阅读说明：本技术 萝芙木乙醇提取物在制备用于舒张预收缩的气管平滑肌药物中的应用 (Application of devilpepper ethanol extract in preparation of medicine for relaxing and pre-contracting tracheal smooth muscle ) 是由 沈金花 李威 于 2021-01-27 设计创作，主要内容包括：本发明涉及医药技术领域,尤其涉及萝芙木乙醇提取物在制备用于舒张预收缩的气管平滑肌的药物中的应用。本发明通过对实验小鼠离体气管环肌张力的检测,发现萝芙木乙醇提取物具有高效的舒张气管平滑肌的作用,提示此物质有望应用于缓解哮喘。为开发萝芙木乙醇提取物在制备用于舒张预收缩的气管平滑肌的药物中的应用提供了依据。(The invention relates to the technical field of medicines, in particular to application of a rauwolfia ethanol extract in preparing a medicine for relaxing pre-contracted tracheal smooth muscle. According to the invention, through detecting the tension of isolated tracheal ring muscle of an experimental mouse, the rauvolfia verticillata ethanol extract is found to have an efficient effect of relaxing tracheal smooth muscle, and the substance is expected to be applied to relieving asthma. Provides basis for developing the application of the rauwolfia ethanol extract in preparing the medicine for relaxing the pre-contracted tracheal smooth muscle.)

1. Application of devilpepper ethanol extract in preparing medicine for relaxing pre-contracted tracheal smooth muscle is provided.

2. Use of an ethanol extract of rauvolfia verticillata according to claim 1 for the preparation of a medicament for relaxing pre-contracted tracheal smooth muscle, characterized in that: the rauwolfia ethanol extract is applied by relaxing the contraction of airway smooth muscle induced by high potassium.

3. Use of an ethanol extract of rauvolfia verticillata according to claim 1 for the preparation of a medicament for relaxing pre-contracted tracheal smooth muscle, characterized in that: the rauwolfia ethanol extract is applied by relaxing acetylcholine-induced contraction of airway smooth muscle.

4. Use of an ethanol extract of rauvolfia verticillata according to any one of claims 1 to 3 for the preparation of a medicament for relaxing pre-contracted tracheal smooth muscle, characterized in that: the medicine is used for treating asthma.

5. Use of an ethanol extract of rauvolfia verticillata according to any one of claims 1 to 3 for the preparation of a medicament for relaxing pre-contracted tracheal smooth muscle, characterized in that: the dosage forms of the medicine at least comprise paste, capsules, tablets and microcapsule preparations.

6. Use of an ethanol extract of rauvolfia verticillata according to any one of claims 1 to 3 for the preparation of a medicament for relaxing pre-contracted tracheal smooth muscle, characterized in that: the administration modes of the medicine at least comprise injection, oral administration and subcutaneous administration.

7. Use of an ethanol extract of rauvolfia verticillata according to claim 1 for the preparation of a medicament for relaxing pre-contracted tracheal smooth muscle, characterized in that: the preparation method of the rauwolfia ethanol extract comprises drying and pulverizing rauwolfia, soaking in 95% ethanol solution at room temperature, and rotary evaporating the filtrate to obtain ethanol extract.

Technical Field

The invention relates to the technical field of medicines, in particular to application of a rauwolfia ethanol extract in preparing a medicine for relaxing pre-contracted tracheal smooth muscle.

Background

Asthma is called bronchial asthma and is commonly involved in structural cells, inflammatory cells, cell components and the like. Asthma is clinically manifested as paroxysmal dyspnea, chest distress, cough, etc., and is usually accompanied by wheezing sounds. Data show that the development of the social industry leads to increasingly poor air quality and increased content of harmful substances in the air, thereby causing the remarkable increase of asthma cases. The traditional Chinese medicine has the advantages of long research history, low price, mild action, difficult generation of drug resistance and the like, and is taken as a research idea to discover a safe and effective medicine for treating asthma.

Rauwolfia is a commonly used medicinal material in traditional Chinese medicine treatment, is taken from dried roots of Rauwolfia of Apocynaceae, is bitter and slightly pungent in taste and cool in nature, has the main effects of clearing heat, reducing blood pressure, promoting urination, calming the nerves and the like, and is mainly used for treating diseases such as cold, fever, sore throat, traumatic injury, hypertension, headache, insomnia and the like. At present, no report on the research of utilizing rauvolfia to relax tracheal smooth muscle so as to treat asthma is found.

Disclosure of Invention

The invention relates to an action mechanism of a rauwolfia ethanol extract in relaxing pre-contracted tracheal smooth muscle, and provides a basis for developing the application of the rauwolfia ethanol extract in relaxing the tracheal smooth muscle for treating asthma.

The technical scheme provided by the invention is the application of the rauwolfia ethanol extract in preparing the medicine for relaxing the pre-contracted tracheal smooth muscle.

Wherein the rauwolfia ethanol extract is used for realizing the application by relaxing the contraction of airway smooth muscle induced by high potassium.

Wherein the rauwolfia ethanol extract is applied by relaxing acetylcholine-induced contraction of airway smooth muscle.

Furthermore, the medicament is for the treatment of asthma.

Moreover, the dosage forms of the medicine at least comprise paste, capsules, tablets and microcapsule preparations.

Furthermore, the administration modes of the drug at least include injection, oral administration and subcutaneous administration.

The preparation method of the rauwolfia ethanol extract comprises the steps of drying and crushing rauwolfia, soaking in 95% ethanol solution at room temperature, and performing rotary evaporation on the filtrate obtained by filtering to obtain an ethanol extract, thus obtaining the rauwolfia ethanol extract.

Compared with the prior art, the technical scheme has the beneficial effects that: according to the invention, through detecting the tension of isolated tracheal ring muscle of an experimental mouse, the rauvolfia verticillata ethanol extract is found to have an efficient effect of relaxing tracheal smooth muscle, and the substance is expected to be applied to relieving asthma. Provides basis for developing the application of the rauwolfia ethanol extract in preparing the medicine for relaxing the pre-contracted tracheal smooth muscle.

Drawings

FIG. 1 is a graph of the vasodilation effect of ethanol extract of Rauwolfia verticillata on pre-constricted tracheal rings induced by high potassium;

FIG. 2 shows the vasodilation effect of the ethanol extract of rauwolfia verticillata on the pre-contracted tracheal rings induced by acetylcholine.

Detailed Description

The present invention will be described in detail with reference to the accompanying drawings and examples, and the present invention is not limited to the examples.

1. Preparing the rauwolfia ethanol extract:

grinding dried root of devilpepper (Rauwolfia Rauvolfia L.) as raw material into powder. 500g of rauvolfia powder is taken and soaked in 95% ethanol solution at room temperature for 4 days according to the solid-to-liquid ratio of 1: 10. Filtering the soaked solution, rotary evaporating to obtain ethanol extract, which is radix Rauvolfiae ethanol extract, and placing in a vacuum drying oven for use. In the experiment, dimethyl sulfoxide (DMSO) is used as a solvent to dissolve the rauvolfia ethanol extract for bioactivity experiment.

2. In vitro isolation of mouse trachea

The animals used in the experiment were male BALB/c mice 6-8 weeks old. After the mice were sacrificed by cervical dislocation, the abdomen was kept upward and fixed. Disinfecting with ethanol, cutting the chest along midline to expose cardiopulmonary tissue, cutting off heart, taking off tissue between laryngeal prominence and lung, immediately soaking in ice-bath PSS solution (135mM NaCl, 10mM glucose, 10mM HEPES, 5mM KCl, 2mM CaCl)₂，1mM MgCl₂pH is adjusted to 7.4 by NaOH solution), and finally the trachea is placed on a dissecting disc containing ice-bath PSS solution, the trachea is trimmed under a stereomicroscope to remove redundant tissues around the tracheal rings, and the tracheal rings with proper length are separated.

3. The tension detection method of the mouse airway smooth muscle comprises the following steps:

after the cut tracheal rings were fixed by two triangular hooks of appropriate size, one end was connected to a tension transducer and the other end was used for fixation, and placed in a constant temperature water bath to which 6mL of PSS solution was added, and oxygen was continuously supplied while maintaining the temperature of the water bath at 37 ℃. The preload was adjusted to about 300mg, and after 15 minutes the 6mL PSS solution preheated to 37 ℃ was replaced and the preload adjusted again to around 300 mg. The above procedure was repeated 4 times for a total of 60 minutes of equilibration. After the balance is finished, 80mmol/L KCl or 100 mu mol/L ACh is added into the water bath to stimulate the tracheal rings, after the tracheal rings are completely contracted, the PSS solution is used for elution to reduce the tension to the baseline level, and the experiment is started after the tracheal rings are stabilized at the baseline level for 30 minutes.

The experimental results are as follows:

(1) relaxation of potassium-induced preshrinked tracheal rings by ethanol extract of devilpepper (EERV)

Potassium ion acts as an agonist of voltage-dependent calcium channels (VDCCs) and causes VDCCs of airway smooth muscle to open. The extracellular calcium ion flows in under the action of potassium ion, and the concentration of the calcium ion in the cell is rapidly increased to cause the contraction of the tracheal smooth muscle. As shown in figure 1, when 80mmol/L KCl is used to make isolated tracheal rings continuously and stably contract, the ethanol extract of rauvolfia verticillata can inhibit the contraction of the isolated tracheal rings in a dose-dependent manner, and the maximum diastole value is (101.88 +/-1.13)%. The rauvolfia ethanol extract can be used for dose-dependently relaxing tracheal smooth muscle pre-contracted by high potassium induction.

(2) Relaxation of acetylcholine (ACh) -induced preshrinked tracheal rings by Ethanol Extract of Rauvolfia Verticillata (EERV)

ACh acts as an agonist of non-selective cation channels (NSCCs) and voltage-dependent calcium channels (VDCCs) and opens NSCCs and VDCCs of airway smooth muscle, promoting both external calcium influx and internal calcium release. As shown in figure 2, after 100. mu. mol/L ACh is added to stimulate the tracheal rings, the isolated tracheal rings produce sustained and stable contraction which can also be dose-dependently inhibited by the ethanol extract of Rauwolfia verticillata, and the maximum diastole value is (99.73 +/-1.11)%. Shows that the rauwolfia ethanol extract can relax the airway smooth muscle pre-contracted by ACh induction in a dose-dependent manner.

In conclusion, the experiment shows that the rauwolfia ethanol extract has the efficient function of relaxing the smooth muscle of the trachea, and the substance is expected to be applied to relieving asthma. Provides basis for developing the application of the rauwolfia ethanol extract in preparing the medicine for relaxing the pre-contracted tracheal smooth muscle.