CN103585152A - Application of Caesanines D in medicament for treating rhinitis - Google Patents

Application of Caesanines D in medicament for treating rhinitis Download PDF

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Publication number
CN103585152A
CN103585152A CN201310607649.5A CN201310607649A CN103585152A CN 103585152 A CN103585152 A CN 103585152A CN 201310607649 A CN201310607649 A CN 201310607649A CN 103585152 A CN103585152 A CN 103585152A
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caesanines
rhinitis
medicament
present
rat
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李强
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Abstract

The invention discloses a Caesanines D for treating immune-inflammation, for preparing a medicament for curing immune-inflammation, and particularly for preparing a medicament for curing rhinitis. Terfenadine and diclofenac sodium are taken as control, Caesanines D is explicit in curative effect and is issued for the first time, because of the novel framework type and the high rhinitis treatment activity, Caesanines D has outstanding substantive characteristics, and meanwhile the prevention and the treatment on rhinitis are greatly improved.

Description

The application of Caesanines D in treatment rhinitis medicine
Technical field
The present invention relates to the new purposes of Compound C aesanines D, relate in particular to the application of Caesanines D 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 C aesanines D the present invention relates to is one and within 2013, delivers (Jingyu Zhang, et al., Caesanines AD, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan.Organic Letters, 2013, 15 (18): 4726 – 4729.) noval chemical compound, this compound has brand-new framework types, find antibiotic (the Jingyu Zhang of its energy, et al., Caesanines AD, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan.Organic Letters, 2013, 15 (18): 4726 – 4729.), the purposes of the Caesanines D 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 Caesanines D research, provides the application of Caesanines D in preparing anti-rhinitis medicament thing.
Described Compound C aesanines D, structure is as shown in formula I:
Figure BDA0000422417970000011
Formula I
Caesanines D10,20mg/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 Caesanines D 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 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 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 C aesanines D involved in the present invention is referring to document (Jingyu Zhang, et al., Caesanines AD, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan.Organic Letters, 2013,15 (18): 4726 – 4729.), prepare according to the method described above Compound C aesanines D.
Embodiment 1: the preparation of Compound C aesanines D tablet involved in the present invention:
Get 5 and digest compound Caesanines D, add 195 grams, dextrin, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of Compound C aesanines D capsule involved in the present invention:
Get 5 and digest compound Caesanines D, add 180 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example 1, Caesanines D 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 Caesanines D of the present invention causes the impact (x ± SD) of rat allergic rhinitis on ovalbumin
Figure BDA0000422417970000021
Figure BDA0000422417970000031
With matched group comparison, * * P<0.01*P<0.05
From table 1, Caesanines D(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, Caesanines D 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 Caesanines D of the present invention causes the impact (x ± SD) of rat rhinitis on histamine
Figure BDA0000422417970000032
With matched group comparison, * * P<0.01*P<0.05
From table 2, Caesanines D(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: Caesanines D 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)

  1. The application of 1.Caesanines D in treatment rhinitis medicine, described Compound C aesanines D structure is as shown in formula I:
    Figure FDA0000422417960000011
    Formula I.
CN201310607649.5A 2013-11-26 2013-11-26 Application of Caesanines D in medicament for treating rhinitis Pending CN103585152A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201310607649.5A CN103585152A (en) 2013-11-26 2013-11-26 Application of Caesanines D in medicament for treating rhinitis

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Application Number Priority Date Filing Date Title
CN201310607649.5A CN103585152A (en) 2013-11-26 2013-11-26 Application of Caesanines D in medicament for treating rhinitis

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CN103585152A true CN103585152A (en) 2014-02-19

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CN201310607649.5A Pending CN103585152A (en) 2013-11-26 2013-11-26 Application of Caesanines D in medicament for treating rhinitis

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JINGYU ZHANG等: "Caesanines A-D, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan", 《ORGANIC LETTERS》 *
董震等: "金黄色葡萄球菌超抗原和慢性鼻黏膜炎症", 《中国耳鼻咽喉头颈外科杂志》 *

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Application publication date: 20140219