In Vitro Bioactivation of a Selective Estrogen Receptor Modulator (2S,3R)-(+)-3-(3-Hydroxyphenyl)-2-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-6-ol (I) in Liver Microsomes: Formation of Adenine Adducts

2012 ◽  
Vol 25 (11) ◽  
pp. 2368-2377 ◽  
Author(s):  
Ying Li ◽  
George A. Doss ◽  
Yan Li ◽  
Qing Chen ◽  
Wei Tang ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Liver Microsomes ◽  
Selective Estrogen Receptor Modulator ◽  
Receptor Modulator ◽  
Adenine Adducts

The selective estrogen receptor modulator raloxifene regulates osteoclast and osteoblast activity in vitro

Bone ◽  
2002 ◽  
Vol 30 (2) ◽  
pp. 368-376 ◽  
Author(s):  
A Taranta ◽  
M Brama ◽  
A Teti ◽  
V De luca ◽  
R Scandurra ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Selective Estrogen Receptor Modulator ◽  
Receptor Modulator ◽  
Osteoblast Activity

scholarly journals Selective estrogen receptor modulator BC-1 activates antioxidant signaling pathway in vitro via formation of reactive metabolites

2013 ◽  
Vol 34 (3) ◽  
pp. 373-379
Author(s):  
Bo-lan Yu ◽  
Zi-xin Mai ◽  
Xu-xiang Liu ◽  
Zhao-feng Huang
Keyword(s):  
Estrogen Receptor ◽  
Signaling Pathway ◽  
Selective Estrogen Receptor Modulator ◽  
Reactive Metabolites ◽  
Receptor Modulator

scholarly journals Concentration-dependent effects of a selective estrogen receptor modulator raloxifene on proliferation and apoptosis in human uterine leiomyoma cells cultured in vitro

2007 ◽  
Vol 22 (5) ◽  
pp. 1253-1259 ◽  
Author(s):  
Jin Liu ◽  
Hiroya Matsuo ◽  
Qin Xu ◽  
Wei Chen ◽  
Jiayin Wang ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Uterine Leiomyoma ◽  
Selective Estrogen Receptor Modulator ◽  
Receptor Modulator ◽  
Proliferation And Apoptosis ◽  
Cells Cultured

Abstract 320: Selective Estrogen Receptor Modulator Retards Arterial Senescence and Atherosclerosis via Upregulation of Sirt-1 and Autophagy in Post-menopause Model Mouse

2015 ◽  
Vol 117 (suppl_1) ◽  
Author(s):  
Yoshiyuki Ikeda ◽  
Takahiro Miyauchi ◽  
Masaaki Iwabayashi ◽  
Yuichi Akasaki ◽  
Yuichi Sasaki ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Selective Estrogen Receptor Modulator ◽  
Sham Operation ◽  
Receptor Modulator ◽  
Molecular Biological Analysis ◽  
Atherosclerotic Lesions ◽  
Protein Expressions ◽  
Model Mouse ◽  
Pai 1

Background: Incidence of cardiovascular disease (CVD) increases with development of arterial senescence and atherosclerosis, which are accelerated after menopause in women. This study aims 1) to clarify the mechanism of which post-menopose facilitates arterial senescence and atherosclerosis, and 2) to develop optical treatment. Methods and results: Female Apolipoprotein E deficient (ApoE KO) mice underwent ovariectomy at 8 weeks old were used as post-menopausal model mice (PM). Age-matched female mice with sham operation were used as control (Ctr). We confirmed that serum estrogen concentration was significantly lower in PM than in Ctr. Twelve weeks after surgery, aortas were harvested to examine molecular biological analysis. Sirt-1 and the ratio of LC3II/LC3I protein expressions were significantly lower in PM than in Ctr. Ratio of senescence associated β galactosidase (SA-β Gal) positive cells and expressions of acetyl (Ac)-p53, p21, and PAI-1 were significantly higher in PM than in Ctr. Aortic atherosclerotic lesions assessed by Oil Red O staining was significantly greater in PM than in Ctr. Overexpression of either Sirt-1 or autophagy retarded arterial senescence in vitro. These results suggest that ovariectomy accelerates arterial senescence and atherosclerotic development through downregulation of Sirt-1 and autophagy. Next, we administrated selective estrogen receptor modulator (SERM) to PM mice. Sirt-1 and the ratio of LC3II/LC3I protein expression were significantly higher in SERM-treated PM mice than in untreated mice. Ratio of SA-β Gal positive cells, protein expressions of Ac-p53, p21, and PAI-1, and aortic atherosclerotic lesions were significantly lower in SERM-treated PM mice than in untreated mice. The effect of SERM on augmentation of autophagy and inhibition of arterial senescence and atherosclerotic development was attenuated by administration of sirtinol, Sirt-1 inhibitor. Conclusion: SERM retards development of arterial senescence and atherosclerosis by activation of Sirt-1 and autophagy in postmenopause mice.

Effects of the selective estrogen receptor modulator LY117018 on growth hormone secretion: in vitro studies

Metabolism ◽  
2004 ◽  
Vol 53 (5) ◽  
pp. 563-570 ◽  
Author(s):  
G Tulipano ◽  
C Bonfanti ◽  
C Poiesi ◽  
A Burattin ◽  
S Turazzi ◽  
...  
Keyword(s):  
Growth Hormone ◽  
Estrogen Receptor ◽  
Hormone Secretion ◽  
Growth Hormone Secretion ◽  
Selective Estrogen Receptor Modulator ◽  
In Vitro Studies ◽  
Receptor Modulator

721: Raloxifene, a Selective Estrogen Receptor Modulator, Induces Apoptosis in Bladder Cancer Cell Lines

2004 ◽  
Vol 171 (4S) ◽  
pp. 191-192 ◽  
Author(s):  
Isaac Y. Kim ◽  
Jian Yu ◽  
Moses M. Kim ◽  
Seth P. Lerner
Keyword(s):  
Bladder Cancer ◽  
Estrogen Receptor ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Selective Estrogen Receptor Modulator ◽  
Bladder Cancer Cell ◽  
Receptor Modulator

scholarly journals Selective estrogen receptor modulator lasofoxifene suppresses spondyloarthritis manifestation and affects characteristics of gut microbiota in zymosan-induced SKG mice

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Hyemin Jeong ◽  
In Young Kim ◽  
Eun-Kyung Bae ◽  
Chan Hong Jeon ◽  
Kwang-Sung Ahn ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Gut Microbiota ◽  
Small Animal ◽  
Joint Inflammation ◽  
Fecal Calprotectin ◽  
Selective Estrogen Receptor Modulator ◽  
Mineral Density ◽  
Receptor Modulator ◽  
Significant Difference ◽  
Microbiota Diversity

AbstractAnkylosing spondylitis is a male-predominant disease and previous study revealed that estrogens have an anti-inflammatory effect on the spondyloarthritis (SpA) manifestations in zymosan-induced SKG mice. This study aimed to evaluate the effect of selective estrogen receptor modulator (SERM) lasofoxifene (Laso) on disease activity of SpA. Mice were randomized into zymosan-treated, zymosan + 17β-estradiol (E2)-treated, and zymosan + Laso-treated groups. Arthritis was assessed by 18F-fluorodeoxyglucose (18F-FDG) small-animal positron emission tomography/computed tomography and bone mineral density (BMD) was measured. Fecal samples were collected and 16S ribosomal RNA gene sequencing was used to determine gut microbiota differences. Both zymosan + E2-treated mice and zymosan + Laso-treated mice showed lower arthritis clinical scores and lower 18F-FDG uptake than zymosan-treated mice. BMD was significantly higher in zymosan + E2-treated mice and zymosan + Laso-treated mice than zymosan-treated mice, respectively. Fecal calprotectin levels were significantly elevated at 8 weeks after zymosan injection in zymosan-treated mice, but it was not significantly changed in zymosan + E2-treated mice and zymosan + Laso-treated mice. Gut microbiota diversity of zymosan-treated mice was significantly different from zymosan + E2-treated mice and zymosan + Laso-treated mice, respectively. There was no significant difference in gut microbiota diversity between zymosan + E2-treated mice and zymosan + Laso -treated mice. Laso inhibited joint inflammation and enhanced BMD in SKG mice, a model of SpA. Laso also affected the composition and biodiversity of gut microbiota. This study provides new knowledge regarding that selected SpA patients could benefit from SERM treatment.

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