TY - JOUR
T1 - Comparative study of estrogen receptor α, β mRNA expressions of endometriosis and normal endometrium in women and analysis of potential synthetic anti-estrogens in silico
AU - Eldafira, Eldafira
AU - Abinawanto, Abinawanto
AU - Sjahfirdi, Luthfiralda
AU - Asmarinah, Asmarinah
AU - Soeharso, Purnomo
AU - Muharam, Muharam
AU - Prasasty, Vivitri D.
AU - Pujianto, Dwi A.
N1 - Funding Information:
The authors would like to thank Prof. Dr. Ichramsyah, Sp.OG (K), Prof. Dr. T.Z. Jakoeb, Sp.OG (KFER), Dr. R. Muharam, Sp.OG (K) who have been willing to provide an opportunity to help in the process of providing tissue samples from patients with endometriosis cases. this research was supported by personal funding and nonfinancial support from Department of Biology of Faculty of Mathematics and Natural Sciences; and Faculty of Medicine, Universitas Indonesia.
Funding Information:
Funding: this research was supported by personal funding and nonfinancial support from Department of Biology of Faculty of Mathematics and Natural Sciences; and Faculty of Medicine, Universitas Indonesia.
Publisher Copyright:
© E. Eldafira et al., 2018.
PY - 2018
Y1 - 2018
N2 - Endometriosis is a multifactorial disease in which genetic and environmental factors interact causing its pathogenesis. The aim of this study was to investigate the expression pattern of estrogen receptor a (ERα) and β (ERβ) in endometriosis patients compared to normal endometrioum (n=18) as a control by using Quantitative Real Time PCR method. Moreover, we also measured serum estradiol levels of endometriosis patients in the proliferation phase of the menstrual cycle using the enzyme-linked immunosorbent assay method. The mRNA expression of ERβ was significantly higher in the endometriosis group compared to control, and the result of t-test showed that were significantly different (P < 0.05). Overexpression of ERβ in endometriosis was likely to have other significant important impacts in the pathology of endometriosis that allowed ERβ to stimulate prostaglandin production in endometriosis tissue and cells. Estradiol content did not correlate with the ERα expression, and it is weakly correlated with ERβ mRNA expression. Molecular docking analysis showed that ERα and ERβ have different binding interactions with synthetic antiestrogens, whereas the best inhibitor was Ral2 to ERα and Aco1 to ERβ. Thus, both inhibitors could be used as leads in further investigation of ERα, ERβ inhibitory activities in vitro and in vivo.
AB - Endometriosis is a multifactorial disease in which genetic and environmental factors interact causing its pathogenesis. The aim of this study was to investigate the expression pattern of estrogen receptor a (ERα) and β (ERβ) in endometriosis patients compared to normal endometrioum (n=18) as a control by using Quantitative Real Time PCR method. Moreover, we also measured serum estradiol levels of endometriosis patients in the proliferation phase of the menstrual cycle using the enzyme-linked immunosorbent assay method. The mRNA expression of ERβ was significantly higher in the endometriosis group compared to control, and the result of t-test showed that were significantly different (P < 0.05). Overexpression of ERβ in endometriosis was likely to have other significant important impacts in the pathology of endometriosis that allowed ERβ to stimulate prostaglandin production in endometriosis tissue and cells. Estradiol content did not correlate with the ERα expression, and it is weakly correlated with ERβ mRNA expression. Molecular docking analysis showed that ERα and ERβ have different binding interactions with synthetic antiestrogens, whereas the best inhibitor was Ral2 to ERα and Aco1 to ERβ. Thus, both inhibitors could be used as leads in further investigation of ERα, ERβ inhibitory activities in vitro and in vivo.
KW - Antiestrogens
KW - Endometriosis
KW - Estrogen receptor
KW - MRNA expression
KW - Molecular docking
UR - http://www.scopus.com/inward/record.url?scp=85058160136&partnerID=8YFLogxK
U2 - 10.4081/jbr.2018.7550
DO - 10.4081/jbr.2018.7550
M3 - Article
AN - SCOPUS:85058160136
SN - 1826-8838
VL - 91
SP - 100
EP - 107
JO - Journal of Biological Research (Italy)
JF - Journal of Biological Research (Italy)
IS - 2
ER -