Effects of PE on estrogen receptor expressions and its transcriptional activation on target genes / 中国药理学通报

ABSTRACT

Aim To investigate the effect of piperazinyl estrone(PE) on estrogen receptor expression and the transcriptional regulation of target genes.Methods Ovariectomized mice were given with PE in different doses (0.5 mg·kg~(-1),1 mg·kg~(-1),2 mg·kg~(-1))and estrone(0.71 mg·kg~(-1)) for 42 days,the protein expressions of Ers(Erαand Erβ)were shown by immunohistochemical method; To study transcriptional regulation of PE, PACT2-hERα and ERE2-TATA-LUC were co-transfected into MCF-7 cells by using Tfx 50 cationic liposome.Results Compared with ovx group, the groups with PE could up-regulate Ers of uteri in a dose-dependent manner,but its effect on Erα subtype was obvious.The classical ER signaling pathways could be activated by PE in co-transfected MCF-7 cells,but activation of PE was feebler than estrone with the same dose.Conclusion PE can up-regulate estrogen receptors in uteri. PE can transactivate ERE reportor gene through Erα and Erβ in MCF-7 cells, but its effect is feeble.