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Use of beta-elemene and derivatives thereof in preventing atherosclerosis

A technology of elemene and derivatives, applied in the preparation of anti-atherosclerotic drugs, in the field of beta-elemene and derivatives thereof, can solve problems such as no reports on the application of anti-atherosclerotic drugs

Inactive Publication Date: 2013-09-11
DALIAN YUANDA PHARMA TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no application report of this type of compound in the preparation of anti-atherosclerotic drugs so far.

Method used

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  • Use of beta-elemene and derivatives thereof in preventing atherosclerosis
  • Use of beta-elemene and derivatives thereof in preventing atherosclerosis
  • Use of beta-elemene and derivatives thereof in preventing atherosclerosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Protective Effects of β-Elemene and Its Derivatives on Peroxidative Damage of HUVEC Cells

[0026] 1.1. Experimental method: HUVEC cells in the logarithmic growth phase were taken, and 2×10 5 Inoculated in 50ml cell culture flasks, cultured for 24 hours, discarded the culture medium, added fresh serum-free DMEM high-glucose medium to the blank group and injured group, and cultured routinely. On this basis, the treatment group was added various drugs with a concentration of 1 μg / ml, and after continuing to culture for 24 hours, adding H 2 o 2 After treatment with DMEM serum-free medium at a final concentration of 100 μmol / L for 2 hours, the contents of malondialdehyde (MDA) and superoxide dismutase (SOD) in the cells were detected.

[0027] SOD increase rate = (administration group - model group) / administration group * 100%

[0028] MDA reduction rate = (model group - drug administration group) / model group * 100%

[0029] 1.2. Experimental results: as described i...

Embodiment 2

[0035] β-Elemene and its derivatives on H 2 o 2 Effects of adhesion factors in HUVEC after injury

[0036] 2.1 Experimental method: Take HUVEC cells in the logarithmic growth phase, and use 1×10 per well 5 The number was added to the 6-well plate. After the cells were cultured for 24 hours, the supernatant was discarded, and the cells were divided into a normal control group, a high-fat cell model group, a high-fat cell model+β-elemene / β-elemene structural derivative, and a solvent control group. After culturing for 24 h, add H 2 o 2 The culture solution with a final concentration of 100 μmol / L was treated for 2 hours, and the intracellular protein was extracted, and the protein was determined by BCA, and human intercellular adhesion factor 1 (ICAM-1) and vascular cell adhesion molecule (VCAM-1) in HUVEC cells were detected by ELISA. -1) content.

[0037] 2.2 Experimental results: as shown in Table 2,

[0038] Table 2 β-elemene and its derivatives on H 2 o 2 Effects o...

Embodiment 3

[0043] Lipid-lowering effect of β-elemene and its derivatives on HepG2 cells in vitro

[0044] 3.1 Experimental method: Take the HepG2 cells in the logarithmic growth phase, and use 1×10 5The number was added to the 6-well plate. After the cells were cultured for 24 hours, the supernatant was discarded, and the cells were divided into a normal control group, a high-fat cell model group, a high-fat cell model+β-elemene / β-elemene structural derivative, and a solvent control group. Among them, FFA with a final concentration of 1 mmol / L was added to all cells in the hyperlipidemia model group, and the remaining volume was made up to 2 mL with DMEM without serum. After 24 hours of administration, they were washed 5 times with PBS at 37 ° C to remove unabsorbed cells. Cells were lysed with FFA, centrifuged at 12,000g for 10min, and the supernatant was taken. Part of the supernatant was used for protein quantification by BCA method, and the remaining supernatant was used for TG and ...

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Abstract

The invention relates to the field of natural medicines, and particularly relates to use of beta-elemene and derivatives thereof in preventing atherosclerosis, and in particular relates to an application in preparation of medicines for treating atherosclerosis. Test results show that beta-elemene and derivatives can remarkably reduce the atherosclerotic plaque area in the coronary artery of an animal model, and meanwhile has remarkable improving effect on two key links in development process of atherosclerosis: adhesion of leukocyte and endothelial cells and peroxidation of lipids. Expression of adherence factors closely related to atherosclerosis can be reduced, so that peroxidation damage of endothelial cells in vitro and in vivo caused by high fat and H2O2 is avoided.

Description

technical field [0001] The invention relates to the field of natural medicines, in particular to the use of β-elemene and its derivatives, in particular to the application in the preparation of anti-atherosclerotic drugs. Background technique [0002] Atherosclerosis (AS) is a common disease that often involves important parts such as the heart and cerebrovascular, leading to serious consequences. Coronary artery atherosclerosis, if the stenosis reaches more than 75%, angina pectoris, myocardial infarction, arrhythmia, and even sudden death may occur. Cerebral arteriosclerosis can cause cerebral ischemia, brain atrophy, or cause cerebral blood vessel rupture and bleeding. The pathogenesis of atherosclerosis is very complex and has not yet been understood. [0003] During the occurrence and development of atherosclerosis, various cytokines, inflammatory mediators, lipids and fiber components will increase, and when their quantity accumulates to a certain extent, clinical ca...

Claims

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Application Information

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IPC IPC(8): A61K31/015A61K31/035A61K31/11A61K31/045A61P9/10A61P9/00A61P7/02A61P9/12A61P13/12A61P39/06
Inventor 尚靖许婷许海何婷毛利飞霍韦敏李妤田友清
Owner DALIAN YUANDA PHARMA TECH DEV
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