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2017 ; 7
(1
): 9153
Nephropedia Template TP
gab.com Text
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English Wikipedia
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.