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Application of oxadiazole piperazine compounds in preparing anti-angiogenesis drug

An oxadiazolyl-piperazine and angiogenesis technology, applied in the field of medicine, can solve the problems of unpublished anti-angiogenesis research data, etc., and achieve inhibition of rat arterial ring microangiogenesis, inhibition of migration with resistance, and inhibition of endothelial cells The effect of microtubule formation

Active Publication Date: 2014-03-12
SHENYANG PHARMA UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the existing data did not disclose any research data on whether it has an anti-angiogenic effect

Method used

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  • Application of oxadiazole piperazine compounds in preparing anti-angiogenesis drug
  • Application of oxadiazole piperazine compounds in preparing anti-angiogenesis drug
  • Application of oxadiazole piperazine compounds in preparing anti-angiogenesis drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1. Effect of PAC-1 and WF-210 on VEGF-induced invasion ability of human umbilical vein endothelial cells (HUVEC)

[0024] 1.1 Materials

[0025] Primary HUVEC cells, culture medium, LSGS, and trypsin were purchased from Gibco, Transwell chambers were purchased from Corning, matrigel was purchased from BD, and calcein was purchased from Sigma.

[0026] 1.2 Experimental method

[0027] PAC-1 and WF-210 were dissolved in DMSO into 100mM stock solution and diluted with culture medium before use; HUVEC cells were cultured in an incubator with 5% CO2 and 37°C saturated humidity. The culture solution was mixed with 90% M200 basal medium and 2% LSGS, and sterilized by filtration through a 0.22 μm filter membrane. The Transwell chamber was coated with 1:8 Matrigel mixed with the culture medium, solidified at 37°C for 0.5 h, and then used for later use. Add 200 μl of VEGF-free culture medium to the upper chamber, 500 μl of VEGF-containing culture medium to the lower cha...

Embodiment 2

[0031] Example 2. Effects of PAC-1 and WF-210 on VEGF-induced tubule formation in human umbilical vein endothelial cells (HUVEC)

[0032] 2.1 Materials

[0033] Primary HUVEC cells, culture medium, LSGS, and trypsin were purchased from Gibco, 96-well plates were purchased from Corning, matrigel was purchased from BD, and calcein was purchased from Sigma.

[0034] 2.2 Method

[0035] PAC-1 and WF-210 were dissolved in DMSO into 100mM stock solution and diluted with culture medium before use; HUVEC cells were cultured in an incubator with 5% CO2 and 37°C saturated humidity. The culture solution was mixed with 90% M200 basal medium and 2% LSGS, and sterilized by filtration through a 0.22 μm filter membrane.

[0036] Add 1:1 Matrigel and culture medium to the 96-well plate, and add 100 μL of HUVEC cell suspension after 1 hour of coagulation at 37 degrees, with 15,000 cells per well. After 12 hours of culture, take pictures and observe. The VEGF stimulation concentration is 10 ng...

Embodiment 3

[0040] Example 3. Effect of PAC-1 and WF-210 on neovascularization of rat arterial ring

[0041] 3.1 Materials

[0042] Male SD rats aged 4-6 weeks were purchased from the Experimental Animal Center, culture medium and Hank’s solution were purchased from Gibco, 96-well plates were purchased from Corning, matrigel was purchased from BD, and calcein was purchased from Sigma.

[0043] 3.2 Method

[0044]PAC-1 and WF-210 were dissolved in DMSO into 100mM stock solution, and diluted with culture medium immediately before use. Take a section of blood vessel from the aortic arch to the renal artery of immature rats, wash it three times with Hank's solution, separate and remove the connective tissue, cut it into small pieces of 1-1.5 mm, and put it into 96 pieces containing 25 μl of solidified Matrigel (1:1). In the well plate, spread 25 μl Matrigel again, solidify at 37°C for more than 1 hour, add 50 μl culture medium, add VEGF and drug stimulation after culturing overnight, and ta...

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Abstract

The invention belongs to the technical field of medicine, and relates to an application of oxadiazole piperazine compounds in preparing an anti-angiogenesis drug. The two oxadiazole piperazine compounds are N'-(3-allyl-2-phenol methylene)-2-(4-benzyl piperazine-1-group) acethydrazide and (E)-N / -(4-((2-((benzo [d][1,3]dioxolane-5-group) methyl) thiazole-4-group) methoxy)-2-phenol methylene)-2-(4-((3-(4-((4-fluorobenzene oxygroup) methyl) phenyl)-1,2,4-oxadiazole-5-group) methyl) piperazine-1-group) acethydrazide hydrochloride. According to the application, the two oxadiazole piperazine compounds have obvious inhibiting effects on a human umbilical vein endothelial cell (HUVEC) microtubule forming experiment, a Transwell chamber migration experiment, a rat arterial ring experiment and the like, can obviously inhibit endothelial cell microtubule forming, can obviously inhibit resistive migration of an endothelial cell, and can obviously inhibit rat arterial ring capillary generation.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to two oxadiazolyl piperazine compounds and a pharmaceutical composition containing the compounds, which can be used as medicines for treating angiogenesis-related diseases. Background technique: [0002] Angiogenesis refers to the process of forming functional new blood vessels on the basis of original capillaries and / or venules through vascular endothelial cell proliferation, migration, adhesion, and vascular lumen formation; this process includes vascular endothelial cells and surrounding cells The interaction between extracellular matrix is ​​mainly regulated by angiogenesis-promoting factors and angiogenesis-inhibiting factors. Studies have found that a variety of growth factors such as vascular endothelial growth factor (VEGF), angiopoietin 2, basic fibroblast growth factor, and epidermal growth factor can regulate angiogenesis through different pathways. Under physiological ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P35/00A61P19/02A61P17/06A61P27/02A61P9/10A61P3/10A61P29/00A61K31/495
Inventor 吴春福宫平杨静玉王立辉赵燕芳王昉旸
Owner SHENYANG PHARMA UNIVERSITY
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