CN105147661B - Application of the macrotin in the medicine or food for preparing preventing and treating ulcerative colitis - Google Patents
Application of the macrotin in the medicine or food for preparing preventing and treating ulcerative colitis Download PDFInfo
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- CN105147661B CN105147661B CN201510478295.8A CN201510478295A CN105147661B CN 105147661 B CN105147661 B CN 105147661B CN 201510478295 A CN201510478295 A CN 201510478295A CN 105147661 B CN105147661 B CN 105147661B
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- macrotin
- ulcerative colitis
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Abstract
The present invention relates to medicine, more particularly to a kind of medical usage of macrotin.The macrotin of the present invention can be used for preventing and treating ulcerative colitis.
Description
Technical field
The present invention relates to Medicines and Health Product field, more particularly to a kind of medical usage of macrotin.
Background technology
Ulcerative colitis (Ulcerative colitis, UC) is chronic, recurrent exerbation the inflammation for betiding colon
Property enteropathy (Inflammatory bowel disease, IBD).Clinic is mainly shown as diarrhoea, mucus pus and blood stool, stomachache.It is main
Complication is wanted to have:Bleeding, enterobrosis, anal fistula, intestinal obstruction, colon cancer and infectious shock etc..
Treatment UC Western medicine mainly has aminosalicylic acids, glucocorticoids and immunodepressant at present.Effect is all
It is not highly desirable, and side effect is big, is not easy long-term use.Salicylazosulfapyridine (SASP) is current clinical the most frequently used Western medicine, is fitted
For moderate, slight and chronic UC patient.Sulfapryidine and 5-aminosalicylic acid are decomposed into the intestine after oral.To colon intestinal wall
Tissue has special affinity, plays antiinflammatory action.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 SASP sulfapyridine moiety.
Macrotin (Cimifugin) is primarily present a kind of chromogen ketones component in Chinese Drug Fangfeng.
The content of the invention
The purpose of the present invention aims to provide a kind of new medical usage of macrotin.
Specifically, the invention provides a kind of macrotin in the medicine or food for preparing preventing and treating ulcerative colitis
Using.
In a preference, the macrotin is to be used to prepare preventing and treating ulcerative colitis as unique active component
Medicine 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.
Brief description of the drawings
Fig. 1-Fig. 4 embodies therapeutic action of the macrotin to ulcerative colitis:
Fig. 1 embodies influence of the macrotin to ulcerative colitis mouse weight;
Fig. 2 embodies influence of the macrotin to ulcerative colitis mouse bloody stool incidence;
Fig. 3 embodies influence of the macrotin to ulcerative colitis mouse Colon length;
Fig. 4 embodies influence of the macrotin to ulcerative colitis mouse Colon Histopathological lesions.
(in figure:A represents Normal group, and b represents model control group, and c represents macrotin group)
Embodiment
The appearance part of the present invention is had been surprisingly found that based on such a:Macrotin can be obviously improved ulcerative colitis
The symptoms such as weight loss, bloody stool, colon shortening and the Histopathological lesions of mouse, therefore, macrotin can be used for preparing preventing and treating intestines
The medicine or food of inflammation, particularly ulcerative colitis.
And then the application the invention provides macrotin in the medicine or food for preparing preventing and treating ulcerative colitis.
The molecular formula of the macrotin of the present invention:C16H18O6, molecular weight:306.31 its structural formula is as follows:
The macrotin of the present invention can be biological from Chengdu Man Site bio tech ltd, Shanghai source leaf by commercial sources
Science and Technology Ltd. etc. purchase obtains.Its purity meets medicinal standard.The purity of macrotin with>98% is optimal.
The macrotin of the present invention can be used alone or be used in the form of pharmaceutical composition.Pharmaceutical composition includes conduct
The macrotin and pharmaceutical acceptable carrier of the invention of active component.It is preferred that the pharmaceutical composition of the present invention contains 0.1-99.9%
The macrotin of the invention as active component of percentage by weight." pharmaceutical acceptable carrier " will not destroy the macrotin 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 is not limited to:Soft phosphatide, aluminum stearate, aluminum 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 conventional 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, Ac-Di-Sol, low-substituted hydroxypropyl
Base cellulose), lubricant (such as magnesium stearate) and sorbefacient, absorption carrier, flavouring agent, sweetener, excipient, dilution
Agent, wetting agent etc..
The macrotin of the present invention and its pharmaceutical composition can be prepared by this area conventional method and can by enteron aisle or
Non-bowel or topical routes.Oral formulations include capsule, tablet, oral liquid, granule, pill, powder, sublimed preparation, cream
Agent etc.;Non-intestinal drug delivery agent is including parenteral solution etc.;Local administration preparation includes creme, patch, ointment, spray etc..It is excellent
Elect oral formulations as.
The macrotin of the present invention and the method for administration of its pharmaceutical composition can be oral, sublingual, percutaneous, through muscle or
Subcutaneously, mucocutaneous, vein, urethra, vagina etc..
In addition to medicament is made, it is various also antioxidant, pigment, enzyme preparation etc. can be added in the macrotin of the present invention
Food additives, health food is made by the conventional method of this area.
With reference to specific embodiment, the present invention is expanded on further.It should be understood that these embodiments are merely to illustrate the present invention
Rather than limitation the scope of the present invention.The experimental method of unreceipted actual conditions in the following example, generally according to conventional strip
Part or according to the condition proposed by manufacturer.Unless otherwise indicated, otherwise all percentage, ratio, ratio or number is pressed
Weight meter.
Unless otherwise defined, anticipated known to all specialties used in text and scientific words and one skilled in the art
Justice is identical.In addition, any method similar or impartial to described content and material all can be applied in the inventive method.Wen Zhong
Described preferable implementation only presents a demonstration with material to be used.
The features described above that the present invention mentions, or the feature that embodiment is mentioned can be in any combination.Patent specification is taken off
All features shown can be used in combination with any combinations thing form, each feature disclosed in specification, can provide phase with any
The alternative characteristics substitution of same, impartial or similar purpose.Therefore except there is special instruction, disclosed feature is only impartial or similar
The general example of feature.
Embodiment 1:
1st, experiment material
1.1 medicinal material
Macrotin (CAS:37921-38-3, molecular weight 306.31, 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).
1.2 experimental animal
20 ± 2g of body weight C57BL/6 female mices (8 weeks), are provided by Shanghai Univ. of Traditional Chinese Medicine's Experimental Animal Center, are moved
Thing quality certification number:SYXK (Shanghai) 2009-0069.It is placed in conventinal breeding environment, ad lib and drinking-water.
2nd, experimental method
The foundation of 2.1 Ulcerative Colitis Models
The homogeneous C57BL/6 female mices (20 ± 2g) of body weight are selected, 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 4% (w/v) DSS, freely drunk 7 days, to draw
Play ulcerative colitis.
2.2 packets and medication
Normal group:10, give normal diet.
Model control group:10, give 4%DSS solution and freely drink 7 days.
Macrotin group:10, gavage gives macrotin (50mg/kg) continuous 7 days while giving 4%DSS solution.
It is fresh daily to prepare dosage particles during experiment, dissolved with 0.5% sodium carboxymethylcellulose, and it is small preparing 1
When interior use.
The assessment of 2.3 enteritis
Diarrhoea, 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).Record body weight becomes daily during experiment
Change, diarrhoea and bloody stool symptom.Anesthesia and cervical dislocation put to death mouse after experiment terminates, and opening abdominal cavity, take out colon, measure from blind
Colon lengths of the intestines to rectum.And take terminal colon to do histotomy, H&E dyeing is carried out, dyeing colon sample to H&E carries out disease
Reason scoring:(1) inflammatory cell oozes out standards of grading:There is very small amount inflammatory cell in 0 point-mucosa lamina propria, 1 point-mucous membrane is solid
Having has the inflammatory cell in more inflammatory cell or mucosa lamina propria to increase in layer, 2 points-inflammatory cell is diffused under mucous membrane
Layer, 3 points-holostrome have inflammatory cell to ooze out;(2) tissue damage standards of grading:0 point-without mucosa injury, 1 point-discrete glutinous
Film epithelial lesions, 2 points-top 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, calculate histopathology scoring (1-6 points).
2.4 statistical analysis
All experimental datas are repeated 3 times, and are as a result represented with mean+SD, using the statistical softwares of SPSS 16.0
Experimental data is examined using One-way ANOVA (One-way ANOVA) and LSD, P<0.05 has significantly for statistically difference
Property.
3rd, result
The influence of 3.1 pairs of ulcerative colitis mouse weights
Fig. 1 embodies influence of the macrotin to ulcerative colitis mouse weight, as seen from Figure 1:Normal group mouse
Increased weight 0.9 ± 0.8%, the weight loss of model group mouse 8.2 ± 0.9%, the body weight of macrotin group mouse subtracts
It is light by 4.4 ± 0.6%;Further illustrate that macrotin can significantly inhibit the Body weight loss of ulcerative colitis mouse caused by DSS
(P<0.01)。
The influence of 3.2 pairs of ulcerative colitis mouse bloody stool incidences
Fig. 2 embodies influence of the macrotin 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%, the bloody stool incidence of macrotin group mouse
For 56.7 ± 5.8%;Further illustrate that macrotin can substantially reduce the bloody stool rate (P of ulcerative colitis mouse caused by DSS<
0.01)。
The influence of 3.3 pairs of ulcerative colitis mouse Colon length
Fig. 3 embodies influence of the macrotin to ulcerative colitis mouse Colon length, as seen from Figure 3:Normal group
Mouse shortens without colon and occurred, and the colon LVFS of model group mouse is 35.3 ± 0.6%, and the colon of macrotin group mouse shortens
Rate is 22.2 ± 0.4%;Further illustrate that macrotin can significantly improve the colon shortening of ulcerative colitis mouse caused by DSS
Symptom (P<0.05).
The influence of 3.4 pairs of ulcerative colitis mouse Colon histopathologies
The colon of model group mouse shows for exemplary inflammatory mucous membrane, mucous membrane, the submucosa even a large amount of inflammatories of muscle layer
Cellular infiltration, institutional framework is disorderly, fracture, submucosa bleeding, oedema, telangiectasis;The colon of macrotin group mouse
Lesion tissue mitigates, ulcer healing, and submucosa bleeding mitigates.Fig. 4 embodies macrotin to ulcerative colitis mouse Colon
The injury repair effect of tissue.As seen from Figure 4:The score of Normal group mouse is 0, the score of model group mouse for 5.7 ±
0.3%, the score of macrotin group mouse is 4.6 ± 0.4%, and compared with model group, difference has conspicuousness (P<0.01).Illustrate rattletop
Element can significantly mitigate colonic mucosa inflammation cellular infiltration and Histopathological lesions symptom (P<0.01).
To sum up result of study shows:Macrotin can be obviously improved the Body weight loss of ulcerative colitis mouse, bloody stool hair
Raw rate, colon LVFS and Histopathological lesions symptom.
Many aspects involved in the present invention have been explained as above.However, it should be understood that without departing from spirit of the invention
Under the premise of, those skilled in the art can carry out equivalent change and modification to it, and the change and modification equally fall into the application
The coverage of appended claims.
Claims (2)
1. application of the macrotin in the medicine or food for preparing preventing and treating ulcerative colitis.
2. application as claimed in claim 1, it is characterised in that the macrotin is to be used to prepare as unique active component
Prevent and treat the medicine or food of ulcerative colitis.
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防风对溃疡性结肠炎治疗作用的研究;席向阳;《中国优秀硕士学位论文全文数据库 医药卫生科技辑(月刊)》;20091016(第11期);第38-40、60页 * |
防风有效部位的药理作用研究;李文等;《中国实验方剂学杂志》;20060630;第12卷(第6期);第29-31页 * |
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