CN104644721A - Alpha-glycosidase inhibitory activity extract of semen cuscutae as well as medical application and preparation methods of compositions thereof - Google Patents
Alpha-glycosidase inhibitory activity extract of semen cuscutae as well as medical application and preparation methods of compositions thereof Download PDFInfo
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Abstract
The invention belongs to the field of medical technologies, and particularly relates to an alpha-glycosidase inhibitory activity extract of semen cuscutae and preparation methods of compositions thereof and medical application of the compositions in the aspects of decreasing blood sugar, losing weight, reducing blood fat, treating diabetes, and the like. The extract is prepared by using the following method: eluting by using a petroleum ether-acetone mixed solvent (the volume ratio of petroleum ether to acetone is 100:17) firstly, then eluting by using a petroleum ether-acetone mixed solvent (the volume ratio of petroleum ether to acetone is 100:50), recovering a solvent from eluent obtained by eluting by using the petroleum ether-acetone mixed solvent (the volume ratio of petroleum ether to acetone is 100:50), and drying the solvent, so that the alpha-glycosidase inhibitory activity extract is obtained.
Description
Technical field
The invention belongs to medical art, be specifically related to the preparation method of a kind of Semen Cuscutae alpha-glucoside inhibiting activity extract and compositions thereof and its medical usage in blood sugar lowering, fat-reducing, blood fat reducing, treatment diabetes etc.
Background technology
Semen Cuscutae name Semen Cuscutae has another name called Herba Melicae Scabrosae, and the herb of Convolvulaceae Herba Melicae Scabrosae platymiscium Herba Melicae Scabrosae Pogonatherum crinitum (Thunb.) Kunth, with all herbal medicine with flowers and fruits.The whole year can adopt.Function cures mainly: heat clearing away, expelling summer-heat, diuresis.Removing heat from blood heat radiation poison, cures mainly haematemesis, epistaxis, metrostaxis, carbuncle poison malignant boil.For high heat of catching a cold, heatstroke, urinary tract infection, oedema due to nephritis, icterohepatitis, diabetes, children's's heat of a specified duration is not moved back.Heat-clearing and toxic substances removing; Cooling blood for hemostasis; Dampness removing.Main calentura excessive thirst; Spit blood; Epistaxis; Hemoptysis; Hematuria; Metrorrhagia; Jaundice; Edema; Stranguria with turbid discharge leukorrhagia, dysentery; Children's's infantile malnutrition with fever; Furuncle carbuncle.
The present invention by a large scale, systematically screening active ingredients, be surprised to find that Uigurs medicine Semen Cuscutae extract and partial chemical component thereof, have alpha-glucoside inhibiting activity significantly, this activity extract and compositions thereof are expected to be applied to the aspects such as blood sugar lowering, fat-reducing, blood fat reducing, diabetes.
Summary of the invention
Technical problem solved by the invention is to provide a kind of Semen Cuscutae extract.
Present invention also offers with Semen Cuscutae extract is the compositions of main active.
Invention also provides the Synthesis and applications of Semen Cuscutae extract and compositions thereof.
The present invention is achieved through the following technical solutions:
Uigurs medicine Semen Cuscutae through methanol supersound extraction, after extracting solution is concentrated, with silica gel (SiO
2) post separation, silicagel column after loading, with petroleum ether-acetone mixed solvent gradient elution (petroleum ether-acetone, ratio is in table 1), each petroleum ether-acetone ratio mixed solvent eluent, concentrated, after drying, in-vitro screening system is utilized to test its alpha-glucoside inhibiting activity, be surprised to find that and first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) petroleum ether-acetone mixed solvent (petroleum ether-acetone of obtaining of eluting, 100:50, volume ratio) eluent through reclaim organic solvent, dry, be alpha-glucoside inhibiting activity extract.And the eluting position of other ratios, there is no the effect of alpha-glucoside inhibiting activity.Optimum for first to use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting 20 times of column volumes, the extract obtained extract being alpha-glucoside inhibiting activity of the present invention after eluent drying.The extract of alpha-glucoside inhibiting activity can obtain enrichment by above method, thus separates with other impurity constituents.This Semen Cuscutae alpha-glucoside inhibiting activity extract 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 (6:1:1) coloration method: vanillin-sulfuric acid develops the color.
Specifically, discovery procedure is as follows:
1, Semen Cuscutae is through the preparation of methanol sonicated extract
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, obtains extract SN0040A, sample 1.9134g, mix sample silica gel 2g, blank silica gel 10g, petroleum ether-acetone system
2, petroleum ether-acetone mixed solvent gradient elution method and result
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, obtain extract SN0040A, sample 1.9134g, upper prop, dissolve with methanol, share methanol 15 mL.Upper silica gel column chromatography, mix sample silica gel 2g, blank silica gel 10g, glass column internal diameter 2 cm, petroleum ether-acetone system gradient elution (condition is in table 1), column volume 25 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, TLC analysis condition: GF254 silica gel plate, development system: petroleum ether: ethyl acetate: acetone (6:1:1) coloration method: vanillin-sulfuric acid develops the color.
Table 1:
3, alpha-glucosidase method for screening active ingredients 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);
α-glucosidase 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 99
μl buffer salt is made into 500
μgmL
-1sample solution.
Add successively in 96 orifice plates
α-glucosidase enzyme PBS solution 20
μl makes its final concentration be 0.07 u/mL, and sample concentration is 500
μgmL
-1pBS solution 10
μl.Ice bath 5 minutes, adds substrate PBS solution 20
μl makes its final concentration be 2.5 mmol/l, and supplying volume by the PBS solution that concentration is 0.1 M, pH 6.84 is 100
μl.Added 96 orifice plates of sample 37 DEG C of water-baths 30 minutes.In the absorbance of 405 nm place assaying reaction things, and using acarbose as positive control.Sample suppresses
α-glucosidase enzymatic activity ratio is with adding sample compared with blank
oDthe ratio of value represents.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:
Optimal case of the present invention is: Uigurs medicine Semen Cuscutae is through organic solvent supersound extraction, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, continues with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, drying, is this extract, is this alpha-glucoside inhibiting activity extract.This alpha-glucoside inhibiting activity extract is from having no bibliographical information, and its TLC analysis and characterization is as Fig. 1.
4, the Study on Extraction Method of alpha-glucoside inhibiting activity 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 alpha-glucoside inhibiting activity 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 alpha-glucoside inhibiting activity 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 alpha-glucosidase 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 alpha-glucoside inhibiting activity extract, wherein, optimum is boulton process, freeze-drying.
Table 5:
Preferably, the preparation method of Semen Cuscutae alpha-glucoside inhibiting activity extract is:
Uigurs medicine Semen Cuscutae is through organic solvent supersound extraction, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 2-50 times column volume, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 2-50 times column volume, with the eluent of petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting through reclaiming organic solvent, drying, is this activity extract.Above condition is optimum for first to use petroleum ether: acetone mixed solvent (petroleum ether: acetone, 100:17, volume ratio) eluting 10 times of column volumes, continues with petroleum ether: acetone mixed solvent (petroleum ether: acetone, 100:50, volume ratio) eluting 20 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. Semen Cuscutae suppresses the medical usage research of alpha-glucosidase activity extract (extract obtained after drying when eluent is 100:50)
By activity extract prepared by the Semen Cuscutae alpha-glucoside inhibiting activity method for preparing extractive optimized, after tested, its alpha-glucoside inhibiting activity is IC
50=22.9 μ g/mL.
There is due to alpha-glucosidase inhibitor the medical usage of the aspects such as blood sugar lowering, fat-reducing, blood fat reducing, diabetes.Therefore, the Semen Cuscutae alpha-glucoside inhibiting activity extract that we find has medical usage widely.
6, Semen Cuscutae suppresses the composition and method of making the same research of alpha-glucosidase activity extract
1) solid dispersion
Prescription
Semen Cuscutae extract 20 g
Vc 1 g
Polyvinylpyrrolidone 79 g
Solid dispersal 100g
Preparation method:
The mass ratio taking Semen Cuscutae 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 Semen Cuscutae 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 Semen Cuscutae effective extract PVP clathrate.
2) cyclodextrin clathrate
Prescription:
Semen Cuscutae 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 Semen Cuscutae 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:
Semen Cuscutae 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 Semen Cuscutae effective extract dispersion, precision takes Semen Cuscutae 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 Semen Cuscutae 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, Semen Cuscutae suppresses the detection method research of alpha-glucosidase activity extract
We find, by the method for thin layer chromatography, can detect and indicate the feature of Semen Cuscutae alpha-glucoside inhibiting activity extract well.See Fig. 1
Actual conditions is: GF
254silica gel plate, development system: petroleum ether: ethyl acetate: acetone (6:1:1) coloration method: vanillin-concentrated sulphuric acid colour developing.
Accompanying drawing illustrates:
The TLC chromatogram of Fig. 1 Semen Cuscutae alpha-glucoside inhibiting activity extract;
The TLC chromatogram of Fig. 2 Semen Cuscutae solvent extractable matter.
Concrete real embodiment
Following examples represent practicality of the present invention, and the present invention is not limited.
Embodiment 1:
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL methanol supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, vacuum drying, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=83.0 μ g/mL.
Embodiment 2:
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL ethanol ultrasonic extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=88.0 μ g/mL.
Embodiment 3:
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL petroleum ether supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, revolve steaming seasoning, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=81.0 μ g/mL.
Embodiment 4:
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL acetone supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, forced air drying, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=80.0 μ g/mL.
Embodiment 5:
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL chloroform supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, centrifugal drying, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=78.0 μ g/mL.
Embodiment 6:
Get Uigurs medicine Semen Cuscutae 20 g, through 100 mL ethyl acetate supersound extraction 15 min, after extracting solution is concentrated, be separated with silicagel column, silicagel column (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=71.0 μ g/mL.
Embodiment 7:
Get Uigurs medicine Semen Cuscutae 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 (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=86.0 μ g/mL.
Embodiment 8:
Get Uigurs medicine Semen Cuscutae 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 (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=57.0 μ g/mL.
Embodiment 9:
Get Uigurs medicine Semen Cuscutae 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 (1.5 cm internal diameter pillar) after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, eluting 10 times of column volumes, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, eluting 20 times of column volumes, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, lyophilization, be this activity extract.After tested, its alpha-glucoside inhibiting activity is IC
50=76.0 μ g/mL.
Embodiment 10: solid dispersion
The mass ratio taking Semen Cuscutae 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 Semen Cuscutae 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 Semen Cuscutae effective extract PVP clathrate.
Embodiment 11: cyclodextrin clathrate
Beta-schardinger dextrin-and 1-5 times of water are ground well, add Semen Cuscutae 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.
Embodiment 12: dispersible tablet
1. the preparation of Semen Cuscutae effective extract dispersion, precision takes Semen Cuscutae 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 Semen Cuscutae 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 (11)
1. a Semen Cuscutae extract, it is characterized by Semen Cuscutae to extract through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, the silicagel column after loading is first the petroleum ether-acetone mixed solvent eluting of 100:17 by volume ratio, continue and feed the petroleum ether-acetone mixed solvent eluting of 100:50 by volume ratio, with the eluent of the petroleum ether-acetone mixed solvent eluting of 100:50 through recycling design, dry, be this extract.
2. Semen Cuscutae 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.
3. Semen Cuscutae extract as claimed in claim 1, it is characterized by Semen Cuscutae to extract through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluent of eluting is through reclaiming organic solvent, dry, is this extract.
4., as a kind of Uigurs medicine Semen Cuscutae extract of claim 1-3 as described in any one, it is characterized by, the elution volume for the petroleum ether-acetone mixed solvent of eluting is 2-50 times of column volume.
5. the preparation method of extract as claimed in claim 1, it is characterized by: Semen Cuscutae extracts through solvent supersonic, after extracting solution is concentrated, be separated with silicagel column, silicagel column after loading, first use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting 2-50 times column volume, continue with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting 2-50 times column volume, with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting eluent through reclaim organic solvent, dry, be this extract, above condition is optimum for first to use petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:17, volume ratio) eluting 10 times of column volumes, continues with petroleum ether-acetone mixed solvent (petroleum ether-acetone, 100:50, volume ratio) eluting 20 times of column volumes.
6. a pharmaceutical composition, is characterized in that, comprises the Uigurs medicine Semen Cuscutae extract of claim 1-5 described in any one and pharmaceutically acceptable carrier.
7. a pharmaceutical preparation, is characterized in that, comprises the Semen Cuscutae 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. claim 1-5 extract described in any one or compositions according to claim 6 or pharmaceutical preparation according to claim 7 are in preparation
αapplication in-glucosidase inhibitory active medicine.
10. apply as claimed in claim 9, it is characterized in that, described
α-glucosidase inhibitory active, can be used for the medical usage of the aspects such as blood sugar lowering, fat-reducing, blood fat reducing, treatment diabetes.
11. as the Uigurs medicine Semen Cuscutae extract of claim 1-5 as described in any one, and it is characterized in that, use TLC detection method, its chromatographic condition is: GF
254silica gel plate, development system: petroleum ether: ethyl acetate: acetone=6:1:1, coloration method: vanillin concentrated sulphuric acid develops the color.
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| CN107412311A (en) * | 2017-07-19 | 2017-12-01 | 深圳弘汇生物医药有限公司 | The medical usage and preparation method of Asian puccoon α glucoside inhibiting activity extracts and combinations thereof |
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2015
- 2015-02-04 CN CN201510058776.3A patent/CN104644721A/en active Pending
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Application publication date: 20150527 |