CN103372006B - The application of Chukrasone B in preparation treatment rhinitis medicine - Google Patents
The application of Chukrasone B in preparation treatment rhinitis medicine Download PDFInfo
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- CN103372006B CN103372006B CN201310280835.2A CN201310280835A CN103372006B CN 103372006 B CN103372006 B CN 103372006B CN 201310280835 A CN201310280835 A CN 201310280835A CN 103372006 B CN103372006 B CN 103372006B
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- rhinitis
- chukrasone
- rat
- treatment rhinitis
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- 206010039083 rhinitis Diseases 0.000 title claims abstract description 25
- 239000003814 drug Substances 0.000 title claims abstract description 16
- 238000002360 preparation method Methods 0.000 title claims abstract description 12
- 229930187319 chukrasone Natural products 0.000 title abstract description 5
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 claims description 6
- 150000001875 compounds Chemical class 0.000 abstract description 8
- 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 6
- 229940079593 drug Drugs 0.000 abstract description 4
- 206010061218 Inflammation Diseases 0.000 abstract description 3
- 230000000694 effects Effects 0.000 abstract description 3
- 230000004054 inflammatory process Effects 0.000 abstract description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 2
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 abstract 1
- 229960001259 diclofenac Drugs 0.000 abstract 1
- 241000700159 Rattus Species 0.000 description 26
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 24
- 108010058846 Ovalbumin Proteins 0.000 description 13
- 229940092253 ovalbumin Drugs 0.000 description 13
- 229960001340 histamine Drugs 0.000 description 12
- 210000003928 nasal cavity Anatomy 0.000 description 12
- 230000008728 vascular permeability Effects 0.000 description 7
- 210000001331 nose Anatomy 0.000 description 6
- 206010039085 Rhinitis allergic Diseases 0.000 description 5
- 201000010105 allergic rhinitis Diseases 0.000 description 5
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 230000002401 inhibitory effect Effects 0.000 description 4
- 239000000427 antigen Substances 0.000 description 3
- 102000036639 antigens Human genes 0.000 description 3
- 108091007433 antigens Proteins 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 230000001629 suppression Effects 0.000 description 3
- 206010070834 Sensitisation Diseases 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 238000006748 scratching Methods 0.000 description 2
- 230000002393 scratching effect Effects 0.000 description 2
- 230000008313 sensitization Effects 0.000 description 2
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 241001062009 Indigofera Species 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
- QGMRQYFBGABWDR-UHFFFAOYSA-M Pentobarbital sodium Chemical compound [Na+].CCCC(C)C1(CC)C(=O)NC(=O)[N-]C1=O QGMRQYFBGABWDR-UHFFFAOYSA-M 0.000 description 1
- 102000004257 Potassium Channel Human genes 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
- 230000037005 anaesthesia Effects 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
- 230000017531 blood circulation Effects 0.000 description 1
- 231100000749 chronicity Toxicity 0.000 description 1
- 229940088529 claritin Drugs 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000011010 flushing procedure Methods 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 229960004958 ketotifen Drugs 0.000 description 1
- JCCNYMKQOSZNPW-UHFFFAOYSA-N loratadine Chemical compound C1CN(C(=O)OCC)CCC1=C1C2=NC=CC=C2CCC2=CC(Cl)=CC=C21 JCCNYMKQOSZNPW-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 229960002275 pentobarbital sodium Drugs 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 108020001213 potassium channel Proteins 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 229960000351 terfenadine Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 210000003437 trachea Anatomy 0.000 description 1
- 238000002627 tracheal intubation Methods 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
- 210000003462 vein Anatomy 0.000 description 1
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
A kind of Chukrasone treating immune inflammation? B, for the preparation for the treatment of immune inflammation disease drug, is particularly useful for the medicine preparing treatment rhinitis, with teldane and diclofenac in contrast, Chukrasone? B clear curative effect.The Chukrasone that the present invention relates to? the purposes of B in preparation treatment rhinitis medicine belongs to first public, because framework types belongs to brand-new framework types, and its treatment rhinitis is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for rhinitis obviously has significant progress.
Description
Technical field
The present invention relates to the application of ChukrasoneB 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 adopt the antihistamine drug such as teldane or the Claritin such as tranilast, ketotifen, these medicines to the chronicity of rhinitis and recurrent exerbation curative effect poor or invalid.Therefore, definite ingredients, quality controllable and safely and efficiently micromolecular compound in development treatment of rhinitis medicine, there is potential value.
The Compound C hukrasoneB that the present invention relates to is one and delivers (Liu in 2012, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to potassium-channel inhibit activities (Liu, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.), the purposes of the ChukrasoneB that the present invention relates in preparation treatment rhinitis medicine is belonged to first public, because framework types belongs to brand-new framework types, and its treatment rhinitis is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for rhinitis obviously has significant progress.
Summary of the invention
The technical problem to be solved in the present invention is the purposes of research ChukrasoneB in preparation treatment rhinitis.
Described Compound C hukrasoneB structure is as shown in formula I:
ChukrasoneB10,20mg/kg oral administration, raises inhibited to scratch nose, sneeze reaction and nasal cavity vascular permeability of rat caused by antigen (ovalbumin) and histamine, therefore, can be used for the medicine preparing treatment rhinitis.
The purposes of ChukrasoneB in preparation treatment rhinitis medicine belongs to first public, because framework types belongs to brand-new framework types, and its treatment rhinitis is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for rhinitis obviously has significant progress.
Detailed description of the invention
The preparation method of Compound C hukrasoneB involved in the present invention is see document (Liu, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of Compound C hukrasoneB tablet involved in the present invention:
Get 20 g of compound ChukrasoneB, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasoneB capsule involved in the present invention:
Get 20 g of compound ChukrasoneB, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1, ChukrasoneB 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 1 time next day of thereafter, totally 7 times.Began from the 14th day, every day instills 1mg/ml ovalbumin normal saline solution 10ul at rat both sides nasal cavity, totally 7 times.Last is observed rat sneeze in 30 minutes at once and is wiped the number of times of nose after instiling, trial drug instils in ovalbumin last and orally to give for first 1 hour.
From table 1, ChukrasoneB (10,20mg/kg) obviously suppresses the sneeze of allergic rhinitis rat caused by ovalbumin and nose reaction of scratching.Teldane 10mg/kg also presents significant inhibitory action.
Table 1 ChukrasoneB of the present invention causes the impact (x ± SD) of rat allergic rhinitis to ovalbumin
* p<0.05, * * p<0.01, compares with matched group
Experimental example 2, ChukrasoneB of the present invention are on the impact of the rat rhinitis that histamine causes
Male SD rat, body weight 180 ~ 220g, orally to give after trial drug 1 hour, and both sides nasal cavity instillation 1M histamine normal saline solution 10ul, observes the number of times of rat sneeze and wiping nose in 30 minutes.
From table 2, ChukrasoneB of the present invention (10,20mg/kg) obviously reduces the sneeze number of times of rhinitis rat caused by histamine, to nose reaction of scratching in suppression trend.Teldane 10mg/kg is then in significant inhibitory action.
Table 2 ChukrasoneB of the present invention causes the impact (x ± SD) of rat rhinitis to histamine
* p<0.05, * * p<0.01, compares with matched group
The impact that experimental example 3, ChukrasoneB of the present invention cause rat nasal cavity vascular permeability to raise on ovalbumin, histamine
Male SD rat, body weight 180 ~ 220g, observe with active sensitization rat and normal rat the nasal cavity vascular permeability that ovalbumin and histamine cause respectively to raise, the method of sensitization of rat is tested with allergic rhinitis, after initial immunity the 14th day, rats by intraperitoneal injection pentobarbital sodium 40mg/kg, after anesthesia from trachea to nasal intubation, be connected this intubate with constant flow pump after fixing (0.25ml/min0, with 37 DEG C of normal saline flushing nasal cavities 10 minutes, thereafter the blue normal saline solution 5ml/kg of rat tail vein injection 1%Evans, perfusate is collected 10 minutes after 3 minutes.At sensitized rats and normal rat, respectively containing ovalbumin 1mg/ml and histamine 40ug/ml in perfusate, the perfusate collected from nasal cavity through 1200 × g centrifugal 10 minutes, the Evans indigo plant concentration in 620nm place colorimetric determination supernatant, test medicine and antigen or histamine perfusion first 1 hour oral administration.
From table 3, ChukrasoneB of the present invention (10,20mg/kg) obviously suppresses the nasal cavity vascular permeability of allergic rhinitis rat caused by ovalbumin, and 5mg/kg is suppression trend, and teldane 10mg/kg presents significant inhibitory action.
The impact (x ± SD) that table 3 ChukrasoneB of the present invention causes rat nasal cavity vascular permeability to raise on ovalbumin
* p<0.01, compares with matched group
From table 4, ChukrasoneB20mg/kg of the present invention obviously reduces the nasal cavity vascular permeability of rat caused by histamine, and 10mg/kg is suppression trend, and terfenadine 10mg/kg presents significant inhibitory action.
The impact (x ± SD) that table 4 ChukrasoneB of the present invention causes rat nasal cavity blood flow permeability to raise on histamine
* p<0.01, compares with matched group
Conclusion: ChukrasoneB oral administration, raises inhibited to scratch nose, sneeze reaction and nasal cavity vascular permeability of rat caused by antigen (ovalbumin) and histamine, therefore, can be used for the medicine preparing treatment rhinitis.
Claims (1)
1. the application of ChukrasoneB in preparation treatment rhinitis medicine, described Compound C hukrasoneB structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310280835.2A CN103372006B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone B in preparation treatment rhinitis medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310280835.2A CN103372006B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone B in preparation treatment rhinitis medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103372006A CN103372006A (en) | 2013-10-30 |
| CN103372006B true CN103372006B (en) | 2015-12-23 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310280835.2A Expired - Fee Related CN103372006B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone B in preparation treatment rhinitis medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103372006B (en) |
-
2013
- 2013-07-04 CN CN201310280835.2A patent/CN103372006B/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| Chukrasones A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis;Liu, H. B. et al.;《Organic Letters》;20121231;第14卷(第17期);第4438-4441页 * |
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| Publication number | Publication date |
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| CN103372006A (en) | 2013-10-30 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20151109 Address after: 266000 Licang, Qingdao, No. nine East water road, No. 320, No. Applicant after: Gu Xiangmao Address before: 210009 Gulou District, Jiangsu, Nanjing Gu Ping Kong, No. 4 Applicant before: Ding Shengyu |
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| CB03 | Change of inventor or designer information |
Inventor after: Xu Yanli Inventor after: Wang Tao Inventor before: Ding Shengyu |
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| COR | Change of bibliographic data | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Han Lin Inventor after: Wang Guimei Inventor before: Xu Yanli Inventor before: Wang Tao |
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| COR | Change of bibliographic data | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20170116 Address after: 261000 Kuiwei City, Weifang Province, No. College Street, building 3, building 2, unit 402, No. 7 Patentee after: Han Lin Address before: 266000 Licang, Qingdao, No. nine East water road, No. 320, No. Patentee before: Gu Xiangmao |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20151223 Termination date: 20180704 |