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Application of pinocembrin to preparation of medicines for preventing and/or treating pulmonary hypertension

A technology for pulmonary arterial hypertension and uses, applied in the directions of drug combination, application, food science, etc., can solve the problem of no effect reported in the literature, and achieve the effects of preventing and treating right ventricular hypertrophy, restoring lung tissue function, and reducing mortality.

Active Publication Date: 2016-12-07
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After reviewing the literature, it was found that there is no literature reporting the effect of this compound on the treatment of pulmonary arterial hypertension.

Method used

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  • Application of pinocembrin to preparation of medicines for preventing and/or treating pulmonary hypertension
  • Application of pinocembrin to preparation of medicines for preventing and/or treating pulmonary hypertension
  • Application of pinocembrin to preparation of medicines for preventing and/or treating pulmonary hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Establishment of a model of pulmonary hypertension in rats.

[0033] Monocrotaline is a kind of pyrrolidine alkaloid extracted from wild lily seeds. It is converted into wild lily pyrrole by mixed function oxidase in the liver in rats, and wild lily pyrrole damages pulmonary vascular endothelial cells, thereby causing pulmonary artery smooth muscle cells Progressive proliferation leads to a progressive increase in pulmonary arterial pressure, resulting in a model of pulmonary hypertension in rats. Dosing was started one week after the model was established, and pinocerine was given continuously for 18 days. In this embodiment, by observing the rat electrocardiogram, measure the rat aortic pressure and pulmonary artery pressure (right ventricular pressure), measure the index of each organ of the experimental rat, the degree of right ventricular thickening, serum enzymes and pulmonary hypertension markers, tissue inflammatory factors As well as histomorphologi...

Embodiment 2

[0038] Example 2: Improvement effect of pinocerin on electrocardiogram in rats with pulmonary arterial hypertension.

[0039] Rats in each of the above groups were fasted overnight after the last administration, anesthetized with pentobarbital sodium 50mg / kg the next day, needle-shaped electrodes were inserted subcutaneously in the front and rear limbs, and the electrocardiogram of lead II of the rats was recorded, and the S wave deepening of the electrocardiogram was observed. case and the R wave inversion case. The results show (attached figure 2 ), the electrocardiogram of normal rats was in a normal state, and the injection of monocrotaline caused the right axis deviation of the electrocardiogram in rats, resulting in R wave inversion and S wave deepening, and right ventricular dysfunction. Two positive drugs, bosentan and fasudil, can significantly improve the ECG changes in rats caused by monocrotaline. failure symptoms, indicating that pinoxetine has a good effect on...

Embodiment 3

[0040] Embodiment 3: the influence of pinoscelin on aortic pressure and heart rate in pulmonary hypertension rats

[0041] Cut the rat neck skin along the midline, bluntly separate the neck muscles, and carefully separate the left common carotid artery obliquely below the trachea. Ligate the distal end, temporarily stop the bleeding with a hemostat at the proximal end, make a V-shaped incision, insert a PE catheter filled with heparin saline into the carotid artery, and fix it with sutures, then loosen the hemostat to allow smooth blood flow , observe the carotid artery pressure, that is, aortic systolic pressure, diastolic blood pressure and heart rate. The results show (attached image 3 ), resulting in a compensatory increase in aortic pressure due to cardiac insufficiency due to pulmonary hypertension. Given the positive drug bosentan, this phenomenon was less improved; another positive drug, Fasudil, could significantly reduce the increase in aortic pressure. Giving pi...

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Abstract

The invention relates to new pharmacological effects of a compound pinocembrin and an application of pinocembrin to preparation of products for preventing, relieving and / or treating pulmonary hypertension and complications thereof. Pinocembrin has the beneficial effects that pinocembrin has the pharmacological effects of relaxing pulmonary arteries, reducing the pulmonary artery pressure, protecting pulmonary vessels from injuries caused by pulmonary hypertension, restoring lung tissue functions, repairing heart and liver injuries, alleviating right ventricular hypertrophy and enlargement, improving heart failure and liver functions, obviously reducing the mortality of animals with pulmonary hypertension and preventing and treating pulmonary hypertension and complications thereof; pinocembrin is an active monomer separated from a natural product propolis, achieves complete synthesis at present, has good application and development prospects, is an ideal compound for treating pulmonary hypertension and complications thereof and can be applied to preparation of the products for preventing, relieving and / or treating pulmonary hypertension and complications thereof, such as chronic obstructive emphysema, chronic pulmonary heart diseases, right heart failure and liver function injuries.

Description

technical field [0001] The invention relates to the new pharmacological action of the innovative drug Pinocembrin and the use of the pinocembrin in the preparation of products for preventing, alleviating and / or treating pulmonary hypertension and its complications, belonging to the technical field of innovative drugs. technical background [0002] Primary pulmonary hypertension is a rare but very serious condition. The age of its onset population is on the low side, about 75% of patients are concentrated in the age group of 20-40 years old, and about 15% of patients are under 20 years old. At present, there is still no clear conclusion on the pathogenesis of pulmonary hypertension, and primary hyperplasia of pulmonary arterioles leading to vascular occlusion may be the main cause of its pathogenesis. [0003] When pulmonary hypertension occurs, the patient will show symptoms such as dyspnea, palpitations, chest pain, hemoptysis, and syncope. In the late stage, hypoxia, righ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/7048A61P9/12A61P9/04A61P9/00A61P11/00A61P1/16A23L33/10
CPCA23V2002/00A61K31/352A61K31/7048A23V2200/314A23V2200/30
Inventor 杜冠华方莲花袁天翊陈俞材阎雨张惠芳林溢煌
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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