CN103585150A - Use of Nitrosporeusines A in drugs for treating rhinitis - Google Patents
Use of Nitrosporeusines A in drugs for treating rhinitis Download PDFInfo
- Publication number
- CN103585150A CN103585150A CN201310636243.XA CN201310636243A CN103585150A CN 103585150 A CN103585150 A CN 103585150A CN 201310636243 A CN201310636243 A CN 201310636243A CN 103585150 A CN103585150 A CN 103585150A
- Authority
- CN
- China
- Prior art keywords
- nitrosporeusines
- rhinitis
- drugs
- present
- rat
- 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.)
- Granted
Links
- 229930191006 nitrosporeusine Natural products 0.000 title claims abstract description 25
- 206010039083 rhinitis Diseases 0.000 title claims abstract description 23
- 239000003814 drug Substances 0.000 title claims abstract description 14
- 229940079593 drug Drugs 0.000 title abstract description 5
- 150000001875 compounds Chemical class 0.000 claims description 13
- 238000002360 preparation method Methods 0.000 abstract description 9
- 230000000694 effects Effects 0.000 abstract description 5
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 abstract description 4
- 206010061218 Inflammation Diseases 0.000 abstract description 2
- 229960001193 diclofenac sodium Drugs 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 abstract 1
- 229960000351 terfenadine Drugs 0.000 abstract 1
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 12
- 108010058846 Ovalbumin Proteins 0.000 description 8
- 229940092253 ovalbumin Drugs 0.000 description 8
- 229960001340 histamine Drugs 0.000 description 6
- 210000001331 nose Anatomy 0.000 description 6
- 206010039085 Rhinitis allergic Diseases 0.000 description 3
- 241001137869 Streptomyces nitrosporeus Species 0.000 description 3
- 229930013930 alkaloid Natural products 0.000 description 3
- 201000010105 allergic rhinitis Diseases 0.000 description 3
- 210000003928 nasal cavity Anatomy 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 239000000427 antigen Substances 0.000 description 2
- 102000036639 antigens Human genes 0.000 description 2
- 108091007433 antigens Proteins 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 238000006748 scratching Methods 0.000 description 2
- 230000002393 scratching effect Effects 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- ZCVMWBYGMWKGHF-UHFFFAOYSA-N Ketotifene Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CC(=O)C2=C1C=CS2 ZCVMWBYGMWKGHF-UHFFFAOYSA-N 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 229940124623 antihistamine drug Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 231100000749 chronicity Toxicity 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 229960004958 ketotifen Drugs 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- NZHGWWWHIYHZNX-CSKARUKUSA-N tranilast Chemical compound C1=C(OC)C(OC)=CC=C1\C=C\C(=O)NC1=CC=CC=C1C(O)=O NZHGWWWHIYHZNX-CSKARUKUSA-N 0.000 description 1
- 229960005342 tranilast Drugs 0.000 description 1
- 230000008728 vascular permeability Effects 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention provides a use of Nitrosporeusines A in preparation of drugs for treating immune-inflammation and especially for treating rhinitis. A contrast test utilizing terfenadine and diclofenac sodium as control groups proves that Nitrosporeusines A has clear effects. Nitrosporeusines A is first disclosed in the invention. Nitrosporeusines A has a novel skeleton type, strong activity of treating rhinitis and substantive distinguishing features, and obviously develops rhinitis prevention and treatment.
Description
Technical field
The present invention relates to the new purposes of compound N itrosporeusines A, relate in particular to the application of Nitrosporeusines A in preparation treatment rhinitis medicine.
Background technology
Rhinitis is common clinical and frequently-occurring disease, and the generation of rhinitis is main relevant with anaphylaxis, belongs to the category of immune inflammation.At present, treatment rhinitis mainly adopts the Claritins such as the antihistamine drug such as teldane or tranilast, ketotifen, and these medicines are poor or invalid to the chronicity of rhinitis and the curative effect of repeatedly showing effect.Therefore, definite ingredients, quality controllable and safely and efficiently micromolecular compound aspect development treatment of rhinitis medicine, there is potential value.
The compound N itrosporeusines A the present invention relates to is one and within 2013, delivers (Aigang Yang, et al., Nitrosporeusines A and B, Unprecedented Thioester-Bearing Alkaloids from the Arctic Streptomyces nitrosporeus.Organic Letters, 2013, 15 (20): 5366 – 5369.) noval chemical compound, this compound has brand-new framework types, find that it can resist H1N1(Aigang Yang, et al., Nitrosporeusines A and B, Unprecedented Thioester-Bearing Alkaloids from the Arctic Streptomyces nitrosporeus.Organic Letters, 2013, 15 (20): 5366 – 5369.), the purposes of the Nitrosporeusines A the present invention relates in preparation treatment rhinitis medicine belongs to open first.
Summary of the invention
The object of the invention is to, according to not finding that it has the present situation of the report of anti-rhinitis activity in existing Nitrosporeusines A research, provides the application of Nitrosporeusines A in preparing anti-rhinitis medicament thing.
Described compound N itrosporeusines A, structure is as shown in formula I:
Formula I
Nitrosporeusines A10,20mg/kg oral administration, raises inhibitedly to scratch nose, sneeze reaction and nasal cavity vascular permeability of rat due to antigen (ovalbumin) and histamine, therefore, can be used for the medicine of preparation treatment rhinitis.
The purposes of Nitrosporeusines A in preparation treatment rhinitis medicine belongs to open first, because framework types belongs to brand-new framework types, and its treatment rhinitis is active strong, possesses outstanding substantive distinguishing features, the control for rhinitis simultaneously obviously has significant progress.
The specific embodiment
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
The preparation method of compound N itrosporeusines A involved in the present invention is referring to document (Aigang Yang, et al., Nitrosporeusines A and B, Unprecedented Thioester-Bearing Alkaloids from the Arctic Streptomyces nitrosporeus.Organic Letters, 2013,15 (20): 5366 – 5369.), prepare according to the method described above compound N itrosporeusines A.
Embodiment 1: the preparation of compound N itrosporeusines A tablet involved in the present invention:
Get 5 and digest compound Nitrosporeusines A, add 195 grams, dextrin, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound N itrosporeusines A capsule involved in the present invention:
Get 5 and digest compound Nitrosporeusines A, add 195 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example 1, Nitrosporeusines A of the present invention cause the impact of rat allergic rhinitis on ovalbumin
Male SD rat, body weight 180～220g, lumbar injection ovalbumin 1mg and gel aluminum hydroxide 10mg, inject the next day of thereafter 1 time, totally 7 times.From the 14th day, begin, splash into 1mg/ml ovalbumin normal saline solution 10ul, totally 7 time at rat both sides nasal cavity every day.After last instils, observe at once rat sneeze in 30 minutes and wipe the number of times of nose, trial drug is in ovalbumin last first 1 hour oral the giving of instiling.
Table 1 Nitrosporeusines A of the present invention causes the impact (x ± SD) of rat allergic rhinitis on ovalbumin
With matched group comparison, * * P<0.01*P<0.05
From table 1, Nitrosporeusines A(10,20mg/kg) obviously suppress sneeze and the nose reaction of scratching of allergic rhinitis rat due to ovalbumin.Teldane 10mg/kg also presents significant inhibitory action.
The impact of the rat rhinitis that experimental example 2, Nitrosporeusines A of the present invention cause histamine
Male SD rat, body weight 180～220g, orally gives after trial drug 1 hour, and both sides nasal cavity splashes into 1M histamine normal saline solution 10ul, observes rat sneeze in 30 minutes and wipes the number of times of nose.
Table 2 Nitrosporeusines A of the present invention causes the impact (x ± SD) of rat rhinitis on histamine
With matched group comparison, * * P<0.01*P<0.05
From table 2, Nitrosporeusines A(10,20mg/kg of the present invention) obviously reduce the sneeze number of times of rhinitis rat due to histamine, to scratching, nose reaction is inhibition trend.Teldane 10mg/kg is significant inhibitory action.
Conclusion: Nitrosporeusines A oral administration, inhibited to scratch nose, sneeze reaction of rat due to antigen (ovalbumin) and histamine, therefore, can be used for the medicine of preparation treatment rhinitis.
Claims (1)
- The application of 1.Nitrosporeusines A in treatment rhinitis medicine, described compound N itrosporeusinesA structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310636243.XA CN103585150B (en) | 2013-12-02 | 2013-12-02 | Use of Nitrosporeusines A in drugs for treating rhinitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310636243.XA CN103585150B (en) | 2013-12-02 | 2013-12-02 | Use of Nitrosporeusines A in drugs for treating rhinitis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103585150A true CN103585150A (en) | 2014-02-19 |
| CN103585150B CN103585150B (en) | 2015-04-29 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310636243.XA Expired - Fee Related CN103585150B (en) | 2013-12-02 | 2013-12-02 | Use of Nitrosporeusines A in drugs for treating rhinitis |
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| Country | Link |
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| CN (1) | CN103585150B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016051425A1 (en) | 2014-10-01 | 2016-04-07 | Council Of Scientific & Industrial Research | Benzenecarbothioccyclopenta[c] pyrrole-1,3-dione compounds and process for synthesis thereof |
-
2013
- 2013-12-02 CN CN201310636243.XA patent/CN103585150B/en not_active Expired - Fee Related
Non-Patent Citations (2)
| Title |
|---|
| AIGANG YANG,ET AL.: "Nitrosporeusines A and B, Unprecedented Thioester-Bearing Alkaloids from the Arctic Streptomyces nitrosporeus", 《ORGANIC LETTERS》 * |
| 郭明荣等: "山莨菪碱临床应用进展", 《基层医学论坛》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016051425A1 (en) | 2014-10-01 | 2016-04-07 | Council Of Scientific & Industrial Research | Benzenecarbothioccyclopenta[c] pyrrole-1,3-dione compounds and process for synthesis thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103585150B (en) | 2015-04-29 |
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| C53 | Correction of patent of invention or patent application | ||
| CB03 | Change of inventor or designer information |
Inventor after: Sun Yuping Inventor after: Chen Licai Inventor after: Song Xiaoling Inventor after: Feng Weiwei Inventor after: Yu Yajun Inventor after: Feng Yulin Inventor after: Peng Ning Inventor after: Chen Bin Inventor before: Chen Bin |
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| COR | Change of bibliographic data |
Free format text: CORRECT: INVENTOR; FROM: CHEN BIN TO: SUN YUPING CHEN LICAI SONG XIAOLING FENG WEIWEI YU YAJUN FENG YULIN PENG NING CHEN BIN |
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Effective date of registration: 20151225 Address after: 223411 Lianshui province Jiangsu County High Town Industrial District Patentee after: JIANGSU KANGQIANG FOOD LIMITED COMPANY Address before: 315700 Xiangshan, Zhejiang, Dandong street, Xiangshan Port Road, No. 79, No. Patentee before: Chen Bin |
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| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150429 Termination date: 20151202 |
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