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Application of bexarotene or/and pharmaceutically acceptable salt thereof in preparation of anti-pulmonary arterial hypertension drugs

A pulmonary arterial hypertension and drug technology, applied in the field of medicine, can solve the problems such as the lack of literature reports, and achieve the effect of reducing the level of pulmonary arteriolar stenosis, reducing the level of NT-proBNP, and inhibiting the increase in systolic blood pressure

Active Publication Date: 2020-11-20
上海宛文创业孵化器管理合伙企业(有限合伙)
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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 bexarotene or/and pharmaceutically acceptable salt thereof in preparation of anti-pulmonary arterial hypertension drugs
  • Application of bexarotene or/and pharmaceutically acceptable salt thereof in preparation of anti-pulmonary arterial hypertension drugs
  • Application of bexarotene or/and pharmaceutically acceptable salt thereof in preparation of anti-pulmonary arterial hypertension drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 : Effect of bexarotene on proliferation of rat pulmonary artery smooth muscle cells

[0036] Primary cultured SD rat pulmonary artery smooth muscle cells. Specifically include: take out the complete heart and lung tissue and put it into a sterile saline culture dish containing (penicillin) double antibody, rinse the heart and lung tissue several times, carefully separate the pulmonary artery, rinse until there is no blood, add 0.2% Ι The mixed solution of type collagenase and 0.1% trypsin was transferred into a constant temperature cell incubator at 37°C and left to stand for 30 minutes for digestion, and DMEM / F12 medium containing 10% FBS was added to terminate the digestion. All experiments used cells of passage P3-P8. In the passaging stage, 0.25% trypsin was used for digestion and passaging. Observe the state of the cells with a microscope, culture to the 3rd to 8th generation, observe the state of the cells with a microscope, and select the cells with...

Embodiment 2

[0039] Example 2 : Effect of Bexarotene on the Migration Activity of Rat Pulmonary Artery Smooth Muscle Cells

[0040] Cell migration activity was detected by Wound-Healing Assay. Plant PASMC in the logarithmic growth phase in a 24-well plate at a density of 105 / mL, with 500 μL of cell suspension per well. When the cells are 80% confluent, replace with serum-free medium and continue to culture for 24 hours to synchronize the cells in the G0 phase. . Use a 200 μL pipette tip to scratch the cells perpendicular to the well plate, and try to ensure that the width of each scratch is consistent. Aspirate the cell culture medium, rinse the well plate three times with normal saline, and wash away the cell debris produced by scratches. Add PDGF to a final concentration of 40ng / mL, and continue culturing. After 24 hours, photographs were recorded under an inverted microscope, and the cell migration ability was evaluated by the ratio of the migration area of ​​each group to the migr...

Embodiment 3

[0042] Example 3 : Preparation of Rat Pulmonary Hypertension Model

[0043] Pulmonary hypertension is caused by many reasons, and the remodeling of pulmonary artery vascular structure is the main pathological reason. One-time injection of monocrotaline (MCT), through delayed and progressive rat pulmonary artery vascular endothelial cell injury, small pulmonary artery platelet thrombosis, abnormal proliferation of smooth muscle cells and other changes, leads to progressive increase of pulmonary dynamic pressure, resulting in rat pulmonary hypertension model . Dosing was started one week after the model was established, and bexarotene was given continuously for 3 weeks. In this embodiment, rat pulmonary artery systolic pressure (pulmonary artery systolic pressure, PASP) and right ventricular systolic pressure (right ventricular systolic pressure, RVSP), right ventricular wall thickness (right ventricular wall thickness, RVWT), serum pulmonary hypertension serum marker amino ...

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PUM

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Abstract

The invention relates to an application of bexarotene (4-[1-(5, 6, 7, 8-tetrahydro-3, 5, 5, 8, 8-pentamethyl-2-naphthyl) vinyl] benzoic acid) or / and a pharmaceutically acceptable salt thereof in preparation of anti-pulmonary arterial hypertension drugs. The chemical structural formula of bexarotene is shown as a formula I in the specification. According to the application, rat pulmonary artery smooth muscle cells are adopted for investigating the smooth muscle cell proliferation and migration inhibiting effect of bexarotene, and the result shows that bexarotene can obviously inhibit PASMCs proliferation and migration. The monocrotaline-induced rat pulmonary arterial hypertension model is adopted to investigate the anti-pulmonary arterial hypertension vascular remodeling of the bexarotene,and the result shows that the oral administration of the bexarotene can significantly inhibit the increase of the pulmonary arterial pressure and the right ventricular systolic pressure of rats, significantly reduce the NT-proBNP level in the rat plasma, can obviously inhibit thickening of pulmonary artery intima media and reduce the narrow level of pulmonary arteriole lumens, and a safe, effective and economical solution is provided for prevention and treatment of pulmonary arterial hypertension and pulmonary vascular remodeling.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of bexarotene or / and a pharmaceutically acceptable salt thereof in the preparation of anti-pulmonary hypertension drugs. Background technique [0002] Pulmonary artery hypertension (PAH), known as "cancer of the cardiopulmonary vascular system", is a rare disease that is difficult to diagnose and treat. It is conservatively estimated that there are about 5 million to 8 million PAH patients in my country. The average age of onset is only 36 years old, and the median survival period is only 2.8 years. During the period of living with the disease, the quality of life is extremely poor. Although new drugs have been released in recent years, the 5-year survival rate of PAH patients is still only 57%. How to further prolong the life of patients and improve the quality of life of patients is a huge challenge. [0003] At present, there is still no clear conclusion on t...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61P11/00A61P9/12
CPCA61K31/192A61P11/00A61P9/12
Inventor 孙韬孙崇岳
Owner 上海宛文创业孵化器管理合伙企业(有限合伙)
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