Application of p-coumaric acid (p-CA) in preparing drug for relaxing airway smooth muscle

A technology of airway smooth muscle and p-coumaric acid, applied in the field of medicine, to achieve the effect of relieving airway obstruction, relieving continuous contraction, and relieving symptoms of asthma and chronic obstructive pulmonary disease

Inactive Publication Date: 2019-08-27
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] p-coumaric acid (p-CA), also known as p-hydroxycinnamic acid, is one of the main components of cell walls in plants. p-coumaric acid is widely found in various plants, such as green peppers, carrots, tomatoes, Strawberries, pineapples, and garlic are rich in p-coumaric acid, but p-coumaric acid is only widely used as a phenolic acid in medicine for weight loss and anti-cancer, and has not been used in the treatment of airway smooth muscle relaxation. Applied in asthma and chronic obstructive pulmonary disease

Method used

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  • Application of p-coumaric acid (p-CA) in preparing drug for relaxing airway smooth muscle
  • Application of p-coumaric acid (p-CA) in preparing drug for relaxing airway smooth muscle
  • Application of p-coumaric acid (p-CA) in preparing drug for relaxing airway smooth muscle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment example 1

[0019] Example 1, p-coumaric acid (p-CA) can relax the contraction of airway smooth muscle induced by acetylcholine.

[0020] 1) Isolation of isolated mouse trachea

[0021] Purchase 6-8 week male adult BALB / c mice, kill the mice by neck dissection, fix them on the dissecting board, spray 75% alcohol to disinfect the surface of the mice, cut the skin, cut along the midline of the abdomen to the neck, and remove Thymus and connective tissue, and remove the trachea tissue from the mouse heart to the larynx, transect the trachea and remove it, and place the trachea tissue in pre-cooled high calcium solution. The main trachea was further separated under the dissecting microscope and put into the perfusion tank after the trachea was flattened with a hook.

[0022] 2) Detection of mouse airway smooth muscle tension

[0023] Clean the perfusion system: remove the perfusion tank and place it in alcohol for 10 minutes of ultrasound, then replace it with ultrapure water for 2-3 times....

Embodiment example 3

[0032] Implementation case 3, p-coumaric acid (p-CA) blocks the Ca of LVDCCs and NSCCs 2+ Inflow to relax tracheal smooth muscle.

[0033] 1) p-CA relaxes the pre-contraction of airway smooth muscle induced by high potassium

[0034] After the tissue is balanced, it is pre-stimulated with 100μMACH, and the tension strength reaches more than 750mg, then the formal experiment can be performed, and then p-coumaric acid is added to interfere with the pre-contraction of tracheal smooth muscle induced by high potassium. The dose-response curve of ESSB to relax high potassium precontracted tracheal smooth muscle was determined.

[0035] The above experimental results show that: the isolated mouse tracheal ring at 80mM K + Stable and continuous pre-contraction occurs under the condition, when p-coumaric acid (p-CA) is added, 0.63-6.30mM p-CA can significantly inhibit 80mM K + The induced tracheal smooth muscle contraction effect, and showed a significant dose-dependent. Among them...

experiment example 4

[0040] Experimental case 4, p-coumaric acid (p-CA) by increasing BK Ca opening to relax tracheal smooth muscle.

[0041] 1) p-CA can relax TEA and Paxiline-induced tracheal smooth muscle contraction

[0042] K was induced by the addition of 100 μMACH Ca open, and then add 10mM TEA to inhibit the K Ca The opening of the tracheal smooth muscle causes further contraction, and finally 3.98mM p-CA can promote K Ca The re-opening of p-CA, thus indicating that the role of p-CA in relaxing tracheal smooth muscle may be related to K Ca and BK Ca relevant. The role of 3.98mMp-CA in relaxing tracheal smooth muscle is due to reactivation of BK Ca Ca 2+ Outflow (p<0.001).

[0043] 2) Whole-cell recording of BK Ca The current confirms that p-CA passes through the open BK Ca channel to relax tracheal smooth muscle

[0044] Whole-cell recording BK Ca The current pulse program is: clamp at -70mV for 50ms, record for 300ms, and return to clamp at -70mV for 50ms. Repeat the above pr...

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Abstract

The invention belongs to the technical field of medicine, and specifically relates to application of p-coumaric acid (p-CA) in preparing a drug for relaxing airway smooth muscle. The invention finds the application of p-CA in preparing the drug for relaxing airway smooth muscle, finds that p-CA has a remarkable interference effect on the stimulation of high potassium and acetylcholine on the shrinkage of the irway smooth muscle and can be used to cure respiratory diseases such as asthma. According to the application of p-CA provided by the invention, detection is performed on tension of isolated tracheal circular muscle and Ca 2+ in airway smooth muscles of an experimental mouse, and it is found that p-CA has a reliving effect on airway obstruction of an asthma patient. The relaxing effectis generated when an LVDCCs and NSCCs ion passageway is blocked to inhibit calcium ion internal currents and a BKCa ion passageway is activated. The application of p-CA in preparing the drug for relaxing the airway smooth muscle is a new application of p-CA and the new application is of great significance.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of p-coumaric acid as a medicine for preparing chronic obstructive pulmonary disease and relaxing airway smooth muscle. Background technique [0002] Sustained contraction of airway smooth muscle and increased calcium sensitivity are one of the main symptoms of asthma and chronic obstructive pulmonary disease. Among the above drugs for the treatment of respiratory diseases, bronchodilator drugs such as glucocorticoids are common clinical drugs. In view of the long-term use of clinical hormone drugs will produce drug resistance and side effects and other disadvantages, the development of safer and more reliable bronchodilators has become the main way to solve the above problems. Commonly used medicines currently used for the treatment of asthma include salbutamol (Salbutamol), terbutaline (Terbutaline) and the like. [0003] p-coumaric acid (p-CA), a...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61P11/06A61P11/00
CPCA61K31/192A61P11/00A61P11/06
Inventor 彭勇波王齐刘庆华
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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