity of acetylcholinesterase, extract is from having no bibliographical information, and its TLC analysis and characterization is as Fig. 1.
4, the Study on Extraction Method of inhibiting activity of acetylcholinesterase, effective extract
1) Research on kinds of Extraction solvent
Use the organic solvent extraction such as methanol, acetone, petroleum ether, chloroform, ethyl acetate, methanol-water mixed solvent, ethanol water mixed solvent respectively, and the inhibiting activity of acetylcholinesterase, of Test extraction thing, experimental result is as follows:
Table 3
Result of study shows: extraction organic solvent can be methanol, petroleum ether, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, ethanol water mixed solvent.
2) Extraction solvent use quantity research
Use 1,2,5,10,20,30,40,50 times of (weight/volume) organic solvent extraction respectively, and the inhibiting activity of acetylcholinesterase, of Test extraction thing, result is as follows:
Table 4
The extraction consumption of organic solvent used of activity extract is 2-50 times (weight/volume) of medical material weight.
3) research of drying means
Respectively with boulton process, freeze-drying, forced air drying, centrifugal drying, revolve and steam the method such as seasoning, drying is carried out to the acetylcholine esterase inhibition activity extract obtained, with water content, TLC, active testing for index, find boulton process, freeze-drying, forced air drying, centrifugal drying, revolve steam seasoning be applicable to carry out drying to inhibiting activity of acetylcholinesterase, extract, wherein, optimum is boulton process, freeze-drying.
Table 5
Preferably, the preparation method of blocking numb diligent You Si inhibiting activity of acetylcholinesterase, extract is:
The diligent You Si of Uigurs medicine card fiber crops is through organic solvent supersound extraction, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use petroleum ether eluting, eluting 2-50 times column volume, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 2-50 times column volume, with the eluent of petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting through reclaiming organic solvent, drying, is this activity extract.Above condition is optimum for first to use petroleum ether eluting 10 times of column volumes, continues with petroleum ether: ethyl acetate mixed solvent (petroleum ether: ethyl acetate, 100:1, volume ratio) eluting 30 times of column volumes.Wherein,
1) extract extraction solvent can be methanol, petroleum ether, water, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, ethanol water mixed solvent, and optimal conditions is methanol and 95% ethanol.Activity extract extraction consumption of organic solvent is 2-50 times (weight/volume) of medical material weight.
2) extract drying means can be boulton process, freeze-drying, forced air drying, centrifugal drying, revolve and steam seasoning etc., and optimum is boulton process, freeze-drying.
5. block the medical usage research of numb diligent You Si acetylcholine esterase inhibition activity extract (when eluent is 100:1 the dry extract obtained)
By activity extract prepared by the diligent You Si inhibiting activity of acetylcholinesterase, method for preparing extractive of card fiber crops optimized, after tested, its inhibiting activity of acetylcholinesterase, is IC 50=15.9 μ g/mL.
There is due to acetylcholinesteraseinhibitors inhibitors the medical usage of the aspects such as treatment Alzheimer.Therefore, the diligent You Si inhibiting activity of acetylcholinesterase, extract of card fiber crops that we find has medical usage widely.
6, the composition and method of making the same research of numb diligent You Si acetylcholine esterase inhibition activity extract is blocked
1) solid dispersion
Prescription
Block numb diligent You Si extract 20 g
Vc 1 g
Polyvinylpyrrolidone 79 g
Solid dispersal 100g
Preparation method:
The mass ratio taking the numb diligent You Si extract of card and carrier polyvinylpyrrolidone (PVP) 1:2,1:4,1:6 in proportion puts into beaker respectively, add appropriate dehydrated alcohol and Vc, dissolve completely to the numb diligent You Si extract of card and carrier by magnetic stirrer, proceed to after abundant mix homogeneously to revolve to steam in instrument and remove organic solvent, dry, pulverized 80 mesh sieves, numb diligent You Si effective extract PVP clathrate must be blocked.
2) cyclodextrin clathrate
Prescription:
Block numb diligent You Si extract 20 g
Vc 1 g
Beta-schardinger dextrin-79 g
Clathrate 100g
Preparation method:
Beta-schardinger dextrin-and 1-5 times of water are ground well, add the numb diligent You Si effective extract of card (should being first dissolved in a small amount of organic solvent of slightly water-soluble) and continue fully to be ground to into pastel, namely cold drying obtains cyclodextrin clathrate.
3) dispersible tablet prescription:
Block numb diligent You Si extract 100
Sodium lauryl sulphate 1
Vc 1
Pregelatinized Starch 10
Soluble starch 100
Polyvinylpolypyrrolidone 10
Microcrystalline Cellulose 9
Differential silica gel 0.3
Pulvis Talci 1
100
Preparation method:
1. block the preparation of numb diligent You Si effective extract dispersion, precision takes the numb diligent You Si extract of card, Vc, add the sodium lauryl sulphate of recipe quantity, be 70% dissolve with ethanol by appropriate concentration and after adding the soluble starch mix homogeneously of equal proportion, evaporate to dryness at the temperature of 70 DEG C, pulverize, cross 100 mesh sieves;
2. by the card diligent You Si effective extract starch dispersions of fiber crops in the first step and the polyvinylpolypyrrolidone of recipe quantity, pregelatinized Starch, be that 70% ethanol makees wetting agent by appropriate concentration, stir while adding, make wet granular and cross 14 mesh sieves, after ambient temperatare puts 15min, 60 DEG C of oven for drying 45min, 16 mesh sieve granulate, add Pulvis Talci and the differential silica gel of recipe quantity, after mix homogeneously, tabletting and get final product.
7, the detection method research of numb diligent You Si acetylcholine esterase inhibition activity extract is blocked
We find, can use the method for thin layer chromatography, well the feature of detection and the diligent You Si inhibiting activity of acetylcholinesterase, extract of designation card fiber crops.See Fig. 1
Actual conditions is: GF 254silica gel plate, development system: petroleum ether: ethyl acetate: acetone (3:1:1) coloration method: vanillin-sulfuric acid develops the color.
Accompanying drawing illustrates:
The TLC chromatogram of the diligent You Si inhibiting activity of acetylcholinesterase, extract of Fig. 1 card fiber crops;
The TLC chromatogram of the diligent You Si solvent extractable matter of Fig. 2 card fiber crops.
Detailed description of the invention:
Following examples represent practicality of the present invention, and the present invention is not limited.
Embodiment 1:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2.0 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, vacuum drying, is this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=86.0 μ g/mL.
Embodiment 2:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL ethanol ultrasonic extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, is this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=89.0 μ g/mL.
Embodiment 3:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL petroleum ether supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, revolve steaming seasoning, be this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=77.0 μ g/mL.
Embodiment 4:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL acetone supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, forced air drying, is this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=80.0 μ g/mL.
Embodiment 5:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL chloroform supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, centrifugal drying, is this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=78.0 μ g/mL.
Embodiment 6:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL ethyl acetate supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=71.0 μ g/mL.
Embodiment 7:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL methanol-water mixed solvents (methanol: water=1:1) supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=88.0 μ g/mL.
Embodiment 8:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL ethanol water mixed solvents (ethanol: water=1:1) supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=62.0 μ g/mL.
Embodiment 9:
Get Uigurs medicine card fiber crops and diligent day especially take charge of 20 g, through 100 mL ethanol-water mixed solvents (ethanol: water=90:10) supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first first use petroleum ether eluting, eluting 10 times of column volumes, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, eluting 30 times of column volumes, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its inhibiting activity of acetylcholinesterase, is IC 50=74.0 μ g/mL.
Embodiment 10: solid dispersion
The mass ratio taking the numb diligent You Si extract of card and carrier polyvinylpyrrolidone (PVP) 1:2,1:4,1:6 in proportion puts into beaker respectively, add appropriate dehydrated alcohol and Vc, dissolve completely to the numb diligent You Si extract of card and carrier by magnetic stirrer, proceed to after abundant mix homogeneously to revolve to steam in instrument and remove organic solvent, dry, pulverized 80 mesh sieves, numb diligent You Si effective extract PVP clathrate must be blocked.
Embodiment 11: cyclodextrin clathrate
Beta-schardinger dextrin-and 1-5 times of water are ground well, add the numb diligent You Si effective extract of card (should being first dissolved in a small amount of organic solvent of slightly water-soluble) and continue fully to be ground to into pastel, namely cold drying obtains cyclodextrin clathrate.
Embodiment 12: dispersible tablet
1. block the preparation of numb diligent You Si effective extract dispersion, precision takes the numb diligent You Si extract of card, Vc, add the sodium lauryl sulphate of recipe quantity, be 70% dissolve with ethanol by appropriate concentration and after adding the soluble starch mix homogeneously of equal proportion, evaporate to dryness at the temperature of 70 DEG C, pulverize, cross 100 mesh sieves;
By the card diligent You Si effective extract starch dispersions of fiber crops in the first step and the polyvinylpolypyrrolidone of recipe quantity, pregelatinized Starch, be that 70% ethanol makees wetting agent by appropriate concentration, stir while adding, make wet granular and cross 14 mesh sieves, after ambient temperatare puts 15min, 60 DEG C of oven for drying 45min, 16 mesh sieve granulate, add Pulvis Talci and the differential silica gel of recipe quantity, after mix homogeneously, tabletting and get final product.

Claims (11)

1. the numb diligent You Si extract of card, it is characterized by the numb diligent You Si of card to extract through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, the silicagel column after loading, first uses petroleum ether-eluting, continue with the petroleum ether-ethyl acetate mixed solvent eluting of volume ratio 100:1, with the eluent of the petroleum ether-ethyl acetate mixed solvent eluting of volume ratio 100:1 through recycling design, dry, be this extract.
2. block numb diligent You Si extract as claimed in claim 1, it is characterized by, the Extraction solvent of this extract can be methanol, petroleum ether, water, acetone, chloroform, ethyl acetate, methanol-water mixed solvent or ethanol water mixed solvent, and optimal conditions is methanol and 95% ethanol; Extract extraction solvent load is 2-50 times (weight/volume) of medical material weight.
3. block numb diligent You Si extract as claimed in claim 1, it is characterized by the numb diligent You Si of card and extract through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, the silicagel column after loading, first uses petroleum ether eluting, continue with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting, with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluent of eluting is through reclaiming organic solvent, dry, is this extract.
4. block numb diligent You Si extract as claimed in claim 1, the consumption of eluent is 2-50 times of column volume.
5. block numb diligent You Si extract as claimed in claim 1, it is characterized by, above condition is optimum for first to use petroleum ether eluting 10 times of column volumes, continues with petroleum ether-ethyl acetate mixed solvent (petroleum ether-ethyl acetate, 100:1, volume ratio) eluting 30 times of column volumes.
6. a pharmaceutical composition, is characterized in that, comprises the Uygur card numb diligent You Si extract of claim 1-5 described in any one and pharmaceutically acceptable carrier.
7. a pharmaceutical preparation, is characterized in that, comprises the card fiber crops diligent You Si extract of claim 1-5 described in any one or pharmaceutical composition according to claim 6.
8. pharmaceutical preparation as claimed in claim 7, it is characterized in that, described preparation is solid dispersion, cyclodextrin clathrate, dispersible tablet.
9. the application in inhibiting activity of acetylcholinesterase, medicine is being prepared in claim 1-5 extract described in any one or compositions according to claim 6 or pharmaceutical preparation according to claim 7.
10. apply as claimed in claim 9, it is characterized in that, described inhibiting activity of acetylcholinesterase, can be used for the medical usage for the treatment of the aspects such as Alzheimer (AD).
11. as the Uigurs medicine card fiber crops diligent You Si extract of claim 1-5 as described in any one, and it is characterized in that, detect by TLC method, its chromatographic condition is: GF 254silica gel plate, development system: petroleum ether: ethyl acetate: acetone=3:1:1, coloration method: vanillin concentrated sulphuric acid develops the color.
CN201510058758.5A 2015-02-04 2015-02-04 Medicinal application and preparation method of Kamaziriyousi (dcroptiol repens) acetyl cholinesterase-inhibiting active extract and composition thereof Pending CN104825520A (en)

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Country Status (1)

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Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
《JOURNAL OF YOUNG PHARMACISTS》 *
《中国优秀硕士学位论文全文数据库 医药卫生科技辑》 *
李素君: "槲皮素对记忆障碍模型小鼠及血管性痴呆大鼠的影响及机制研究", 《延边大学硕士学位论文》 *
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Application publication date: 20150812