CN103083376A - Ligusticum extractive capable of treating rhinitis - Google Patents

Ligusticum extractive capable of treating rhinitis Download PDF

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CN103083376A
CN103083376A CN201210177843XA CN201210177843A CN103083376A CN 103083376 A CN103083376 A CN 103083376A CN 201210177843X A CN201210177843X A CN 201210177843XA CN 201210177843 A CN201210177843 A CN 201210177843A CN 103083376 A CN103083376 A CN 103083376A
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rhizoma ligustici
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洪铁
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Jilin University
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Abstract

The invention provides a Ligusticum extractive capable of treating rhinitis, relating to water extractives obtained from three aqueous solvent containing Ligusticum plants (comprising Ligusticum sinense Oliv, Ligusticum jeholense Nakai et Kitag and Conioselinum uaginatum (Spreng.)Thell), preparation methods thereof, compositions containing the water extractives, and purposes of the water extractives and the compositions for preventing and treating rhinitis. The water extractives contain coumarins, lactones, alkaloid, polyphenols, flavonoid, organic acids, peptides and saccharides. Experiments show that the extractives are nontoxic and have the effect of preventing or treating rhinitis.

Description

Can be used for treating the Rhizoma Ligustici extract of rhinitis
Technical field
The present invention relates to Rhizoma Ligustici extract.Especially, the present invention relates to extract with aqueous solvent the purposes that Rhizoma Ligustici (comprising Rhizoma Ligustici Ligusticum sinense Oliv and Rhizoma Ligustici Ligusticum jeholense Nakai et Kitag and Xinjiang Rhizoma Ligustici Conioselinum uaginatum (Spreng.) Thell) water extract, its preparation method, the compositions that contains this water extract and water extract that vegetable material obtains and compositions are used for the treatment of rhinitis.
Summary of the invention
The present invention adopts water and contains three kinds of Rhizoma Ligustici plants of aqueous solution extract of organic solvent (comprising Ligusticum sinense Oliv and Ligusticum jeholense Nakai et Kitag and Conioselinum uaginatum (Spreng.) Thell) herb and obtains extract.These three kinds of extracts have stronger improve mice that egg protein (ova) induces and the effect of Cavia porcellus rhinitis, by literature search, have no Rhizoma Ligustici plant (comprising Ligusticum sinense Oliv and Ligusticum jeholense Nakai et Kitag and Conioselinum uaginatum (Spreng.) Thell) report identical with this research, this research belongs to finds that first this plant has the activity of prevention or treatment rhinitis.
The present invention is embodied in the paragraph of following numbering:
1. a method for preparing the water extract of Rhizoma Ligustici, comprising: obtain the Rhizoma Ligustici vegetable material; Extract the Rhizoma Ligustici vegetable material with aqueous solvent, obtain the water extract of Rhizoma Ligustici.
2. the method for paragraph 1, wherein extract the Rhizoma Ligustici vegetable material with aqueous solvent and comprise: (1) extracts the Rhizoma Ligustici vegetable material with aqueous solvent under proper condition; (2) separate liquid phase and solid phase; (3) randomly, repeating step (1) and (2) one or many (for example repeat 1-for several times, 1-5 time, 1-2 time, 2-5 time, 3 times, 4 times); (4) randomly, merge liquid phase; (5) randomly, will be concentrated by the liquid phase that step (2) or step (4) obtain.
3. the method for paragraph 2, wherein described in step (1), felicity condition comprises: temperature is about 0-100 ℃, for example approximately 60-100 ℃, preferred 90-100 ℃ can be also about 0-60 ℃; Pressure is about 0.1 atmospheric pressure-5 atmospheric pressure, for example about 0.5 atmospheric pressure-3 atmospheric pressure, for example about 1 atmospheric pressure, about normal pressure easily; Decocting time is about at least 0.15 hour, grows to for example 10 hours, for example about 0.15 hour-1 hour, about 0.5 hour-3 hours, for example about 0.5,1,2,3 hour, perhaps wherein any time, preferably is not shorter than 1 hour; The w/v of Rhizoma Ligustici vegetable material and aqueous solvent is about 1: 1 to about 1: 100 (kg/liter), for example about 1: 1 to about 1: 50, about 1: 2 to about 1: 40, preferably approximately 1: 5 to about 1: 20, more preferably about 1: 5 to about 1: 15 (kg/liter); Preferably stir when soaking.
4. the method for paragraph 2-3 any one, wherein separate in step (2) by filtering, and centrifugal, natural subsidence etc. realized.
5. the method for paragraph 2-4 any one, wherein the concentrated of step (5) is concentrating under reduced pressure, temperature can be at about 0 ℃ to about 80 ℃, preferably be no more than about 60 ℃, for example room temperature arrives about 60 ℃, for example about 30-60 ℃, as about 55 ℃, step (5) can be lyophilization.
6. paragraph 1-5 any one method, wherein said Rhizoma Ligustici is Ligusticum sinense Oliv and Ligusticum jeholense Nakai et Kitag and Conioselinum uaginatum (Spreng.) Thell.
7. paragraph 1-6 any one method, wherein said Rhizoma Ligustici vegetable material is the herb of Rhizoma Ligustici, for example root and rhizome.
8. the method for paragraph 1-7 any one, wherein said aqueous solvent are the water of the water of water or acidify or alkalization or aqueous solution or the aqueous solution that contains organic solvent acidify or alkalization that contains organic solvent; Wherein organic solvent can be methanol, ethanol, propanol, isopropyl alcohol, acetone or n-butyl alcohol or their any combination.
9. any one method of paragraph 1-7 wherein can be used organic solvent extraction before extracting the Rhizoma Ligustici vegetable material in advance containing aqueous solvent.Organic solvent includes but not limited to: petroleum ether, chloroform, ethyl acetate, ether, methanol, ethanol, propanol, isopropyl alcohol, acetone or n-butyl alcohol or their any combination etc.
10. the water extract of Rhizoma Ligustici.
11. the water extract of paragraph 10, it is to obtain by any one method of paragraph 1-9.
12. the water extract of the Rhizoma Ligustici that can obtain by any one method of paragraph 1-9.
13. a compositions, it contains any one Rhizoma Ligustici water extract of paragraph 10-12.
14. the compositions of paragraph 13, it also contains excipient or carrier.
15. the compositions of paragraph 13 or 14, it is pharmaceutical composition, health composition or beverage composition for treating dental erosion.
16. paragraph 10-12 any one the Rhizoma Ligustici water extract or the compositions of paragraph 13 or 14 for the preparation of the purposes in the treatment rhinitis.
17. Rhizoma Ligustici vegetable material or its extract (preferential water extract) are for the production of the purposes in the compositions that can be used for treating rhinitis.
18. the purposes of paragraph 16, wherein said compositions are pharmaceutical composition, health composition, food compositions or beverage composition for treating dental erosion.
19. the method for the treatment of rhinitis comprises to the patient giving Rhizoma Ligustici vegetable material or its extract (preferred water extract) or containing this extract or other has product after Rhizoma Ligustici vegetable material processing.
Compositions or the other side of this extract thing of the present invention will be described hereinafter, but they not should be understood to limit the scope of the present invention.
The specific embodiment
Purpose of the present invention is obtain Rhizoma Ligustici plant (comprising Ligusticum sinense Oliv and Ligusticum jeholense Nakai et Kitag and Conioselinum uaginatum (Spreng.) Thell) water extract and contain the water extract of organic solvent and contain the water extract of organic solvent, and these extracts are due to treatment of rhinitis.
Therefore, first aspect the present invention relates to a kind of method for preparing the water extract (perhaps extractum) of Rhizoma Ligustici, comprising: obtain the Rhizoma Ligustici vegetable material.The aqueous solvent of containing extract (perhaps leaching) Rhizoma Ligustici vegetable material is arranged.Obtain the water extract of Rhizoma Ligustici.Method of the present invention is used for extracting from the Rhizoma Ligustici vegetable material active component that can be used for treating rhinitis.
Can be by decocting method, soak method, percolation or steam distillation etc. and extract (perhaps leaching) Rhizoma Ligustici vegetable material.
In a specific embodiments, comprise with aqueous solvent extract Rhizoma Ligustici vegetable material: (1) decocts the Rhizoma Ligustici vegetable material with aqueous solvent under suitable condition; (2) separate liquid phase and solid phase; (randomly, repeating step (1) and (2) one or many (for example repeat 1-for several times, 1-5 time, 1-2 time, 2-5 time, 3 times, 4 times); (4) randomly, merge liquid phase; (5) randomly, will be concentrated by the liquid phase that step (2) or step (4) obtain.
In step (1), described felicity condition can be determined by test.Temperature is about 0-100 ℃, and for example about 60-100 ℃, preferred 90-100 ℃ can be also about 0-60 ℃;About 0.1 atmospheric pressure-5 atmospheric pressure of pressure, about 0.5 atmospheric pressure-3 atmospheric pressure for example, for example an about atmospheric pressure, be about normal pressure easily.Decocting time is about at least 0.15 hour, grows to for example 10 hours, for example about 0.15 hour-1 hour, about 0.5 hour-3 hours, for example about 0.5,1,2,3 hour, perhaps wherein any time, preferably is not shorter than 1 hour; The w/v of Rhizoma Ligustici vegetable material and aqueous solvent is about 1: 1 to about 1: 100 (kg/liter), for example about 1: 1 to about 1: 50, about 1: 2 to about 1: 40, preferably approximately 1: 5 to about 1: 20, more preferably about 1: 5 to about 1: 15 (kg/liter); Preferably stir when soaking.
Separation in step (2) can realize by any method known in the art, includes but not limited to, filters, centrifugal, natural subsidence etc.The concentrated of step (5) can be realized by any method known in the art.This concentrated having no particular limits, prerequisite is not destroy active component.For example, this concentrated can be concentrating under reduced pressure.Temperature can be at about 0 ℃ to about 80 ℃, and for example approximately room temperature to about 80 ℃, preferably is no more than about 60 ℃; For example about 0 ℃ to about 60 ℃; For example about 50-60 ℃, as about 55 ℃.The concentrated of step (5) can be also lyophilization.
A kind of common method is evaporation, atmospheric evaporation for example, reduction vaporization, thin film evaporation etc.
Can carry out drying after after concentrated, constant pressure and dry for example, drying under reduced pressure, spray drying, lyophilization etc.Drying is not necessary step, but preferred in certain embodiments.
In some embodiment, concentration step also can omit.For example, can directly use leachate, for example directly take to the patient or directly prepare as raw material the compositions that contains Rhizoma Ligustici.
Water extract of the present invention (as the extractum after decoction liquor or concentrate drying) can also further carry out purification.This can adopt one or more in many purification process known in the art to carry out.In purge process, the existence of best detection active component.
In the present invention, described Rhizoma Ligustici vegetable material can be Ligusticum sinense Oliv and Ligusticum jeholense Nakai et Kitag and Conioselinum uaginatum (Spreng.) Thell or their combination.
In the inventive method, described Rhizoma Ligustici vegetable material can be Rhizoma Ligustici plant Herb or any part, and for example its organ, tissue or cell, comprise flower, fruit, seed, stem, leaf, root, preferably the under ground portion of Rhizoma Ligustici, RUGEN and rhizome.The Rhizoma Ligustici vegetable material can be medical material, can be also crude drug.The Rhizoma Ligustici vegetable material can be tissue culture, cell culture.The Rhizoma Ligustici plant can be natural or genetically modified.The Rhizoma Ligustici material can be drying or fresh.
In extracting method of the present invention, described Rhizoma Ligustici vegetable material can be through pretreated.These processing comprise physical treatment, chemical treatment, biological treatment etc.For example: the Rhizoma Ligustici vegetable material can be simply to wash in advance, pulverize.In one embodiment, can use in advance organic solvent extraction before extracting the Rhizoma Ligustici vegetable material with aqueous solvent.Organic solvent includes but not limited to: petroleum ether, chloroform, ethyl acetate, ether, methanol, ethanol, propanol.Isopropyl alcohol, acetone or n-butyl alcohol or their any combination etc., as ether, as ethanol as 95% ethanol.
In the present invention, described " aqueous solvent " is any moisture solvent, and it can be water or the aqueous solution that contains organic solvent; Wherein organic solvent can be methanol, ethanol, propanol, acetone or n-butyl alcohol or their any combination.Water can be for example distilled water, ion exchange water or tap water.Aqueous solvent can also add the extraction water of suitable other material.Other material can be such as organic solvent, buffer agent, acid or alkali etc.Preferably, described moisture or contain the aqueous solution of organic solvent.In aqueous solvent, the content of water (volume ratio) can be for example about at least 5%, 10%, 20%, 30%, 40%, 50%, 60%, 70%, 80%, 90%, 95% or higher, preferably about at least 10%, more preferably about at least 20%, 50% or more.
On the other hand, the present invention relates to the water extract (perhaps water extraction) of Rhizoma Ligustici.
" water extract (the perhaps water extraction) " of Rhizoma Ligustici of the present invention refers to by with aqueous solvent (as water or contain the water of organic solvent), the Rhizoma Ligustici extract that extracts from the Rhizoma Ligustici vegetable material, and this Rhizoma Ligustici extract thing can be used for treating rhinitis.
Water extract of the present invention can obtain by the extracting method of the present invention of above definition.
On the other hand, the present invention relates to the water extract of the Rhizoma Ligustici that can obtain by any method of the present invention.
For example, can pass through decocting method, infusion process, percolation or steam distillation etc. and extract (perhaps leaching) Rhizoma Ligustici vegetable material, obtain leachate.Then, randomly concentrate, dry or purification or their any combination.
Gained extractum or purified product can further be mixed with the purpose compositions, as pharmaceutical composition, health composition, food compositions or beverage composition for treating dental erosion.
Mainly contain coumarin, lactone, alkaloid, polyphenol, flavone, organic acid, sugar and peptide constituents in extract of the present invention.
Extract of the present invention has the effect that improves allergic rhinitis, and the medicine that it can be used for preparing Prevention or treatment rhinitis comprises oral medicine and injection, also can prepare health product.
On the other hand, the present invention relates to contain the compositions of Rhizoma Ligustici water extract of the present invention.Preferably, said composition also contains excipient or carrier.
In specific embodiments, described compositions is pharmaceutical composition, health composition, food compositions or beverage composition for treating dental erosion.
The method that Rhizoma Ligustici water extract of the present invention is mixed with the purpose compositions is known in the art.According to different needs, those skilled in the art of the invention can select suitable additive, compound method, dosage form, unit dose etc.
When the present composition is pharmaceutical composition, can contain suitable pharmaceutical excipient, carrier or diluent.Can adopt the known technology of pharmaceutical field to carry out preparation.
Pharmaceutical composition of the present invention can adopt multiple dosage form, and this often depends on route of administration.For example, Rhizoma Ligustici water extract of the present invention can for the preparation of the medicine for the treatment of rhinitis, comprise the preparation that oral medicine and parenteral are used, as injection.Drug regimen of the present invention can pass through the number of ways administration, such as oral, parenteral etc.Dosage regimen mediating recipe amount depends on many factors, as route of administration, patient health situation etc., and can be determined by the doctor.Dosage range can be determined by normal experiment by those skilled in the art.
On the other hand, the compositions that the present invention relates to Rhizoma Ligustici extract or Rhizoma Ligustici water extract is for the preparation of the purposes in the medicine for the treatment of rhinitis.
On the other hand, the present invention relates to Rhizoma Ligustici vegetable material or its extract (preferred water extract) for the production of the purposes in the compositions that can be used for rhinitis.Described compositions is pharmaceutical composition, health composition, food compositions or beverage composition for treating dental erosion preferably.On the other hand, the present invention relates to a kind of method for the treatment of rhinitis, comprise to the patient giving Rhizoma Ligustici vegetable material or its extract (comprising water extract) or containing the compositions of this extract or other product after by Rhizoma Ligustici materials processing.
" patient " comprises any animal, preferred mammal, particularly house pet, letting animals feed.In a preferred embodiment, the patient is the people." patient " suffers from or suspects individuality or the normal individual of suffering from rhinitis.Therefore, Rhizoma Ligustici vegetable material of the present invention or extract (preferred water extract) or contain the compositions of this extract or the purposes of other product after by the processing of Rhizoma Ligustici vegetable material not only comprises treatment also comprise the prevention rhinitis.
Embodiment 1
Rhizoma Ligustici (Ligusticum sinense Oliv) root and rhizome 1kg adds 95% ethanol 8L reflux, extract.Filter, merging filtrate, centrifugal, 45 ℃ of concentrating under reduced pressure of supernatant are to ethanol extraction extractum 51 grams, yield 5.1%.Residue 1kg after ethanol extraction decocts 1hr with distilled water 8L, and residue decocts twice with the 4L distilled water at every turn continuously, and each 1hr filters, merging filtrate, and concentrating under reduced pressure is dried to get the water extracted immersing paste 110.3 grams, yield 11.03% for 55 ℃.
Rhizoma Ligustici (Ligusticum jeholense Nakai et Kitag) root and rhizome 1kg adopts same method to extract, alcohol extract yield 4.8%, water extraction extract yield 10.2%.
Xinjiang Rhizoma Ligustici (Conioselinum uaginatum (Spreng.) Thell) root and rhizome 1kg adopts same method to extract, alcohol extract yield 5.5%, water extraction extract yield 12.3%
Embodiment 2
Water extract to three kinds of Rhizoma Ligusticis carries out qualitative reaction, and analysis result is as follows:
Figure BSA00000726972400041
The qualitative examination result shows in these two kinds of Rhizoma Ligustici water extracts and all contains coumarin, lactone, alkaloid, polyphenol, flavone, organic acid, sugar and peptides.
Embodiment 3
Rat is divided into 6 groups at random, 10 every group, is respectively blank group, model group, the high, medium and low dosage group of medicine Rhizoma Ligustici and hismanal group.Except the blank group gave isopyknic normal saline, other 5 groups with 0.3mg, Al (OH) 3300mg, the suspension lumbar injection that adds the 1ml normal saline to make, 1 time every other day, totally 8 times.With 5%OVA normal saline solution collunarium, every side nostril 50ul, was total to every day 1 time since the 16th day.10 times.Normal group is with isopyknic physiologic saline for substitute.After collunarium excited, the number of times of observation rat sneeze in 30min, the intensity of scratching nose, observation were drawn nasal cavity secretions repeatedly with filter paper after finishing, and the difference before and after drawing is counted the nasal secretion amount.Adopt the addition method to calculate total points, total points surpasses 6 and is divided into the model success.Rhinocnesmus: without scratching nose 0 minute, slightly scratched nose 1 minute, frequently scratched nose (10~20 times per minute) 2 minutes, scratched nose more than 3 minutes; Sneeze: without sneeze 0 minute, 1~3 of sneeze 1 minute, 4~10 2 minutes, greater than 11 3 minutes; Nasal mucus: without nasal mucus 0 minute, flow to prenaris 1 minute, exceeded prenaris 2 minutes, full 3 minutes of nasal mucus stream.After the model success, gavage gives Rhizoma Ligustici (Ligusticum sinense Oliv) high dose group 1g/kg, middle dosage group 0.5g/kg, low dose group 0.25g/kg (amount of water extract is pressed the amount of the water extract extractum of embodiment 1 and calculated), hismanal group 0.3mg/kg, successive administration 10 days.The results are shown in Table 1,2,3,4
Table 1 rat sneeze number relatively
Figure BSA00000726972400042
Compare ###p<0.001 compares with model group with the blank group *P<0.01
During table 2 administration, rat is scratched the nose strength ratio
Figure BSA00000726972400044
Compare ###p<0.001 compares with model group with the blank group *P<0.01
Table 3 rat nasal secretion
Figure BSA00000726972400052
Figure BSA00000726972400053
Compare ###p<0.001 compares with model group with the blank group *P<0.01
The table of integrals before and after the administration of table 4 rat
Figure BSA00000726972400054
Group n Dosage Integration before administration Integration after administration
Normal group 10 - 4.31±2.31 4.42±2.62
Model group 10 - 7.69±3.68 8.21±4.32#
Low dose group 10 0.25g/kg 7.88±3.81 5.12±3.62 *
Middle dosage group 10 0.5g/kg 7.29±3.43 4.80±3.21 *
High dose group 10 1g/kg 7.90±3.84 4.68±3.72 *
The hismanal group 10 0.3mg/kg 7.63±4.08 4.53±3.24 *
Compare #p<0.05 compares with model group with the blank group *P<0.05
Table 5 rat blood serum histamine, IgE content
Figure BSA00000726972400055
Group n Dosage Histamine (mg/L) IgE(pg/ml)
Normal group 10 - 6.13±0.68 27.69±2.31
Model group 10 - 13.38±1.29### 63.38±4.96###
Low dose group 10 0.25g/kg 7.58±0.82 * 43.88±3.63
Middle dosage group 10 0.5g/kg 6.95±0.76 ** 39.47±3.21 ▲▲
High dose group 10 1g/kg 6.42±0.68 ** 32.43±2.98 ▲▲
The hismanal group 10 0.3mg/kg 6.28±0.70 ** 30.97±2.68 ▲▲
Compare ###p<0.001 compares with model group with the blank group *P<0.05, *P<0.01; P<0.05, ▲ ▲P<0.01
Embodiment 4
Rhizoma Ligustici water extract 200g, medical starch is appropriate, and both fully mix, and are encapsulated, make 100 capsules, and every heavy 0.25 gram contains 200 milligrams of Rhizoma Ligustici water extract.

Claims (10)

1. compositions that is used for prevention or treatment rhinitis, it contains useful aqueous solvent and extracts the Rhizoma Ligustici water extract that the Rhizoma Ligustici vegetable material obtains, and randomly, also contains excipient or carrier.
2. the compositions of claim 1, wherein, described compositions is pharmaceutical composition, health composition, food compositions or beverage composition for treating dental erosion.
3. the compositions of claim 1, wherein said Rhizoma Ligustici vegetable material is the Rhizoma Ligustici herb.The compositions of claim 1, described Rhizoma Ligustici vegetable material is root and rhizome.
4. the compositions of claim 1, wherein said aqueous solvent are the water of the water of water or acidify or alkalization or aqueous solution or the aqueous solution that contains organic solvent acidify or alkalization that contains organic solvent.
5. the compositions of claim 5, wherein organic solvent is methanol, ethanol, propanol, acetone or n-butyl alcohol or their any combination.
With aqueous solvent extract any one compositions of Rhizoma Ligustici water extract that the Rhizoma Ligustici vegetable material obtains or claim 1-6 in preparation due to the purposes in the medicine of prevention or treatment rhinitis.
7. the purposes of claim 7, wherein said Rhizoma Ligustici vegetable material is the Rhizoma Ligustici herb.The purposes of claim 7, described Rhizoma Ligustici vegetable material is root and rhizome.The purposes of claim 7, wherein said aqueous solvent are water water or acidify or alkalization or the aqueous solution that contains organic solvent or the aqueous solution organic solvent that contains organic solvent acidify or alkalization.
8. the purposes of claim 10, wherein organic solvent is methanol, ethanol, propanol, acetone or n-butyl alcohol or their any combination.
9. Rhizoma Ligustici vegetable material or extract thing are for the production of can be used for preventing or treating purposes in the compositions of rhinitis.
10. the purposes of claim 12, wherein said extract is water extract.The purposes of claim 12, wherein said compositions is pharmaceutical composition, health composition, food compositions or beverage composition for treating dental erosion.
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