CN106361755A - Zoarenone containing drug for treating ulcerative colitis - Google Patents
Zoarenone containing drug for treating ulcerative colitis Download PDFInfo
- Publication number
- CN106361755A CN106361755A CN201610924007.1A CN201610924007A CN106361755A CN 106361755 A CN106361755 A CN 106361755A CN 201610924007 A CN201610924007 A CN 201610924007A CN 106361755 A CN106361755 A CN 106361755A
- Authority
- CN
- China
- Prior art keywords
- zoarenone
- medicine
- treating
- delphinidin
- ulcerative colitis
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
Abstract
The invention discloses a Zoarenone containing drug for treating ulcerative colitis. The effective components of the Zoarenone containing drug include Zoarenone and chlorinated delphinidin. An experimental result show through united application of the Zoarenone and the chlorinated delphinidin that the Zoarenone and the chlorinated delphinidin have the very good effect on the ulcerative colitis based on the ratio of 12 to 1.
Description
Technical field
The present invention relates to a kind of zoarenone that comprises, for treating the medicine of ulcerative colitiss, belongs to medical science neck
Domain.
Background technology
Ulcerative colitiss are a kind of cause of disease colon still not fully aware of and rectum chronic nonspecific inflammation disease,
Pathological changes are confined to rectum and sigmoid colon, also can invade and other part or all of colons;Pathological changes severe patient, wherein minority may occur in which
" reflux ileitises " within 10cm.The course of disease is very long, normal recurrent exerbation.Primary disease is found in any age, but 20~30 years old
Common.Clinical symptoms are based on mucopurulent bloody stool, stomachache, diarrhoea or tenesmus;Acute critical illness example, has General Symptomies, and
It is often accompanied by parenterally disease and hepatic injury, arthritis, skin lesion, cardiomyopathy, oral ulcer, iridocyclitises and interior point
Secrete disease.
Compound zoarenone delivered (francisco cen-pacheco, et al, zoaramine a in 2014
Zoanthamine-like alkaloid with a new skeleton.organic letters, 2014,16,2880-
2883.), this compound has brand-new framework types, yet there are no with regard to zoarenone and chlorination delphinidin in treatment
The report of ulcerative colitiss.
Content of the invention
The problem existing for above-mentioned prior art, the present invention provide one kind comprise zoarenone be used for treating exedens
The medicine of colitis.
To achieve these goals, the technical solution used in the present invention is: one kind comprises zoarenone and is used for treating ulcer
The medicine of property colitis, effective ingredient includes zoarenone, and structural formula is as follows:
Effective ingredient includes also including chlorination delphinidin.
Calculate according to weight, zoarenone and chlorination delphinidin ratio are 1:1-20:1.
The preferred solid orally ingestible of this pharmaceutical composition;
Further, described oral formulations are tablet, capsule, granule, dry suspension or drop pill.
It should be noted that available adjuvant on pharmaceuticss of the present invention, refer to be included in addition to the active ingredient (s agent
Inert matter in type, includes but are not limited to filler (diluent), lubricant (fluidizer or antitack agent), dispersion
Agent, wetting agent, binding agent, solubilizing agent, antioxidant, antibacterial, emulsifying agent, disintegrating agent etc..Binding agent comprises syrup, Arab
Glue, gelatin, Sorbitol, tragacanth, cellulose and its derivates are (as Microcrystalline Cellulose, sodium carboxymethyl cellulose, ethyl cellulose
Or hydroxypropyl methylcellulose etc.), gelatine size, syrup, starch slurry or Polyvinylpyrrolidone etc.;Filler comprise Lactose, Icing Sugar,
Dextrin, starch and its derivant, cellulose and its derivates, inorganic calcium salt are (as calcium sulfate, calcium phosphate, calcium hydrogen phosphate, sedimentation carbon
Sour calcium etc.), Sorbitol or glycine etc.;Lubricant comprises micropowder silica gel, magnesium stearate, Pulvis Talci, aluminium hydroxide, boric acid, hydrogen
Change vegetable oil, Polyethylene Glycol etc.;Disintegrating agent comprises starch and its derivant (as carboxymethyl starch sodium, Explotab, pre- glue
Change starch, modified starch, hydroxypropyl starch, corn starch etc.), Polyvinylpyrrolidone or Microcrystalline Cellulose etc.;Wetting agent bag
Containing sodium lauryl sulphate, water or alcohol etc.;Antioxidant packages contain sodium sulfite, sodium sulfite, sodium pyrosulfite, dibutyl benzoic acid
Deng;Antibacterial comprises 0.5% phenol, 0.3% cresol, 0.5% chlorobutanol etc.;Emulsifying agent comprises Tween-80, does not have acid
Pyrusussuriensiss are smooth, lecithin, fabaceous lecithin etc.;Solubilizing agent comprises tween 80, bile, glycerol etc..
A kind of zoarenone that comprises that the present invention provides is used for treating the medicine of ulcerative colitiss, by zoarenone
With chlorination delphinidin use in conjunction, test result indicate that, zoarenone and chlorination delphinidin are in 12:1 for treating exedens knot
Enteritis has good cooperative effect.
Specific embodiment
Described above is only the general introduction of technical solution of the present invention, in order to better understand the technological means of the present invention,
And can be practiced according to the content of description and ordinary skill in the art means, below the animal experiment example of the present invention is done
Described in further detail.
Chinese: chlorination delphinidin, No. cas: 528-53-0, the company such as Chengdu Si Tiande bio tech ltd is equal
On sale.
The preparation method of compound zoarenone involved in the present invention is referring to document: (francisco cen-pacheco,
et al.,zoaramine a zoanthamine-like alkaloid with a new skeleton.organic
Letters, 2014,16,2880-2883.).
Modeling: cleaning grade male rat 210, body weight 80-100g, 22~25 DEG C of experimental animal feeding temperature, relatively wet
Degree 45%~75%..Configuration 4%dss solutions i p injection each group rat, continuous 5d causes rat ulcer membranous conjunctivitis.
It is divided into 21 groups, every group ten, daily gavage is administered respectively, blank group is saline solution.
Experimental technique:
Occludin protein expression analysis are cut: the conventional dewaxing of piece, Microwave method after aquation, 0.3%trition rupture of membranes. Deca
Occludin mono- resists (1:50), overnight incubation in 4 DEG C of wet box, adds goat anti-mouse fluorescent antibody (1:50), constant temperature and humidity is incubated
Educate 2h and add incubation 10min under hochest (1:50) dye core room temperature, mounting.Every section randomly chooses 5 visuals field and adopts image
Pro pius 6.0 image software.Fluorescence intensity integrated absorbance ia in each section is represented.
Colonic mucosa barrier is assessed: the quantitative analyses of mucus ab-pas dyeing, by embedded colon's section, difference
Carry out conventional ab-pas dyeing.Under high power lenses, 5 visuals field of colonic epithelia tissue random choose at section anus end are clapped
According to.Using computer image analysis software image pro pius 6.0 image software, carried out with the absorbance a of ab-pas dyeing
Quantitative analyses.
A is zoarenone, and b is chlorination delphinidin,
The colitis mice colonic epithelium mucilage secretion of each group rat dss induction, occludin is worth comparing (g/l, x ± s),
p<0.05
Test result indicate that: each group rat epithelial mucilage secretion, the comparison of occludin value, give zoarenone and chlorine after experiment
Change mucus expression/a in two groups of rats of 12:1 for the delphinidin, occludin/a is all remarkably higher than blank group and its other groups.Can
See that medicine zoarenone and chlorination delphinidin have good cooperative effect in 12:1 for treatment colitis.
Claims (4)
1. a kind of containing zoarenone be used for treat the medicine of ulcerative colitiss it is characterised in that effective ingredient includes
Zoarenone, structural formula is as follows:
.
2. according to claim 1 a kind of be used for treating the medicine of ulcerative colitiss containing zoarenone, its feature exists
In effective ingredient also includes chlorination delphinidin.
3. according to claim 2 a kind of be used for treating the medicine of ulcerative colitiss containing zoarenone, its feature exists
According to weight calculating, zoarenone and chlorination delphinidin ratio are 1:1-20:1.
4. according to claim 3 a kind of be used for treating the medicine of ulcerative colitiss containing zoarenone, its feature exists
In each component weighing up by formula ratio is ground into 150-200 mesh powder, mix homogeneously;Then carried out with 1: 20-30 weight ratio
It is watered mediation.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CN201610924007.1A CN106361755A (en) | 2016-10-23 | 2016-10-23 | Zoarenone containing drug for treating ulcerative colitis |
Applications Claiming Priority (1)
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---|---|---|---|
CN201610924007.1A CN106361755A (en) | 2016-10-23 | 2016-10-23 | Zoarenone containing drug for treating ulcerative colitis |
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CN106361755A true CN106361755A (en) | 2017-02-01 |
Family
ID=57895884
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CN201610924007.1A Pending CN106361755A (en) | 2016-10-23 | 2016-10-23 | Zoarenone containing drug for treating ulcerative colitis |
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Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101495114A (en) * | 2006-07-28 | 2009-07-29 | 因德纳有限公司 | Treatment and prevention mucositis by anthocyanidin derivatives |
CN104870001A (en) * | 2012-11-15 | 2015-08-26 | 赛博尔泰克股份公司 | Delphinidin complex as an antiphlogistic or immunosuppressive active ingredient |
CN105596351A (en) * | 2015-11-10 | 2016-05-25 | 淄博齐鼎立专利信息咨询有限公司 | Applications of Zoarenone in preparing drugs used for treating hemorrhagic fever with renal syndrome |
-
2016
- 2016-10-23 CN CN201610924007.1A patent/CN106361755A/en active Pending
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101495114A (en) * | 2006-07-28 | 2009-07-29 | 因德纳有限公司 | Treatment and prevention mucositis by anthocyanidin derivatives |
CN104870001A (en) * | 2012-11-15 | 2015-08-26 | 赛博尔泰克股份公司 | Delphinidin complex as an antiphlogistic or immunosuppressive active ingredient |
CN105596351A (en) * | 2015-11-10 | 2016-05-25 | 淄博齐鼎立专利信息咨询有限公司 | Applications of Zoarenone in preparing drugs used for treating hemorrhagic fever with renal syndrome |
Non-Patent Citations (2)
Title |
---|
ARPIT SAXENA ET AL: "Dietary Agents and Phytochemicals in the Prevention and Treatment of Experimental Ulcerative Colitis", 《JOURNAL OF TRADITIONAL AND COMPLEMENTARY MEDICINE》 * |
FRANCISCO CEN-PACHECO ET AL: "Zoaramine, a Zoanthamine-like Alkaloid with a New Skeleton", 《ORGANIC LETTERS》 * |
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SE01 | Entry into force of request for substantive examination | ||
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WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170201 |
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