CN105079012B - Application of the Gastrodin in the drug or food for preparing prevention ulcerative colitis - Google Patents
Application of the Gastrodin in the drug or food for preparing prevention ulcerative colitis Download PDFInfo
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- CN105079012B CN105079012B CN201510478294.3A CN201510478294A CN105079012B CN 105079012 B CN105079012 B CN 105079012B CN 201510478294 A CN201510478294 A CN 201510478294A CN 105079012 B CN105079012 B CN 105079012B
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- gastrodin
- ulcerative colitis
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Abstract
The present invention relates to medicines, more particularly to a kind of medical usage of Gastrodin.The Gastrodin of the present invention can be used for preventing ulcerative colitis.
Description
Technical field
The present invention relates to Medicines and Health Product fields, more particularly to a kind of medical usage of Gastrodin.
Background technology
Ulcerative colitis (Ulcerative colitis, UC) is chronic, recurrent exerbation the inflammation for betiding colon
Property enteropathy (Inflammatory bowel disease, IBD).Clinical manifestation is diarrhea, mucus pus and blood stool, abdominal pain.It is main
Complication is wanted to have：Bleeding, enterobrosis, anal fistula, intestinal obstruction, colon cancer and infectious shock etc..
The Western medicine for the treatment of UC mainly has aminosalicylic acids, glucocorticoids and immunosuppressor at present.Effect is all
It is not highly desirable, and side effect is big, is not easy to be used for a long time.Salicylazosulfapyridine (SASP) is current clinical most common Western medicine, is fitted
For moderate, slight and chronic UC patient.It is decomposed into sulfapryidine and 5-aminosalicylic acid in the intestine after oral.To colon intestinal wall
Group is woven with special affinity, plays anti-inflammatory effect.Have after oral SASP 10%~40% patient occur nausea, indigestion,
The adverse reactions such as headache, leucocyte decline, occasionally have and cause arthralgia, fash, albuminuria and pancreatitis etc., most adverse reactions are all
It is attributed to the sulfapyridine moiety of SASP.
Gastrodin (Gastrodin) is a kind of chemical composition extracted from rare Chinese medicine Rhizoma Gastrodiae, has calm, town
Bitterly, the multiple pharmacological effects such as neuron, sleeping and anticonvulsion, anti-epileptic, anti-oxidant, improvement microcirculation, improvement memory are protected.Face
It is widely used in the diseases such as dizziness, vestibular neuronitis, vertebrobasilar insufficiency, headache, neurasthenia and hypertension on bed
Treatment.
Invention content
The purpose of the present invention is intended to provide a kind of new medical usage of Gastrodin.
Specifically, the present invention provides a kind of Gastrodins in the drug or food for preparing prevention ulcerative colitis
Using.
In a preferred example, the Gastrodin is to be used to prepare prevention ulcerative colitis as unique active constituent
Drug or food.
The details of various aspects of the present invention will be able to detailed description in subsequent chapters and sections.By hereafter and claim
Description, the features of the present invention, purpose and advantage will become apparent from.
Description of the drawings
Fig. 1-Fig. 4 embodies therapeutic effect of the Gastrodin to ulcerative colitis：
Fig. 1 embodies influence of the Gastrodin to ulcerative colitis mouse weight；
Fig. 2 embodies influence of the Gastrodin to ulcerative colitis mouse bloody stool incidence；
Fig. 3 embodies influence of the Gastrodin to ulcerative colitis mouse Colon length；
Fig. 4 mouse Colon tissue pathological slices embody Gastrodin to ulcerative colitis mouse Colon Histopathological lesions
Influence；
The scoring of Fig. 5 mouse Colon histopathologies embodies Gastrodin to ulcerative colitis mouse Colon Histopathological lesions
Influence；
(in figure：A indicates that Normal group, b indicate that model control group, c indicate that SASP groups, d indicate Gastrodin group)
Specific implementation mode
The appearance part of the present invention is had been surprisingly found that based on such a：Gastrodin can be obviously improved ulcerative colitis
The weight loss of mouse, bloody stool, colon shorten and the symptoms such as Histopathological lesions, and therefore, Gastrodin can be used for preparing prevention intestines
The drug or food of inflammation, especially ulcerative colitis.
In turn, the application the present invention provides Gastrodin in the drug or food for preparing prevention ulcerative colitis.
The molecular formula of the Gastrodin of the present invention：C13H18O7, molecular weight：286.28 structural formula is as follows：
The Gastrodin of the present invention can be by commercial sources from the Chengdu bio tech ltd Man Site, Sichuan Province Wei Keqi
Bio tech ltd etc. purchase obtains.Its purity meets medicinal standard.The purity of Gastrodin with>98% is best.
The Gastrodin of the present invention can be used alone or be used in the form of pharmaceutical composition.Pharmaceutical composition includes conduct
The Gastrodin and pharmaceutical acceptable carrier of the present invention of active constituent.Preferably, the pharmaceutical composition of the present invention contains 0.1-99.9%
The Gastrodin of the present invention as active constituent of weight percent." pharmaceutical acceptable carrier " will not destroy the Gastrodin of the present invention
Pharmaceutical active, while its effective dose, dosage when can play pharmaceutical carrier effect are nontoxic to human body.
Described pharmaceutical acceptable carrier includes but not limited to：Soft phosphatide, aluminum stearate, aluminium oxide, ion exchange material, self-emulsifying
Drug delivery system, tween or other surfaces activator, haemocyanin, buffer substance for example phosphate, amion acetic acid, sorbic acid,
Water, salt, electrolyte such as sulfate protamine, disodium hydrogen phosphate, potassium hydrogen phosphate, sodium chloride, zinc salt, magnesium silicate, saturated fatty acid
Partial glyceride mixtures etc..
Other common excipient substance such as adhesives (such as microcrystalline cellulose), filler (such as starch, glucose, anhydrous lactitol
Sugar and lactose bead), disintegrant (such as cross-linked pvp, crosslinked carboxymethyl fecula sodium, croscarmellose sodium, low-substituted hydroxypropyl
Base cellulose), lubricant (such as magnesium stearate) and sorbefacient, absorption carrier, flavouring agent, sweetener, excipient, dilution
Agent, wetting agent etc..
The Gastrodin of the present invention and its pharmaceutical composition can be prepared by this field conventional method and can by enteron aisle or
Non-bowel or topical routes.Oral preparation includes capsule, tablet, oral solution, granule, pill, powder, sublimed preparation, cream
Agent etc.；Non-intestinal drug delivery agent includes injection etc.；Local administration preparation includes creme, patch, ointment, spray etc..It is excellent
It is selected as oral preparation.
The Gastrodin of the present invention and the administration route of its pharmaceutical composition can be oral, sublingual, percutaneous, through muscle or
Subcutaneously, mucocutaneous, vein, urethra, vagina etc..
Other than medicament is made, it is various also antioxidant, pigment, enzyme preparation etc. can be added in the Gastrodin of the present invention
Health food is made by the conventional method of this field in food additives.
Present invention will be further explained below with reference to specific examples.It should be understood that these embodiments are merely to illustrate the present invention
Rather than it limits the scope of the invention.In the following examples, the experimental methods for specific conditions are not specified, usually according to conventional strip
Part or according to the normal condition proposed by manufacturer.Unless otherwise stated, otherwise all percentage, ratio, ratio or number is pressed
Weight meter.
Unless otherwise defined, all professional and scientific terms used in text and meaning known to one skilled in the art
Justice is identical.In addition, any method and material similar or impartial to described content can be applied to the method for the present invention.Wen Zhong
The preferred implement methods and materials are for illustrative purposes only.
The feature that the features described above or embodiment that the present invention mentions are mentioned can be in any combination.Patent specification is taken off
All features shown can be used in combination with any composition form, and each feature disclosed in specification any can provide phase
The alternative characteristics substitution of same, impartial or similar purpose.Therefore it is only impartial or similar except having special instruction, revealed feature
The general example of feature.
Embodiment 1：
1, experiment material
1.1 medicinal material
Gastrodin (CAS：62499-27-8, molecular weight 286.28, HPLC purity >=98%, by Chengdu Man Site biologies section
Skill Co., Ltd produces)；Dextran sulfate sodium (DSS, CAS：9011-18-1, MW 36-50kDa, by U.S. MP
Biomedicals companies produce)；Salicylazosulfapyridine (SASP, CAS：599-79-1, molecular weight 398.39, HPLC purity >=
98%, produced by Sigma-Aldrich).
1.2 experimental animal
The C57BL/6 female mices (8 weeks) of 20 ± 2g of weight, are provided by Shanghai Univ. of Traditional Chinese Medicine's Experimental Animal Center, are moved
Object quality certification number：SYXK (Shanghai) 2009-0069.It is placed in conventinal breeding environment, ad lib and drinking-water.
2, experimental method
The foundation of 2.1 Ulcerative Colitis Models
The C57BL/6 female mices (20 ± 2g) for selecting weight uniform, using international ulcerative colitis modeling
Method (Gastroenterology 2002,123:256-70；PLoS One 2012,7:E36075), the incipient stage is being studied,
Make mouse ad lib and drinking-water, after the laundering period in the early stage into, water is changed to the DSS of 4% (w/v), freely drunk 7 days, to draw
Play ulcerative colitis.
2.2 groupings and medication
Normal group：10, give normal diet.
Model control group：It 10, gives 4%DSS solution and freely drinks 7 days.
SASP groups：10, gavage gives SASP and (is converted into mouse according to quantity to use while giving 4%DSS solution
Amount：520mg/kg) continuous 7 days.
Gastrodin group：10, gavage gives Gastrodin (50mg/kg) continuous 7 days while giving 4%DSS solution.
It is fresh daily to prepare dosage particles during experiment, it is dissolved with 0.5% sodium carboxymethylcellulose, and small preparing 1
When interior use.
The assessment of 2.3 enteritis
Diarrhea, bloody stool, histopathological analysis etc. publish thesis (PLoS One 2012,7 with reference to early-stage study:
e36075；J Pharmacol Exp Ther 2013,345:Method described in 473-82).Weight change is recorded during experiment daily
Change, diarrhea and bloody stool symptom.It is anaesthetized after experiment and cervical dislocation puts to death mouse, opened abdominal cavity, take out colon, measure from blind
Colon lengths of the intestines to rectum.And terminal colon is taken to do histotomy, H＆E dyeing is carried out, disease is carried out to H＆E dyeing colon samples
Reason scoring：(1) the exudation standards of grading of inflammatory cell：There are minute quantity inflammatory cell, 1 point-mucous membrane solid in 0 point-mucosa lamina propria
Having has the inflammatory cell in more inflammatory cell or mucosa lamina propria to increase in layer, 2 points-inflammatory cell diffuses under mucous membrane
Layer, 3 points-holostrome have inflammatory cell exudation；(2) tissue damage standards of grading：0 point-without mucosa injury, 1 point-discrete glutinous
Film epithelial lesions, 2 points-surface layer mucosal erosion, 3 points-extensive mucous membrane is damaged and is extended to intestinal wall deep layer.By oozing for inflammatory cell
Go out score to be added with tissue damage score, calculates histopathology scoring (1-6 points).
2.4 statistical analysis
All experimental datas are repeated 3 times, and are as a result indicated with mean+SD, using 16.0 statistical softwares of SPSS
Experimental data is examined using One-way ANOVA (One-way ANOVA) and LSD, P<0.05 has significantly for statistically difference
Property.
3, result
The influence of 3.1 pairs of ulcerative colitis mouse weights
Fig. 1 embodies influence of the Gastrodin to ulcerative colitis mouse weight, as seen from Figure 1：Normal group mouse
Weight gain 0.9 ± 0.8%, the weight loss of model group mouse 8.2 ± 0.9%, the weight of positive controls mouse
Alleviate 4.6 ± 0.9%, the weight loss of Gastrodin group mouse 2.1 ± 0.9%；Further illustrate that Gastrodin can significantly press down
Weight loss (the P of ulcerative colitis mouse caused by DSS processed<0.001)；Also, in the case of being administered orally, Gastrodin
(50mg/kg) is better than positive control drug SASP (520mg/kg) (P to the inhibiting effect significant effect of weight loss<0.05).
The influence of 3.2 pairs of ulcerative colitis mouse bloody stool incidences
Fig. 2 embodies influence of the Gastrodin to ulcerative colitis mouse bloody stool incidence, as seen from Figure 2：Normal control
Group mouse occurs without bloody stool, and the bloody stool incidence of model group mouse is 96.7 ± 5.8%, and the bloody stool of positive controls mouse occurs
Rate is 53.3 ± 5.8%, and the bloody stool incidence of Gastrodin group mouse is 33.3 ± 5.8%；Further illustrate that Gastrodin can be significantly
Reduce the bloody stool rate (P of ulcerative colitis mouse caused by DSS<0.001)；Also, in the case of being administered orally, Gastrodin
(50mg/kg) is better than positive control drug SASP (520mg/kg) (P to the inhibiting effect significant effect of bloody stool incidence<0.05).
The influence of 3.3 pairs of ulcerative colitis mouse Colon length
Fig. 3 embodies influence of the Gastrodin to ulcerative colitis mouse Colon length, as seen from Figure 3：Normal group
Mouse shortens without colon and occurs, and the colon shortening rate of model group mouse is 35.3 ± 0.6%, and the colon of positive controls mouse contracts
Short rate is 17.1 ± 0.2%, and the colon shortening rate of Gastrodin group mouse is 11.1 ± 0.4%；Further illustrate that Gastrodin can be shown
The colon for writing ulcerative colitis mouse caused by improving DSS shortens symptom (P<0.01)；Also, in the case of being administered orally, day
The improvement result significant effect that numb element (50mg/kg) shortens colon symptom is better than positive control drug SASP (520mg/kg) (P<
0.05)。。
The influence of 3.4 pairs of ulcerative colitis mouse Colon histopathologies
Fig. 4 and Fig. 5 embodies Gastrodin and acts on the injury repair of ulcerative colitis mouse Colon tissue, can by Fig. 4
See：The colonic tissue of model group mouse shows for exemplary inflammatory mucous membrane, it is seen that mucous membrane, the submucosa even a large amount of inflammatories of muscle layer are thin
Born of the same parents infiltrate, and institutional framework is disorderly, is broken, submucosa bleeding, oedema, telangiectasis；Positive controls mouse and Rhizoma Gastrodiae
The colonic tissue lesions visible of element group mouse mitigates, and ulcer healing, submucosa bleeding mitigates.As seen from Figure 5：Normal group
Mouse score is 0, and the score of model group mouse is 5.7 ± 0.3%, and the score of positive controls mouse is 3.2 ± 0.3%, Gastrodin
Group mouse score is 2.7 ± 0.2%, compared with model group, the significant (P of difference<0.001).Illustrate that Gastrodin can be notable
Mitigate colonic mucosa inflammation cellular infiltration and Histopathological lesions situation (P<0.001).Also, in the case of being administered orally, Rhizoma Gastrodiae
Plain (50mg/kg) is significantly better than positive control drug SASP (520mg/kg) (P to the repairing effect of colon pathology damage<0.01).
To sum up result of study shows：Gastrodin can be obviously improved the weight loss of ulcerative colitis mouse, bloody stool hair
Raw rate, colon shortening rate and Histopathological lesions symptom.Also, in the case of being administered orally, Gastrodin (50mg/kg) is to bursting
The weight loss of ulcer colitis mouse, bloody stool incidence, the improvement result of colon shortening rate and Histopathological lesions are notable
Better than positive control drug SASP (520mg/kg) (P<0.01).
Many aspects according to the present invention have done elaboration as above.However, it should be understood that without departing from spirit of that invention
Under the premise of, those skilled in the art can carry out it equivalent change and modification, and the change and modification equally fall into the application
The coverage area of appended claims.
Claims (2)
1. Gastrodin prepare the prevention intestinal inflammatory of ulcerative colitis, bleeding, ulcer drug in application.
2. application as described in claim 1, which is characterized in that the Gastrodin is used to prepare as unique active constituent
Prevent the intestinal inflammatory of ulcerative colitis, bleeding, ulcer drug.
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| CN201510478294.3A CN105079012B (en) | 2015-08-07 | 2015-08-07 | Application of the Gastrodin in the drug or food for preparing prevention ulcerative colitis |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102613551A (en) * | 2012-03-28 | 2012-08-01 | 浙江农林大学 | Health food for improving intestinal function, and making method and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102613551A (en) * | 2012-03-28 | 2012-08-01 | 浙江农林大学 | Health food for improving intestinal function, and making method and application thereof |
Non-Patent Citations (3)
| Title |
|---|
| 5-羟色胺与焦虑、抑郁的关系及其在溃疡性结肠炎发病中的作用;田志颖 等;《胃肠病学和肝病学杂志》;20110930;第20卷(第9期);827-828 * |
| 天麻素治疗腹泻型肠易激综合征的临床研究;王国彧;《中医药学报》;20121231;第40卷(第6期);75-77 * |
| 黄绿蜜环菌生物合成的天麻素抗炎及免疫调节活性评价;冯宇 等;《中国食品学报》;20111031;第11卷(第7期);41-45 * |
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