CN104644704A - Medical application and preparation method of fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract and composition of fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract - Google Patents
Medical application and preparation method of fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract and composition of fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract Download PDFInfo
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Abstract
The invention belongs to the technical field of medicines and in particular relates to a preparation method of fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract and a composition of the fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract as well as a medical application of the fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract in the aspects of alzheimer disease treatment and the like. The fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract is obtained by adopting a method comprising the following steps: firstly eluting with a chloroform-methanol mixed solvent (a volume ratio of chloroform to methanol is 100:1), further eluting with the chloroform-methanol mixed solvent (volume ratio of chloroform to methanol is 100:6), recycling the solvent from eluent obtained during eluting with the chloroform-methanol mixed solvent (the volume ratio of chloroform to methanol is 100:6), and drying, so that the fructus terminaliae billericae pulp butyrylcholinesterase inhibitory activity extract is obtained.
Description
Technical field
The invention belongs to medical art, be specifically related to the medical usage of a kind of Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities extract and compositions thereof and preparation method and it medical usage in treatment Alzheimer (AD) etc.
Background technology
Fructus Terminaliae Billericae be Combretum Racemosum vegetable hair Fructus Chebulae (
terminalia bellirica Roxb) dry fruit, Fructus Terminaliae Billericae is deciduous tree, high 12-15 m, and the diameter of a cross-section of a tree trunk 1.3 meters above the ground can reach 1 m, branch Lycoperdon polymorphum Vitt, tool longitudinal grin, sprig spire and petiole base normal tool rust fine hair.The raw branch top of leaf helical form collection, the long 3-9 cm of petiole, without hair, spike axil is raw.Pluck during fruit maturation autumn and winter, dry.China is produced in south of Yunnan, Xinjiang, is distributed in Vietnam, Laos, Thailand etc. abroad.
Fructus Terminaliae Billericae fruit is raw dry raw cold, body fluid is burnt in purification abnormal blood matter and removing, and antidiarrheal is astringent or styptic treatment for spontaneous sweating, supplementing the brain, improving eyesight, nourishing the intestines and stomach, and loose gas disappears nevus.Cure mainly humid or blood matter disease, as stomach enterogenous diarrhoea, enteral burns body fluid to be increased, and the empty poor or weak eyesight of brain, epiphora induced by wind, the intestines and stomach is weak, depressed hemorrhoid etc.Modern pharmacological research shows, Fructus Terminaliae Billericae fruit can promote bile secretion, makes total solids content in bile have obvious increase, and the LD that Mouse oral alcohol extraction is right
50be 4.25 mg/kg.
In the process of high flux screening, the present invention is surprised to find that great Ye Fructus Terminaliae Billericae has the activity well suppressing butyrylcholine esterase, and 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 a kind of Fructus Terminaliae Billericae extract.
Present invention also offers with Fructus Terminaliae Billericae extract is the compositions of main active.
Invention also provides the Synthesis and applications of Fructus Terminaliae Billericae extract and compositions thereof.
The present invention is achieved through the following technical solutions:
Uigurs medicine Fructus Terminaliae Billericae is through methanol supersound extraction, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, with stone chloroform-methanol mixed solvent gradient elution (chloroform-methanol, ratio is in table 1), each chloroform-methanol ratio mixed solvent eluent, concentrated, after drying, in-vitro screening system is utilized to test its butyrylcholine esterase inhibit activities, be surprised to find that and first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) the chloroform-methanol mixed solvent (chloroform: methanol that obtains of eluting, 100:6, volume ratio) eluent through reclaim organic solvent, dry, be butyrylcholine esterase inhibit activities extract.And the eluting position of other ratios, there is no the effect of butyrylcholine esterase inhibit activities.Especially, preferably first use chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting 25 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:6, volume ratio) eluting 20 times of column volumes, be the extract of butyrylcholine esterase inhibit activities of the present invention after eluent drying.The extract of butyrylcholine esterase inhibit activities can obtain enrichment by above method, thus separates with other impurity constituents.This Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities extract is from having no bibliographical information, and its thin layer chromatography (TLC) analysis result is shown in Fig. 1, TLC analysis condition: GF
254silica gel plate, development system: chloroform: ethyl acetate: methanol (3:1:1) coloration method: vanillin-sulfuric acid develops the color.
Specifically, discovery procedure is as follows:
1, Fructus Terminaliae Billericae is through the preparation of methanol sonicated extract
Get Uigurs medicine Fructus Terminaliae Billericae 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, obtain extract SN0047 sample 7.0540 g, keep sample 4.2032 g, and upper prop 2.8508 g mixes sample silica gel 3 g, blank silica gel 10g, chloroform-methanol system.
2, chloroform-methanol mixed solvent gradient elution method and result
Get Uigurs medicine Fructus Terminaliae Billericae 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, obtain extract SN0047 sample 7.0540 g, keep sample 4.2032 g, upper prop 2.8508 g, dissolve with methanol, shares methanol 15 mL.Upper silica gel column chromatography, mixes sample silica gel 3 g, blank silica gel 10 g, glass column internal diameter 1.6cm, chloroform-methanol system gradient elution (condition is in table 1), column volume 22 mL, each gradient elution 200mL, obtains, and each concentration extracts the eluate of eluent, recycling design, obtain, petroleum ether: acetone gradient elution extract, TLC analysis result is shown in Fig. 2, Fig. 3, TLC analysis condition: GF
254silica gel plate, development system: chloroform: ethyl acetate: methanol (3:1:1), chloroform: ethyl acetate: methanol (1:1:1), coloration method: vanillin-sulfuric acid develops the color.
Table 1
3, the activity of BuChE screening technique and result is suppressed
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); BuChE 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.
Butyrylcholine esterase inhibit activities assay method:
The BuchE inhibit activities of working sample on 96 orifice plates.Concrete operations are as follows: in 96 orifice plates, add 25 successively
μl PBS (100 mM, pH 8.0), 25
μl BuChE (>=0.04 U/mL, pH 8.0 PBS dissolved dilution), 25
μl sample solution (200
μgmL
-1).Add 25
μl BuSCH (1.6 mM, pH 8.0 PBS dissolved dilution) and 25
μl DTNB (4.0 mM, pH 8.0 PBS dissolved dilution), 37 DEG C hatch 60 min after, under 412 nm, measure its absorbance by microplate reader.Sample inhibition percentage calculates as follows:
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:
Preferred version of the present invention is: Uigurs medicine Fructus Terminaliae Billericae extracts through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, continues with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, with the eluent of chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting through reclaiming organic solvent, drying, is this butyrylcholine esterase inhibit activities extract.This butyrylcholine esterase inhibit activities extract is from having no bibliographical information, and its TLC analysis and characterization is as Fig. 1.
4, the Study on Extraction Method of butyrylcholine esterase inhibit activities 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 butyrylcholine esterase inhibit activities 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 butyrylcholine esterase inhibit activities 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 suppression the activity of BuChE 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 butyrylcholine esterase inhibit activities extract, wherein, optimum is boulton process, freeze-drying.
Table 5
Preferably, the preparation method of Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities extract is:
Uigurs medicine Fructus Terminaliae Billericae extracts through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 2-50 times column volume, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 2-50 times column volume, with the eluent of chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting through reclaiming organic solvent, drying, is this activity extract.Above condition is optimum for first to use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting 20 times of column volumes, continues with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting 15 times of column volumes.
Wherein,
1) extract extraction organic 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. Fructus Terminaliae Billericae suppresses the medical usage research of the activity of BuChE extract (when eluent is 100:6, drying is extract obtained)
By activity extract prepared by the Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities method for preparing extractive optimized, after tested, its butyrylcholine esterase inhibit activities is IC
50=16.7 μ g/mL.
There is due to butyrylcholinesterase inhibitor the medical usage of the aspects such as treatment Alzheimer.Therefore, the Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities extract that we find has medical usage widely.
6, Fructus Terminaliae Billericae suppresses the composition and method of making the same research of the activity of BuChE extract
1) solid dispersion
Prescription
Fructus Terminaliae Billericae extract 20 g
Vc 1 g
Polyvinylpyrrolidone 79 g
Solid dispersal 100g
Preparation method:
The mass ratio taking Fructus Terminaliae Billericae extract 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 Fructus Terminaliae Billericae extract and carrier by magnetic stirrer, proceed to after abundant mix homogeneously to revolve to steam in instrument and remove organic solvent, dry, pulverize 80 mesh sieves, obtain Fructus Terminaliae Billericae effective extract PVP clathrate.
2) cyclodextrin clathrate
Prescription:
Fructus Terminaliae Billericae 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 Fructus Terminaliae Billericae effective extract (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:
Fructus Terminaliae Billericae 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. the preparation of Fructus Terminaliae Billericae effective extract dispersion, precision takes Fructus Terminaliae Billericae extract, 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 polyvinylpolypyrrolidone of the Fructus Terminaliae Billericae effective extract starch dispersions in the first step and 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, Fructus Terminaliae Billericae suppresses the detection method research of the activity of BuChE extract
We find, by the method for thin layer chromatography, can detect and indicate the feature of Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities extract well, see Fig. 1.
Actual conditions is: GF
254silica gel plate, development system: chloroform: ethyl acetate: methanol (3:1:1) coloration method: vanillin-sulfuric acid develops the color.
Accompanying drawing illustrates:
The TLC chromatogram of Fig. 1 Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities extract;
The TLC chromatogram of Fig. 2 Fructus Terminaliae Billericae butyrylcholine esterase inhibit activities extract;
The TLC chromatogram of Fig. 3 Fructus Terminaliae Billericae solvent extractable matter.
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 Fructus Terminaliae Billericae 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, vacuum drying, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=83.0 μ g/mL.
Embodiment 2:
Get Uigurs medicine Fructus Terminaliae Billericae 20 g, through 100 mL ethanol ultrasonic extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=86.0 μ g/mL.
Embodiment 3:
Get Uigurs medicine Fructus Terminaliae Billericae 20 g, through 100 mL petroleum ether supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, revolve steaming seasoning, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=78.0 μ g/mL.
Embodiment 4:
Get Uigurs medicine Fructus Terminaliae Billericae 20 g, through 100 mL acetone supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, forced air drying, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=81.0 μ g/mL.
Embodiment 5:
Get Uigurs medicine Fructus Terminaliae Billericae 20 g, through 100 mL chloroform supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, centrifugal drying, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=75.0 μ g/mL.
Embodiment 6:
Get Uigurs medicine Fructus Terminaliae Billericae 20 g, through 100 mL ethyl acetate supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=67.0 μ g/mL.
Embodiment 7:
Get Uigurs medicine Fructus Terminaliae Billericae 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 (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=85.0 μ g/mL.
Embodiment 8:
Get Uigurs medicine Fructus Terminaliae Billericae 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 (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=62.0 μ g/mL.
Embodiment 9:
Get Uigurs medicine Fructus Terminaliae Billericae 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 (1.6cm internal diameter pillar) after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, eluting 15 times of column volumes, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, eluting 25 times of column volumes, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its butyrylcholine esterase inhibit activities is IC
50=73.0 μ g/mL.
Embodiment 10: solid dispersion
The mass ratio taking Fructus Terminaliae Billericae extract 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 Fructus Terminaliae Billericae activity extract and carrier by magnetic stirrer, proceed to after abundant mix homogeneously to revolve to steam in instrument and remove organic solvent, dry, pulverize 80 mesh sieves, obtain Fructus Terminaliae Billericae effective extract PVP clathrate.
Embodiment 11: cyclodextrin clathrate
Beta-schardinger dextrin-and 1-5 times of water are ground well, add Fructus Terminaliae Billericae activity extract (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. the preparation of Fructus Terminaliae Billericae activity extract dispersion, precision takes Fructus Terminaliae Billericae extract, 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 polyvinylpolypyrrolidone of the Fructus Terminaliae Billericae effective extract starch dispersions in the first step and 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 (10)
1. a Fructus Terminaliae Billericae extract, it is characterized by Fructus Terminaliae Billericae to extract through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, the silicagel column after loading is first the chloroform-methanol mixed solvent eluting of 100:1 by volume ratio, continuing by volume ratio is the chloroform-methanol mixed solvent eluting of 100:6, with the eluent of the chloroform-methanol mixed solvent eluting of 100:6 through reclaiming organic solvent, dry, be this extract.
2. Fructus Terminaliae Billericae extract as claimed in claim 1, wherein, Extraction solvent can be methanol, petroleum ether, water, acetone, chloroform, ethyl acetate, methanol-water mixed solvent or ethanol water mixed solvent to its feature, and optimal conditions is methanol and 95% ethanol.
3. Fructus Terminaliae Billericae extract as claimed in claim 1, it is characterized by Fructus Terminaliae Billericae to extract through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use chloroform-methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, continue with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluting, with chloroform-methanol mixed solvent (chloroform: methanol, 100:6, volume ratio) eluent of eluting is through reclaiming organic solvent, dry, is this extract.
4. the preparation method of extract as claimed in claim 1, as a kind of Uigurs medicine Fructus Terminaliae Billericae extract of claim 1-3 as described in any one, it is characterized by, the elution volume for the chloroform-methanol of eluting is 2-50 times of column volume.
5. the preparation method of extract described in claim 1, it is characterized by: Fructus Terminaliae Billericae extracts through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting 2-50 times column volume, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:6, volume ratio) eluting 2-50 times column volume, with chloroform-methanol mixed solvent (chloroform-methanol, 100:6, volume ratio) eluent of eluting is through reclaiming organic solvent, dry, is this extract; Above condition is optimum for first to use chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting 25 times of column volumes, continues with chloroform-methanol mixed solvent (chloroform-methanol, 100:6, volume ratio) eluting 20 times of column volumes.
6. a pharmaceutical composition, is characterized in that, comprises the extract of claim 1-5 described in any one and pharmaceutically acceptable carrier.
7. a pharmaceutical preparation, is characterized in that, comprises the extract of claim 1-5 described in any one or pharmaceutical composition according to claim 6.
8. the application in the activity of BuChE medicine is being prepared in the Fructus Terminaliae Billericae extract of claim 1-5 described in any one or compositions according to claim 6 or pharmaceutical preparation according to claim 7.
9. Uigurs medicine Fructus Terminaliae Billericae extract as claimed in claim 8, is characterized by, described the activity of BuChE, can be used for the medical usage for the treatment of the aspects such as Alzheimer (AD).
10. a kind of Uigurs medicine Fructus Terminaliae Billericae extract of claim 1-5 described in any one, is characterized in that, detect by TLC method; Chromatographic condition: GF
254silica gel plate, development system: chloroform: ethyl acetate: methanol (3:1:1) coloration method: vanillin-sulfuric acid develops the color.
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Non-Patent Citations (3)
| Title |
|---|
| GARGI NAG AND BRATATI DE*: "ACETYLCHOLINESTERASE INHIBITORY ACTIVITY OF TERMINALIA CHEBULA, TERMINALIABELLERICA AND EMBLICA OFFICINALIS AND SOME PHENOLIC COMPOUNDS", 《INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES》 * |
| 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》 * |
| 阳小勇: "诃子化学成分的研究", 《西昌学院学报》 * |
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