CN102872034B - Application of Gypensapogenin B in medicaments for treating rhinitis - Google Patents
Application of Gypensapogenin B in medicaments for treating rhinitis Download PDFInfo
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- CN102872034B CN102872034B CN 201210417159 CN201210417159A CN102872034B CN 102872034 B CN102872034 B CN 102872034B CN 201210417159 CN201210417159 CN 201210417159 CN 201210417159 A CN201210417159 A CN 201210417159A CN 102872034 B CN102872034 B CN 102872034B
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Abstract
The invention discloses Gypensapogenin B for preparing medicaments for treating immunity inflammation, which is particularly suitable for preparing medicaments for treating rhinitis. By taking Terfenadine and diclofenac sodium as controls, Gypensapogenin B has definite curative effects. The application of Gypensapogenin B in preparing medicaments for treating rhinitis, involved in the invention, is disclosed for the first time. As the skeleton type is brand new, and the strong activity of Gypensapogenin B on treating rhinitis is unexpectedly strong, the possibility that any enlightenments are given by other compounds does not exist. Gypensapogenin B has prominent substantive features and has notable progress when being used for preventing and treating rhinitis.
Description
Technical field
The present invention relates to the application of Gypensapogenin 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, the treatment rhinitis mainly adopts antihistamine drug or the Claritins such as tranilast, ketotifen such as teldane, 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 Gypensapogenin B the present invention relates to is one and within 2012, delivers (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to the cytotoxic activity (Li of human tumor cell line, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.), , purposes for the Gypensapogenin 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 do not is 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 Gypensapogenin B aspect preparation treatment rhinitis.
Described compound Gypensapogenin B structure is as shown in formula I:
Formula I
Gypensapogenin 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 Gypensapogenin 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 do not is 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 Gypensapogenin B involved in the present invention is referring to document (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178. and Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45 (3): 167-171.).
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 Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example 1, Gypensapogenin 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, the next day of thereafter, injection is 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.Observe at once rat sneeze in 30 minutes after last instils 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, Gypensapogenin 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 Gypensapogenin 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 relatively
The impact of the rat rhinitis that experimental example 2, Gypensapogenin B of the present invention cause histamine
Male SD rat, body weight 180 ~ 220g, orally give after trial drug 1 hour, and the 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, Gypensapogenin B(10,20mg/kg of the present invention) obviously reduce the sneeze number of times of rhinitis rat due to histamine, to scratching, the nose reaction is inhibition trend.Teldane 10mg/kg is significant inhibitory action.
Table 2 Gypensapogenin B of the present invention causes the impact (x ± SD) of rat rhinitis on histamine
* p<0.05, * * p<0.01, with matched group relatively
Experimental example 3, Gypensapogenin 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, observing with active sensitization rat and normal rat 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, collected perfusate 10 minutes after 3 minutes.At sensitized rats and normal rat, contain respectively ovalbumin 1mg/ml and histamine 40ug/ml in perfusate, the perfusate of collecting from nasal cavity centrifugal 10 minutes through 1200 * g, the blue concentration of the Evans in 620nm place colorimetric determination supernatant, first 1 hour oral administration of tested medicine and antigen or histamine perfusion.
From table 3, Gypensapogenin 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 Gypensapogenin B of the present invention causes on ovalbumin the impact (x ± SD) that rat nasal cavity vascular permeability raises
* p<0.01, compare with matched group
From table 4, Gypensapogenin 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 Gypensapogenin B of the present invention causes on histamine the impact (x ± SD) that rat nasal cavity blood flow permeability raises
* p<0.01, compare with matched group
Conclusion: Gypensapogenin 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)
1. the Gypensapogenin B application in preparation treatment rhinitis medicine, described compound Gypensapogenin B structure as
formula Ishown in:
Formula I.
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| CN 201210417159 CN102872034B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicaments for treating rhinitis |
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| CN 201210417159 CN102872034B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicaments for treating rhinitis |
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| CN102872034B true CN102872034B (en) | 2013-12-18 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105188661A (en) * | 2013-03-08 | 2015-12-23 | 深圳华大基因科技有限公司 | Composition and food comprising same and preparation method of food |
| CN106551936A (en) * | 2016-11-18 | 2017-04-05 | 苏州枫灵医药科技有限公司 | One kind treats rhinitis medicine and its application |
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