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10.1038/s41598-017-09655-7

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suck abstract from ncbi


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pmid28831201
      Sci+Rep 2017 ; 7 (1 ): 9153
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  • BHX, a novel pyrazoline derivative, inhibits breast cancer cell invasion by reversing the epithelial-mesenchymal transition and down-regulating Wnt/?-catenin signalling #MMPMID28831201
  • Bao H ; Zhang Q ; Zhu Z ; Xu H ; Ding F ; Wang M ; Du S ; Du Y ; Yan Z
  • Sci Rep 2017[Aug]; 7 (1 ): 9153 PMID28831201 show ga
  • The novel pyrazoline derivative, BHX, has recently been shown to exhibit potent anti-tumour activity by blocking the Wnt/?-catenin signalling pathway. However, its effect on breast cancer growth and invasion are unknown. Our results show that BHX suppresses MDA-MB-231 cell viability and colony formation in a dose-dependent manner, and induces apoptosis and G0/G1 phase arrest. BHX-treated breast cancer cells showed morphological characteristics of cells undergoing apoptosis. Furthermore, BHX inhibited cell migration and invasion, which was associated with increased E-cadherin mRNA and protein expression, and down-regulation of SNAIL and vimentin. In addition, BHX induced the generation of intracellular ROS and decreased ?-catenin protein and mRNA expression. We used a mouse xenograft model to investigate the effects of BHX in vivo, where the growth of MDA-MB-231 xenografted tumours was suppressed in nude mice treated continuously with BHX for 21 days. Finally, the rat plasma concentration of BHX was measured by ultra-performance liquid-chromatography tandem mass spectrometry and the pharmacokinetic parameters of BHX were processed by non-compartmental analysis. In conclusion, BHX merits further study as a novel therapeutic small molecule for the treatment of breast cancer.
  • |*Down-Regulation [MESH]
  • |Animals [MESH]
  • |Antinematodal Agents/*administration & dosage/pharmacokinetics [MESH]
  • |Breast Neoplasms/*drug therapy/genetics/metabolism [MESH]
  • |Cell Line, Tumor [MESH]
  • |Cell Movement/drug effects [MESH]
  • |Cell Proliferation/drug effects [MESH]
  • |Cell Survival/drug effects [MESH]
  • |Dose-Response Relationship, Drug [MESH]
  • |Epithelial-Mesenchymal Transition/drug effects [MESH]
  • |Female [MESH]
  • |Gene Expression Regulation, Neoplastic/drug effects [MESH]
  • |Humans [MESH]
  • |Mice [MESH]
  • |Mice, Nude [MESH]
  • |Neoplasm Invasiveness [MESH]
  • |Pyrazoles/*administration & dosage/pharmacokinetics [MESH]
  • |Rats [MESH]
  • |Treatment Outcome [MESH]
  • |Wnt Signaling Pathway/*drug effects [MESH]


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