CN105147703A - Application of obakurone to preparation of medicines or food for preventing and treating ulcerative colitis - Google Patents
Application of obakurone to preparation of medicines or food for preventing and treating ulcerative colitis Download PDFInfo
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- CN105147703A CN105147703A CN201510478406.5A CN201510478406A CN105147703A CN 105147703 A CN105147703 A CN 105147703A CN 201510478406 A CN201510478406 A CN 201510478406A CN 105147703 A CN105147703 A CN 105147703A
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- ulcerative colitis
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Abstract
The invention relates to the field of medicines, in particular to medical application of obakurone which can be used for preventing and treating ulcerative colitis.
Description
Technical field
The present invention relates to Medicines and Health Product field, particularly relate to a kind of medical usage of obacunone.
Background technology
Ulcerative colitis (Ulcerativecolitis, UC) is the inflammatory bowel (Inflammatoryboweldisease, IBD) of chronic, the recurrent exerbation betiding colon.Clinical main manifestations is diarrhoea, mucus bloody purulent stool, stomachache.Major complications has: hemorrhage, intestinal perforation, anal fistula, intestinal obstruction, colon cancer and septic shock etc.
The Western medicine of current treatment UC mainly contains aminosalicylic acids, glucocorticoids and immunosuppressant.Effect is all not bery desirable, and side effect is large, not easily life-time service.Sulfasalazine (SASP) is current clinical the most frequently used Western medicine, is applicable to moderate, slight and chronic UC patient.Be sulfapyridine and 5-aminosalicylic acid at intestinal degradation after oral.There is special affinity to colon intestinal tissue, play antiinflammatory action.Have the patient of 10% ~ 40% to occur feeling sick after oral SASP, dyspepsia, headache, the untoward reaction such as leukopenia, occasionally have and cause arthralgia, erythra, albuminuria and pancreatitis etc., most untoward reaction is all owing to the sulfapyridine moiety of SASP.
Obacunone (Obacunone) is a kind of limonin constituents be mainly present in rutaceae, has anticancer, parasite killing, blood fat reducing isoreactivity.
Summary of the invention
Object of the present invention aims to provide a kind of new medical usage of obacunone.
Specifically, the invention provides a kind of obacunone and prepare the application in the medicine or food preventing and treating ulcerative colitis.
In a preference, described obacunone is for the preparation of medicine or the food of preventing and treating ulcerative colitis as unique active component.
The details of various aspects of the present invention is able to detailed description by chapters and sections subsequently.By hereafter and the description of claim, feature of the present invention, object and advantage will be more obvious.
Accompanying drawing explanation
Fig. 1-Fig. 4 embodies the therapeutical effect of obacunone to ulcerative colitis:
Fig. 1 embodies the impact of obacunone on ulcerative colitis Mouse Weight;
Fig. 2 embodies the impact of obacunone on ulcerative colitis mice hemafecia incidence rate;
Fig. 3 embodies the impact of obacunone on ulcerative colitis mouse Colon length;
Fig. 4 mouse Colon tissue pathological slice embodies the impact of obacunone on ulcerative colitis mouse Colon Histopathological lesions;
The scoring of Fig. 5 mouse Colon histopathology embodies the impact of obacunone on ulcerative colitis mouse Colon Histopathological lesions;
(in figure: a represents Normal group, b represents model control group, and c represents SASP group, and d represents obacunone group)
Detailed description of the invention
Appearance part of the present invention unexpected to find based on such one: obacunone obviously can improve the losing weight of ulcerative colitis mice, hemafecia, colon shorten and the symptom such as Histopathological lesions, therefore, obacunone can be used for preparation and prevents and treats enteritis, particularly the medicine of ulcerative colitis or food.
And then, the invention provides obacunone and prepare the application in the medicine or health food preventing and treating enteritis.
The molecular formula of obacunone of the present invention (obacunone): C
26h
30o
7, molecular weight: 454.51, its structural formula is as follows:
Obacunone of the present invention obtains from the purchase such as Sigma chemical company, Man Site bio tech ltd, Chengdu by commercial sources.Its purity all meets medicinal standard.The purity of obacunone is best with >98%.
Obacunone of the present invention can be used alone or uses with the form of pharmaceutical composition.Pharmaceutical composition comprises obacunone of the present invention as active component and pharmaceutically suitable carrier.Preferably, pharmaceutical composition of the present invention contains the obacunone of the present invention as active component of 0.1-99.9% percentage by weight." pharmaceutically suitable carrier " can not destroy the pharmaceutical active of obacunone of the present invention, simultaneously its effective dose, and consumption when can play pharmaceutical carrier effect is to human non-toxic.
Described pharmaceutically suitable carrier includes but not limited to: soft phospholipid, aluminium stearate, aluminium oxide, ion exchange material, self-emulsifying drug delivery system, tween or other surfactants, serum albumin, buffer substance are if phosphate, glycine, sorbic acid, water, salt, electrolyte are as sulfate protamine, sodium hydrogen phosphate, potassium hydrogen phosphate, sodium chloride, zinc salt, magnesium silicate, satisfied fatty acid partial glyceride mixtures etc.
Other conventional excipient substances are as binding agent (as microcrystalline Cellulose), filler (as starch, glucose, Lactis Anhydrous and lactose beadlet), disintegrating agent (as cross-linked pvp, crosslinked carboxymethyl fecula sodium, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose), lubricant (as magnesium stearate) and absorption enhancer, absorption carrier, flavouring agent, sweeting agent, excipient, diluent, wetting agent etc.
Obacunone of the present invention and its pharmaceutical composition can by the preparations of this area conventional method and can by intestinal or non-bowel or topical routes.Oral formulations comprises capsule, tablet, oral liquid, granule, pill, powder, sublimed preparation, unguentum etc.; Non-intestinal drug delivery agent comprises injection etc.; Local administration preparation comprises cream, patch, ointment, spray etc.Be preferably oral formulations.
The route of administration of obacunone of the present invention and its pharmaceutical composition can be oral, Sublingual, percutaneous, through muscle or subcutaneous, mucocutaneous, vein, urethra, vagina etc.
Except making medicament, also can add the various food additive such as antioxidant, pigment, enzyme preparation in obacunone of the present invention, make health food by the conventional method of this area.
Below in conjunction with specific embodiment, set forth the present invention further.Should be understood that these embodiments are only not used in for illustration of the present invention to limit the scope of the invention.The experimental technique of unreceipted actual conditions in the following example, the usually conveniently conditioned disjunction condition of advising according to manufacturer.Unless otherwise indicated, otherwise all percent, ratio, ratio or number by weight.
Unless otherwise defined, all specialties used in literary composition and scientific words and one skilled in the art the same meaning be familiar with.In addition, any method similar or impartial to described content and material all can be applicable in the inventive method.The use that better implementation method described in literary composition and material only present a demonstration.
The above-mentioned feature that the present invention mentions, or the feature that embodiment is mentioned can combination in any.All features that patent specification discloses can with any composition forms and use, each feature disclosed in description, anyly can provide identical, alternative characteristics that is impartial or similar object replaces.Therefore apart from special instruction, the feature disclosed is only general example that is impartial or similar features.
Embodiment 1:
1, experiment material
1.1 medical material
Obacunone (CAS:751-03-1, molecular weight 454.51, HPLC purity >=98% are produced by Man Site bio tech ltd, Chengdu); Dextran sulfate sodium (DSS, CAS:9011-18-1, MW36-50kDa are produced by MPBiomedicals company of the U.S.); Sulfasalazine (SASP, CAS:599-79-1, molecular weight 398.39, HPLC purity >=98%, is produced by Sigma-Aldrich).
1.2 laboratory animal
The C57BL/6 female mice (8 weeks) of body weight 20 ± 2g, is provided by Shanghai Univ. of Traditional Chinese Medicine's Experimental Animal Center, the animal quality certification number: SYXK (Shanghai) 2009-0069.Be placed in conventional feeding environment, ad lib and drinking-water.
2, experimental technique
The foundation of 2.1 Ulcerative Colitis Models
The C57BL/6 female mice (20 ± 2g) of selective body weight average one, adopts international ulcerative colitis modeling method (Gastroenterology2002,123:256-70; PLoSOne2012,7:e36075), in the research incipient stage, make mice ad lib and drinking-water, in the early stage after adaptive phase, water is changed into the DSS of 4% (w/v), freely drink 7 days, to cause ulcerative colitis.
2.2 grouping and medications
Normal group: 10, give normal diet.
Model control group: 10, gives 4%DSS solution and freely drinks 7 days.
SASP group: 10, while giving 4%DSS solution, gavage gives SASP and (is converted into mice consumption according to quantity: 350mg/kg) continuous 7 days.
Obacunone group: 10, while giving 4%DSS solution, gavage gives obacunone (50mg/kg) continuous 7 days.
Experimental session, every day is fresh prepares dosage particles, and the sodium carboxymethyl cellulose with 0.5% dissolves, and uses in 1 hour in preparation.
The assessment of 2.3 enteritis
Diarrhoea, hemafecia, histopathological analysis etc. all to publish thesis (PLoSOne2012,7:e36075 with reference to early-stage Study; JPharmacolExpTher2013,345:473-82) described in method.Experimental session records body weight change, diarrhoea and hemafecia symptom every day.Experiment terminates rear anesthesia and cervical dislocation puts to death mice, opens abdominal cavity, takes out colon, measures the colon lengths from caecum to rectum.And get DC and make tissue slice, carry out H & E to dye, pathological score is carried out to dye colon specimen of H & E: (1) inflammatory cell ooze out standards of grading: have minute quantity inflammatory cell in 0 point-mucosa lamina propria, the inflammatory cell in more inflammatory cell or mucosa lamina propria is had to increase in 1 point-mucosa lamina propria, 2 points-inflammatory cell diffuses to Submucosa, and 3 points-holostrome all has inflammatory cell to ooze out; (2) tissue damage standards of grading: 0 point-without mucosa injury, 1 point-discrete mucosal epithelium is damaged, 2 points-top layer mucosal erosion, and 3 points-mucosa breakage widely is also expanded to intestinal wall deep layer.Oozing out of inflammatory cell is scored and tissue damage score addition, calculates histopathology scoring (1-6 divides).
2.4 statistical analysis
All experimental datas all repeat 3 times, result represents with mean+SD, adopt SPSS16.0 statistical software to adopt one way analysis of variance (One-wayANOVA) and LSD inspection to experimental data, P<0.05 is that statistically difference has significance.
3 results
3.1 impacts on ulcerative colitis Mouse Weight
Fig. 1 embodies the impact of obacunone on ulcerative colitis Mouse Weight, as seen from Figure 1: the body weight of Normal group mice adds 0.9 ± 0.8%, model group mice lost weight 8.2 ± 0.9%, positive controls mice lost weight 5.0 ± 0.8%, obacunone group mice lost weight 2.9 ± 0.3%; Further illustrate the weight loss (P<0.001) of the ulcerative colitis mice that obacunone can significantly suppress DSS to cause; Further, in oral administration situation, the inhibitory action Be very effective of obacunone (50mg/kg) to weight loss is better than positive control drug SASP (350mg/kg) (P<0.05).
3.2 impacts on ulcerative colitis mice hemafecia incidence rate
Fig. 2 embodies the impact of obacunone on ulcerative colitis mice hemafecia incidence rate, as seen from Figure 2: mice occurs without hemafecia Normal group, the hemafecia incidence rate of model group mice is 96.7 ± 5.8%, the hemafecia incidence rate of positive controls mice is 60.0 ± 10.0%, and the hemafecia incidence rate of obacunone group mice is 43.3 ± 5.8%; Further illustrate the hemafecia rate (P<0.001) that obacunone significantly can reduce the ulcerative colitis mice that DSS causes; Further, in oral administration situation, the inhibitory action Be very effective of obacunone (50mg/kg) to hemafecia incidence rate is better than positive control drug SASP (350mg/kg) (P<0.05).
3.3 impacts on ulcerative colitis mouse Colon length
Fig. 3 embodies the impact of obacunone on ulcerative colitis mouse Colon length, as seen from Figure 3: Normal group mice shortens generation without colon, the colon LVFS of model group mice is 35.3 ± 0.6%, the colon LVFS of positive controls mice is 19.4 ± 0.3%, and the colon LVFS of obacunone group mice is 14.3 ± 0.2%; Further illustrate colon shortening symptom (P<0.01) that obacunone significantly can improve the ulcerative colitis mice that DSS causes; Further, in oral administration situation, obacunone (50mg/kg) is better than positive control drug SASP (350mg/kg) (P<0.01) the improvement result Be very effective that colon shortens symptom.。
3.4 impacts on ulcerative colitis mouse Colon histopathology
Fig. 4 and Fig. 5 embodies the injury repairing effect of obacunone to ulcerative colitis mouse Colon tissue, as seen from Figure 4: the colon of model group mice is the performance of exemplary inflammatory mucosa, visible mucosa, Submucosa be muscle layer massive inflammatory cells infiltrated even, organizational structure is disorderly, fracture, Submucosa is hemorrhage, edema, telangiectasis; Colon's lesions visible of positive controls mice and obacunone group mice alleviates, ulcer healing, and Submucosa is hemorrhage to be alleviated.As seen from Figure 5: the score of Normal group mice is 0, the score of model group mice is 5.7 ± 0.3%, and the score of positive controls mice is 3.4 ± 0.4%, and the score of obacunone group mice is 3.0 ± 0.2%, compared with model group, difference has significance (P<0.001).Illustrate that obacunone significantly can alleviate colonic mucosa inflammation cellular infiltration and Histopathological lesions situation (P<0.001).Further, in oral administration situation, obacunone (50mg/kg) is significantly better than positive control drug SASP (350mg/kg) (P<0.05) the repairing effect of colon pathology damage.
To sum up result of study shows: obacunone obviously can improve the weight loss of ulcerative colitis mice, hemafecia incidence rate, colon LVFS and Histopathological lesions symptom.And, in oral administration situation, the improvement result of obacunone (50mg/kg) to the weight loss of ulcerative colitis mice, hemafecia incidence rate, colon LVFS and Histopathological lesions is significantly better than positive control drug SASP (350mg/kg) (P<0.05).
Many aspects involved in the present invention have been done and have as above been set forth.It is to be understood, however, that put before not departing from spirit of the present invention, those skilled in the art can carry out equivalent change and modification to it, and described change and modification fall into the coverage of the application's claims equally.
Claims (2)
1. obacunone is preparing the application in the medicine or food preventing and treating ulcerative colitis.
2. apply as claimed in claim 1, it is characterized in that, described obacunone is for the preparation of medicine or the food of preventing and treating ulcerative colitis as unique active component.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769880A (en) * | 2016-03-09 | 2016-07-20 | 广东省中医院 | Application of obakunone to preparation of medicine for preventing and treating lung injury and pulmonary fibrosis |
| CN115252630A (en) * | 2022-09-02 | 2022-11-01 | 深圳技术大学 | Application of obacunone in preparation of medicine for preventing, improving or treating non-alcoholic fatty liver disease |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102344483A (en) * | 2010-07-29 | 2012-02-08 | 杨槐 | Preparation method for limonin analogues |
| CN103705525B (en) * | 2014-01-06 | 2015-09-23 | 江苏省中医院 | A kind of medicine containing limonin treatment ulcerative colitis and its preparation method and application |
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Non-Patent Citations (2)
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| JINHEE KIM等: "Obacunone exhibits anti-proliferative and anti-aromatase activity in vitro by inhibiting the p38 MAPK signaling pathway in MCF-7 human breast adenocarcinoma cells", 《BIOCHIMIE》 * |
| 稽汝运等: "《药学大辞典》", 30 September 2006 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769880A (en) * | 2016-03-09 | 2016-07-20 | 广东省中医院 | Application of obakunone to preparation of medicine for preventing and treating lung injury and pulmonary fibrosis |
| WO2017152796A1 (en) * | 2016-03-09 | 2017-09-14 | 广东省中医院 | Application of obacunone in preparation of drug for preventing and treating lung damage and pulmonary fibrosis |
| CN105769880B (en) * | 2016-03-09 | 2018-05-15 | 广东省中医院 | Application of the obakunone in the medicine of prevention injury of lungs and pulmonary fibrosis is prepared |
| US10632100B2 (en) | 2016-03-09 | 2020-04-28 | Guangdong Provincial Hospital Of Traditional Chinese Medicine | Application of obacunone in preparation of drug for preventing and treating lung damage and pulmonary fibrosis |
| CN115252630A (en) * | 2022-09-02 | 2022-11-01 | 深圳技术大学 | Application of obacunone in preparation of medicine for preventing, improving or treating non-alcoholic fatty liver disease |
| CN115252630B (en) * | 2022-09-02 | 2024-02-09 | 深圳技术大学 | Application of phellodendron ketone in preparing medicine for preventing, improving or treating non-alcoholic fatty liver disease |
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