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Use of 1-erucic acyl-4-(3'-chloro-)benzylpiperazine in medicine preparation

A technology of sinapinyl and benzylpiperazine, which is applied in the application field of compound 1-sinacinyl-4-benzylpiperazine in pharmaceuticals, can solve problems such as unapplied introductions, and achieve the treatment of vascular diseases and the protection of endothelial cell function Effect

Inactive Publication Date: 2012-04-18
SHANTOU UNIV MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is currently no drug that directly protects the function of endothelial cells. The 1-sinacinyl-4-(3'-Cl-)benzylpiperazine in the present invention has significant antioxidant, anti-inflammatory and antagonizing effects on adhesion molecules. Become a new drug that effectively protects the function of endothelial cells for the treatment of vascular diseases
[0003] Chinese patent 201010112900.7 has disclosed the preparation of 1-sinapinyl-4-(3'-Cl-)benzylpiperazine, but has not yet introduced its application in pharmaceuticals, nor has it been reported in other documents

Method used

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  • Use of 1-erucic acyl-4-(3'-chloro-)benzylpiperazine in medicine preparation
  • Use of 1-erucic acyl-4-(3'-chloro-)benzylpiperazine in medicine preparation
  • Use of 1-erucic acyl-4-(3'-chloro-)benzylpiperazine in medicine preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Using fluorescent probe dihydroethidium (DHE) labeling to determine that 1-sinoyl-4-(3'-Cl-)benzylpiperazine (SA9) has the effect of inhibiting oxidative stress in vascular endothelial cells.

[0022] The experiment was divided into four groups, the vascular endothelial cell control group (Ctrl) without any treatment, the vascular endothelial cell group with SA9 only (SA9), and the vascular endothelial cell group with stimulating factor TNF-α (TNF-α). The vascular endothelial cell group (SA9+TNF-α) was added with SA9 and stimulating factor TNF-α. Vascular endothelial cells (HUVECs) cells grow to 90%, labeled with fluorescent probe Dihydroethidium (DHE) (5uM), incubated for 20m in a 37° incubator, 1uM SA9 acts for 0.5h, and then TNF is added to the culture medium -α(10ng / ml) acts for 20m, and the fluorescence microplate reader measures superoxide anion at 485 / 620 wavelength. The result is figure 1 As shown, TNF-α increases the superoxide anion production of vasc...

Embodiment 2

[0023] Example 2 Using the fluorescent probe dichlorofluorescein diacetate (2',7'-dichlorofluorescein diacetate, DCFH-DA) labeling and determination of 1-sinapicoyl-4-(3'-Cl-)benzylpiperazine (SA9) has the effect of inhibiting the oxidative stress of vascular endothelial cells.

[0024] The experiment was divided into four groups, the vascular endothelial cell control group (Ctrl) without any treatment, the vascular endothelial cell group with SA9 only (SA9), and the vascular endothelial cell group with stimulating factor TNF-α (TNF-α). The vascular endothelial cell group (SA9+TNF-α) was added with SA9 and stimulating factor TNF-α. After vascular endothelial cells (HUVECs) cells grow to 90%, add 1μM SA9 for 0.5h, then incubate with 10ng / ml TNF-α and 5μM DCFH-DA for 0.5h. Fluorescence microplate reader measures the total Active oxygen ROS. The result is figure 2 As shown, TNF-α increases the total active oxygen production of vascular endothelial cells, and SA9 inhibits the effe...

Embodiment 3

[0025] In Example 3, it was determined that 1-sinoyl-4-(3'-Cl-)benzylpiperazine (SA9) has the effect of inhibiting the oxidative stress of vascular endothelial cells based on the nuclear translocation of NF-κB.

[0026] The experiment was divided into four groups, the vascular endothelial cell control group (Ctrl) without any treatment, the vascular endothelial cell group with SA9 only (SA9), and the vascular endothelial cell group with stimulating factor TNF-α (TNF-α). The vascular endothelial cell group (SA9+TNF-α) was added with SA9 and stimulating factor TNF-α. After vascular endothelial cells (HUVECs) cells grew to 90%, 1uM SA9 was treated for 0.5h, and then incubated with 10ng / ml TNF-a for 2h. Fixation: 4% paraformaldehyde, 10min; blocking, goat serum working solution 100μL, 10min; primary antibody incubation: anti-p65 polyclonal antibody (Santa Cruz, C372) (1:75) 4℃, overnight; secondary antibody incubation: FITC Labeled goat anti-rabbit IgG (1:100), protected from light ...

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Abstract

The invention belongs to the field of medicines and particularly relates to the use of 1-erucic acyl-4-(3'-chloro-)benzylpiperazine in medicine of inhibition of vascular endothelial cell oxidative stress, inflammation and adhesion. The concrete structure of the compound is shown in the description. 1-erucic acyl-4-(3'-chloro-)benzylpiperazine has obvious effects on inhibiting oxidant stress generated by vascular endothelial cells and monocyte and adhering action and inflammation generating effect of the vascular endothelial cells, and can be used for preparing medicines for treating vascular diseases.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to the application of a compound 1-sinapinyl-4-(3'-Cl-)benzylpiperazine in pharmacy. Background technique [0002] Vascular endothelium is not only the barrier of blood vessels, but also an important endocrine organ. Maintain normal vascular function and blood flow status by producing and releasing various active substances. Factors such as oxidative stress and inflammatory response can lead to damage of endothelial cells, and then the adhesion of monocytes to endothelial cells can occur, thus causing a variety of vascular diseases. The injury of vascular endothelial cells is the main link of many vascular diseases. The key to preventing and treating vascular diseases is to protect the function of vascular endothelium. Therefore, the development of drugs to protect vascular endothelial function has become an important measure for the treatment of vascular diseases. At present, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61P9/14A61P39/06A61P29/00
Inventor 朱毅曾小耘
Owner SHANTOU UNIV MEDICAL COLLEGE
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