• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Drug Design, Development and Therapy >In vivo Screening of Natural Products Against Angiogenesis and Mechanisms of Anti-Angiogenic Activity of Deoxysappanone B 7,4?-Dimethyl Ether
【24h】

In vivo Screening of Natural Products Against Angiogenesis and Mechanisms of Anti-Angiogenic Activity of Deoxysappanone B 7,4?-Dimethyl Ether

机译：在脱雄肠酮B 7,4-二甲醚的抗血管生成活性血管生成和抗血管生成活性机制的体内筛选

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Introduction: The aim of this study was to screen the leading compounds of natural origin with anti-angiogenic potential and to investigate their anti-angiogenic mechanism preliminarily. Materials and Methods: An initial screening of 240 compounds from the Natural Products Collection of MicroSource was performed using the transgenic zebrafish strain Tg [fli1a: enhanced green fluorescent protein (EGFP)]y1 . The zebrafish embryos at 24 h post-fertilization were exposed to the natural compounds for an additional 24 h; then, morphological changes in the intersegmental vessels (ISVs) were observed and quantified under a fluorescence microscope. The expression profiles of angiogenesis-related genes in the zebrafish embryos were detected using quantitative real-time PCR. Results: Five compounds were identified with potential anti-angiogenic activity on the zebrafish embryogenesis. Among them, deoxysappanone B 7.4?-dimethyl ether (Deox B 7,4) showed anti-angiogenic activity on the formation of ISVs in a dose-dependent manner. The inhibition of ISV formation reached up to 99.64% at 5 μM Deox B 7,4. The expression of delta-like ligand 4 ( dll4 ), hes-related family basic helix-loop-helix transcription factor with YRPW motif 2, ephrin B2, fibroblast growth factor receptor ( fgfr ) 3, cyclooxygenase-2, protein tyrosine phosphatase, receptor type B ( ptp-rb ), phosphoinositide-3-kinase regulatory subunit 2, slit guidance ligand ( slit ) 2, slit3 , roundabout guidance receptor ( robo ) 1, robo2 , and robo4 were down-regulated, while vascular endothelial growth factor receptor-2, fgfr 1, and matrix metallopeptidase 9 were up-regulated in the zebrafish embryos treated with Deox B 7,4. Conclusion: Deox B 7,4 has a therapeutic potential for the treatment of angiogenesis-dependent diseases and may exert anti-angiogenic activities by suppressing the slit2/robo1/2, slit3/robo4, cox2/ptp-rb/pik3r2, and dll4/hey2/efnb2a signaling pathways as well as activation of vegfr-2/fgfr1/mmp9.
机译：介绍：本研究的目的是筛选抗血管生成潜力的天然原产地的主要化合物，并初步研究其抗血管生成机制。材料和方法：使用转基因斑马鱼菌株Tg [Fli1a：增强的绿色荧光蛋白（EGFP）] Y1，进行MicroSource的自然产品收集初始筛选240化合物。施肥后24小时的斑马鱼胚胎暴露于天然化合物，另外24小时;然后，在荧光显微镜下观察和定量体内血管（ISV）的形态变化。使用定量实时PCR检测斑马鱼胚胎中血管生成相关基因的表达谱。结果：在斑马鱼胚胎发生上鉴定出五种化合物，含有抗血管生成活性。其中，脱氧性化合物B 7.4-二甲醚（DEOX B 7,4）显示抗血管生成活性以剂量依赖性方式形成ISV。抑制ISV形成达到5μmDoOxB 7,4的含量高达99.64％。 δ状配体4（DLL4）的表达，HES相关的族碱性螺旋环 - 螺旋转录因子，具有YRPW基序2，ephrin B2，成纤维细胞生长因子受体（FGFR）3，环氧氧基酶-2，蛋白酪氨酸磷酸酶，受体B型（PTP-RB），磷酸阳性-3-激酶调节亚基2，狭缝引导配体（SLIT）2，SLIT3，环形交叉引导受体（ROBO）1，ROBO2和ROBO4被下调，而血管内皮生长因子受体-2，FGFR1和基质金属肽酶9在用DEOX B 7,4处理的斑马鱼胚中上调。结论：DEOX B 7,4具有治疗血管生成依赖性疾病的治疗潜力，并可通过抑制粘液2 / ROBO1 / 2，SLIT3 / ROBO4，COX2 / PTP-RB / PIK3R2和DLL4 /）发挥抗血管生成活性。 HEY2 / EFNB2A信令路径以及VEGFR-2 / FGFR1 / MMP9的激活。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号