CN103751170B - The application of Trigoxyphin K in treatment rhinitis medicine - Google Patents

The application of Trigoxyphin K in treatment rhinitis medicine Download PDF

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Publication number
CN103751170B
CN103751170B CN201310597038.7A CN201310597038A CN103751170B CN 103751170 B CN103751170 B CN 103751170B CN 201310597038 A CN201310597038 A CN 201310597038A CN 103751170 B CN103751170 B CN 103751170B
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rhinitis
trigoxyphin
trigoxyphink
medicine
treatment rhinitis
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CN103751170A (en
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田丽华
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Yiheng Pharmaceutical Co., Ltd., Nanjing
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Zibo Qidingli Patent Information Consulting Co Ltd
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Abstract

A kind of Trigoxyphin that treats immune inflammation? K, for the preparation for the treatment of immune inflammation disease drug, is particularly useful for the medicine of preparation treatment rhinitis, use teldane and diclofenac sodium in contrast, Trigoxyphin? K curative effect is clear and definite. The Trigoxyphin the present invention relates to? the purposes of K 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, obviously has significant progress for the control of rhinitis simultaneously.

Description

The application of Trigoxyphin K in treatment rhinitis medicine
Technical field
The present invention relates to the new purposes of compound TrigoxyphinK, relate in particular to TrigoxyphinK in preparation treatment rhinitisApplication in medicine.
Background technology
Rhinitis is common clinical and frequently-occurring disease, and the generation of rhinitis is main relevant with allergic reaction, belongs to the category of immune inflammation.At present, treatment rhinitis mainly adopts the Claritins such as antihistamine drug or tranilast, Ketotifen such as teldane, these medicinesChronicity and repeatedly the show effect curative effect of thing to rhinitis is poor or invalid. Therefore, definite ingredients, quality controllable and safely and efficiently littleMolecular compound, aspect development treatment of rhinitis medicine, has potential value.
The compound TrigoxyphinK the present invention relates to is one and within 2013, delivers (BiaoYang, etal., FivenewdegradedditerpenoidsfromTrigonostemonxyphophylloides.Bioorganic&MedicinalChemistryLetters, 23 (2013) 5748 – 5751.) noval chemical compound, this compound has entirelyNew framework types, does not find its active function (BiaoYang, etal., Fivenewdegraded at presentditerpenoidsfromTrigonostemonxyphophylloides.Bioorganic&MedicinalChemistryLetters, 23 (2013) 5748 – 5751.), the TrigoxyphinK the present invention relates to is in preparation treatment rhinitis medicinePurposes belong to first open.
Summary of the invention
The object of the invention is to according to not finding showing of its report with anti-rhinitis activity in existing TrigoxyphinK researchShape, provides TrigoxyphinK in the application of preparing in anti-rhinitis medicament thing.
Described compound TrigoxyphinK, structure is suc as formula shown in (I):
Formula (I)
TrigoxyphinK10,20mg/kg oral administration, to the nose of scratching of rat due to antigen (ovalbumin) and histaminePortion, sneeze reaction and nasal cavity vasopermeability raise inhibited, therefore, can be used for the medicine of preparation treatment rhinitis.
The purposes of TrigoxyphinK in preparation treatment rhinitis medicine belongs to open first, because framework types belongs to brand-newFramework types, and its treatment rhinitis is active strong, possesses outstanding substantive distinguishing features, obviously has for the control of rhinitis simultaneouslySignificant progressive.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to specific embodimentAny restriction, but be limited by claim.
Detailed description of the invention
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to specific embodimentAny restriction, but be limited by claim.
The preparation method of compound TrigoxyphinK involved in the present invention is referring to document (BiaoYang, etal., FivenewdegradedditerpenoidsfromTrigonostemonxyphophylloides.Bioorganic&MedicinalChemistryLetters, 23 (2013) 5748 – 5751.), prepare according to the method described above compoundTrigoxyphinK。
Embodiment 1: the preparation of compound TrigoxyphinK tablet involved in the present invention:
Get 5 and digest compound TrigoxyphinK, add 195 grams, dextrin, mix, conventional compressing tablet is made 1000.
Embodiment 2: the preparation of compound TrigoxyphinK capsule involved in the present invention:
Get 5 and digest compound TrigoxyphinK, add 195 grams of starch, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example 1, TrigoxyphinK of the present invention cause the impact of rat allergic rhinitis on ovalbumin
Male SD rat, body weight 180-220g, Nanjing Medical University's Experimental Animal Center, lumbar injection ovalbumin 1mg andGel aluminum hydroxide 10mg, injects the next day of thereafter 1 time, totally 7 times. Began from the 14th day, every day is in the nasal cavity of rat both sidesSplash into 1mg/ml ovalbumin normal saline solution 10ul, totally 7 times. Last is observed at once rat in 30 minutes after instiling and is beatenSneeze and wipe the number of times of nose, trial drug is in ovalbumin last first 1 hour oral the giving of instiling.
Table 1 TrigoxyphinK of the present invention causes the impact (x ± SD) of rat allergic rhinitis on ovalbumin
With control group comparison, * * P < 0.01*P < 0.05
From table 1, TrigoxyphinK(10,20mg/kg) obviously suppress allergic rhinitis rat due to ovalbuminSneeze and the nose reaction of scratching. Teldane 10mg/kg also presents significant inhibitory action.
The impact of the rat rhinitis that experimental example 2, TrigoxyphinK of the present invention cause histamine
Male SD rat, body weight 180~220g, Nanjing Medical University's Experimental Animal Center, oral give after trial drug 1 littleTime, in the nasal cavity of both sides, splash into 1M histamine normal saline solution 10ul, observe the number of times that rat in 30 minutes is sneezed and wipes nose.
Table 2 TrigoxyphinK of the present invention causes the impact (x ± SD) of rat rhinitis on histamine
With control group comparison, * * P < 0.01*P < 0.05
From table 2, TrigoxyphinK(10,20mg/kg of the present invention) obviously reduce the sneeze of rhinitis rat due to histamineNumber of times, to scratching, nose reaction is inhibition trend. Teldane 10mg/kg is significant inhibitory action.
Conclusion: TrigoxyphinK oral administration, to rat due to antigen (ovalbumin) and histamine scratch nose, play spraySneeze reaction inhibited, therefore, can be used for the medicine of preparation treatment rhinitis.

Claims (1)

  1. The application of 1.TrigoxyphinK in preparation treatment rhinitis medicine, described compound TrigoxyphinK structureShown in (I):
    Formula (I).
CN201310597038.7A 2013-11-22 2013-11-22 The application of Trigoxyphin K in treatment rhinitis medicine Active CN103751170B (en)

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CN103751170B true CN103751170B (en) 2016-05-18

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103271913A (en) * 2013-06-03 2013-09-04 南京正亮医药科技有限公司 Application of Myriberine A in preparing thrombocyte-increasing medicines

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103271913A (en) * 2013-06-03 2013-09-04 南京正亮医药科技有限公司 Application of Myriberine A in preparing thrombocyte-increasing medicines

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Five new degraded diterpenoids from Trigonostemon xyphophylloides;Biao Yang等;《Bioorganic & Medicinal Chemistry Letters》;20130131;5748-5751 *
Three new terpenoids from Trigonostemon xyphophylloides (Croiz.)L.K.Dai and T.L.Wu;Li Yu等;《Phytochemistry Letters》;20130619;472-475 *

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Address after: 211800 No. 22 Tianpu Road, Jiangbei New District, Nanjing City, Jiangsu Province

Patentee after: Yiheng Pharmaceutical Co., Ltd., Nanjing

Address before: 255086 Room 301, Yuqiao Industrial Park, 87 Wan Jie Road, hi tech Zone, Zibo, Shandong

Patentee before: Zibo Qidingli Patent Information Consulting Co., Ltd.