CN102988393B - Application of Houttuynoid B for preparing medicine for treating rhinitis - Google Patents
Application of Houttuynoid B for preparing medicine for treating rhinitis Download PDFInfo
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- CN102988393B CN102988393B CN201210469166.9A CN201210469166A CN102988393B CN 102988393 B CN102988393 B CN 102988393B CN 201210469166 A CN201210469166 A CN 201210469166A CN 102988393 B CN102988393 B CN 102988393B
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- houttuynoid
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Abstract
The invention relates to Houttuynoid B for treating immunity inflammation, which is used for preparing a medicine for treating immunity inflammation, in particular for preparing a medicine for treating rhinitis. Houttuynoid B has definite curative effect by using terfenadine and diclofenac sodium as contrasts. The application of Houttuynoid B for preparing the medicine for treating rhinitis is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the rhinitis curative activity of Houttuynoid B is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Houttuynoid B has outstanding substantive characteristics; and simultaneously, Houttuynoid B has obvious progress for preventing and treating rhinitis.
Description
Technical field
The present invention relates to the application of Houttuynoid B 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 H outtuynoid B the present invention relates to is one and within 2012, delivers (Cai, J. Y. et al., 2012. Houttuynoid B, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to DEF(Cai, J. Y. et al., 2012. Houttuynoid B, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), purposes for the Houttuynoid B the present invention relates in preparation treatment rhinitis medicine belongs to open first, because framework types belongs to brand-new framework types, and its treatment rhinitis is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for rhinitis simultaneously obviously has significant progress.
Summary of the invention
The technical problem to be solved in the present invention is the purposes of research Houttuynoid B aspect preparation treatment rhinitis.
Described compound H outtuynoid B structure is as shown in formula I:
Houttuynoid B 10,20 mg/kg oral administrations, raise 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 Houttuynoid B in preparation treatment rhinitis medicine belongs to open first, because framework types belongs to brand-new framework types, and its treatment rhinitis is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for rhinitis simultaneously obviously has significant progress.
The specific embodiment
The preparation method of compound H outtuynoid B involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Houttuynoid B, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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.
Embodiment 1: the preparation of compound H outtuynoid B tablet involved in the present invention:
Get 20 and digest compound Houttuynoid B, add 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound H outtuynoid B capsule involved in the present invention:
Get 20 and digest compound Houttuynoid B, add the conventional adjuvant of preparing capsule as 180 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example 1, Houttuynoid B 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.
From table 1, Houttuynoid B(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.
Table 1 Houttuynoid B of the present invention causes the impact (x ± SD) of rat allergic rhinitis on ovalbumin
* p<0.05, * * p<0.01, with matched group comparison
The impact of the rat rhinitis that experimental example 2, Houttuynoid B 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.
From table 2, Houttuynoid B(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.
Table 2 Houttuynoid B of the present invention causes the impact (x ± SD) of rat rhinitis on histamine
* p<0.05, * * p<0.01, with matched group comparison
Experimental example 3, Houttuynoid B of the present invention cause on ovalbumin, histamine the impact that rat nasal cavity vascular permeability raises
Male SD rat, body weight 180 ~ 220g, with active sensitization rat and normal rat, observing the nasal cavity vascular permeability that ovalbumin and histamine cause respectively raises, the sensitization method 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, (0.25ml/min0 is connected this intubate after fixing with constant flow pump, with 37 ℃ of normal saline flushing nasal cavities 10 minutes, thereafter the blue normal saline solution 5ml/kg of rat tail vein injection 1%Evans, collects perfusate 10 minutes after 3 minutes.At sensitized rats and normal rat, in perfusate, contain respectively ovalbumin 1mg/ml and histamine 40ug/ml, the perfusate of collecting from nasal cavity centrifugal 10 minutes through 1200 * g, the blue concentration of Evans in 620nm place colorimetric determination supernatant, first 1 hour oral administration of tested medicine and antigen or histamine perfusion.
From table 3, Houttuynoid B(10 of the present invention, 20 mg/kg) obviously suppress the nasal cavity vascular permeability of allergic rhinitis rat due to ovalbumin, 5 mg/kg are inhibition trend, and teldane 10mg/kg presents significant inhibitory action.
Table 3 Houttuynoid B of the present invention causes on ovalbumin the impact (x ± SD) that rat nasal cavity vascular permeability raises
* p<0.01, with matched group comparison
From table 4, Houttuynoid B 20 mg/kg of the present invention obviously reduce the nasal cavity vascular permeability of rat due to histamine, and 10 mg/kg are inhibition trend, and terfenadine 10mg/kg presents significant inhibitory action.
Table 4 Houttuynoid B of the present invention causes on histamine the impact (x ± SD) that rat nasal cavity blood flow permeability raises
* p<0.01, with matched group comparison
Conclusion: Houttuynoid B oral administration, to scratch nose, sneeze reaction and nasal cavity vascular permeability of rat due to antigen (ovalbumin) and histamine, raise inhibitedly, therefore, can be used for the medicine of preparation treatment rhinitis.
Claims (1)
- The application of 1.Houttuynoid B in preparation treatment of allergic rhinitis medicine, described compound H outtuynoid B structure as formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210469166.9A CN102988393B (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid B for preparing medicine for treating rhinitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210469166.9A CN102988393B (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid B for preparing medicine for treating rhinitis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102988393A CN102988393A (en) | 2013-03-27 |
| CN102988393B true CN102988393B (en) | 2014-04-16 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201210469166.9A Expired - Fee Related CN102988393B (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid B for preparing medicine for treating rhinitis |
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| Country | Link |
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| CN (1) | CN102988393B (en) |
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2012
- 2012-11-19 CN CN201210469166.9A patent/CN102988393B/en not_active Expired - Fee Related
Non-Patent Citations (5)
| Title |
|---|
| Houttuynoids A-E,anti-herpes simplex virus active flavonoids with novel skeletons from houttuynia cordata;Shao-dan Chen et al.;《Organic Letters》;20130313;第14卷(第7期);第1772-1775页 * |
| Shao-danChenetal..HouttuynoidsA-E anti-herpes simplex virus active flavonoids with novel skeletons from houttuynia cordata.《Organic Letters》.2013 |
| 张娟.鱼腥草滴鼻液治疗鼻炎.《云南中医中药杂志》.1994,(第04期), |
| 方晓阳等.慢性鼻炎.《袖珍中草药图本》.1997,(第1版), * |
| 鱼腥草滴鼻液治疗鼻炎;张娟;《云南中医中药杂志》;19940830(第04期);第9页 * |
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