Application of N-[2-methyl-1-(pyrrolidine-1-carbonyl)-propyl]-3-phenyl propionamide in pharmacy

A technology of phenylpropanamide and pyrrolidine, applied in the field of small molecule compound N-[2-methyl-1--propyl]-3-phenylpropanamide, which can solve the prevention and treatment of heart failure has not been reported, etc. problems, to achieve good medicinal prospects and strong pharmacological effects

Inactive Publication Date: 2009-07-08
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on its preventive effect in ventricular remodeling and heart failure

Method used

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  • Application of N-[2-methyl-1-(pyrrolidine-1-carbonyl)-propyl]-3-phenyl propionamide in pharmacy
  • Application of N-[2-methyl-1-(pyrrolidine-1-carbonyl)-propyl]-3-phenyl propionamide in pharmacy
  • Application of N-[2-methyl-1-(pyrrolidine-1-carbonyl)-propyl]-3-phenyl propionamide in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 (Observation of the protective effect of AS-1 on pressure load-induced ventricular remodeling)

[0048] Male C57BL / 6 mice of SPF grade were selected and randomly divided into 4 groups for 7 to 8 weeks: sham operation group (Sham), operation group (TAC), operation+solvent control group (DMSO), operation+administration group (AS -1), 6-8 per group. Mice were artificially ventilated after anesthesia, the thorax was opened at the 2nd-3rd intercostal space on the left side of the chest, the aortic arch was separated, the aortic arch (Transverse aortic constriction, TAC) was narrowed according to the uniform standard, and the thorax was closed. Except that TAC was not performed in the sham operation group, the rest of the operation procedure was completely the same as that in the model group. The DMSO and AS-1 groups were administered intraperitoneally after operation, once a day, and the concentration of AS-1 was 50 mg / kg. After continuous administration for 2 wee...

Embodiment 2

[0062] Embodiment 2 (observation of the effect of AS-1 on hypertrophic primary cardiomyocytes)

[0063] The method of culturing primary cardiomyocytes in vitro is as follows: After the clean-grade SD suckling mice were sacrificed by neck dislocation, the heart was collected, the apex was cut off, digested, centrifuged, and placed in DMEM medium containing 15% calf serum, 37°C, 5% CO 2 Cultivate in the incubator for 36-48hr. When the cell growth is observed to be good, change the medium and divide into groups. The experiment was divided into four groups: blank (control) group; IL-1 stimulation group; IL-1 stimulation+DMSO group; IL-1 stimulation+AS-1 group. The stimulation concentration of IL-1 was 10ng / mL, and the concentration of AS-1 was 100umol / L.

[0064] 2.1 Detection of cardiomyocyte hypertrophy

[0065] 24 hours after primary cultured cardiomyocytes were stimulated, the area of ​​cardiomyocytes was detected by α-actinin immunofluorescence staining, and the protein syn...

Embodiment 3

[0070] Example 3 (observation of the protective effect of AS-1 on the heart of acute ischemia-reperfusion mice)

[0071] SPF male C57BL / 6 mice were selected and randomly divided into 4 groups for 6 to 7 weeks: sham operation group (Sham), operation group (I / R), operation+solvent control group (DMSO), operation+administration group (AS-1), 6-8 per group. Mice were artificially ventilated after anesthesia, and the ischemia / reperfusion (I / R) model was established. The main steps were: open the chest cavity at the 3rd to 4th intercostal space on the left side of the chest, cut the pericardium, and ligate according to uniform standards The left anterior descending coronary artery blocked the blood flow for 45 minutes, then restored blood reperfusion, and closed the chest cavity. Immediately after reperfusion, DMSO or AS-1 was intraperitoneally administered, and the concentration of AS-1 was 50 mg / kg. After 4 hours of reperfusion, myocardial tissue was taken to detect various indi...

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Abstract

The invention relates to an application of N-(2-methyl-1-(pyrrolidine-1-carbonyl)-propyl)-3-phenyl propanamide (AS-1) in pharmaceuticals for preventing and treating ventricular remodeling and cardiac failure, application of N-(2-methyl-1-(pyrrolidine-1-carbonyl)-propyl)-3-phenyl propanamide (AS-1) in pharmaceuticals for preventing and treating myocardial hypertrophy and ventricular remodeling resulting from pressure load, and application of N-(2-methyl-1-(pyrrolidine-1-carbonyl)-propyl)-3-phenyl propanamide (AS-1) in pharmaceuticals for preventing and treating acute ischemic heart disease and cardiac ischemia-reperfusion injury.

Description

1. Technical field [0001] The present invention relates to chemically synthesized small molecular compound N-[2-methyl-1-(pyrrolidine-1-carbonyl)-propyl]-3-phenylpropanamide (hydrocinnamoyl-L-valyl pyrrolidine, AS-1 ) purposes, especially related to the application in the field of pharmacy. 2. Background technology [0002] Since the 1990s, the morbidity and mortality of cardiovascular diseases have increased significantly worldwide, and heart failure has become the leading cause of death. Heart failure refers to the disorder of systolic and / or diastolic function of the heart under the action of various pathogenic factors, resulting in an absolute or relative decrease in cardiac output, that is, the weakening of the heart pump function, so that it cannot meet the pathological requirements of the body's metabolism. Physiological process or syndrome. Hypertension, myocardial infarction, aortic valve stenosis, and myocarditis are common causes of heart failure. The basis of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/40A61P9/04A61P9/00A61P9/10
Inventor 李跃华刘春样李婷曹志娟胡玉龙李金恒
Owner NANJING MEDICAL UNIV
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