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Anti-implantation effect of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H- benzo(b)pyran, a potent antiestrogenic agent in rats  Geetika Kharkwal,

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Presentation on theme: "Anti-implantation effect of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H- benzo(b)pyran, a potent antiestrogenic agent in rats  Geetika Kharkwal,"— Presentation transcript:

1 Anti-implantation effect of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H- benzo(b)pyran, a potent antiestrogenic agent in rats  Geetika Kharkwal, Ph.D., Iram Fatima, M.Sc., Shakti Kitchlu, M.Sc., Bishambhar Singh, M.Sc., Kanchan Hajela, Ph.D., Anila Dwivedi, Ph.D.  Fertility and Sterility  Volume 95, Issue 4, Pages (March 2011) DOI: /j.fertnstert Copyright © 2011 American Society for Reproductive Medicine Terms and Conditions

2 Figure 1 (A) Chemical structure of compound K-1. (B) Uterine weight gain in immature ovariectomized rats treated with E2 (10 μg/kg) or K-1 at various doses for 3 days. Details are given in the Materials and Methods section. P-values vs. control: (a) P<.001; (b) P>.05; n = 6 per group. (C) Uterine wet weight of immature rats treated with K-1 along with E2 for 3 consecutive days. Details are given in the Materials and Methods section. P-values vs. control: (a) P<.001; (b) P>.05; n = 6 per group. Fertility and Sterility  , DOI: ( /j.fertnstert ) Copyright © 2011 American Society for Reproductive Medicine Terms and Conditions

3 Figure 2 (A) Competitive binding curve of K-1 (●) and E2 (■) to human ERα. 3H-E2 binding was determined by charcoal adsorption assay at 4°C as given in the Materials and Methods section. Data are the mean of three observations. (B) Transcriptional activation of the reporter (luciferase) gene by ERα in response to K-1 alone for agonistic activity, and in the presence of 10 nM E2 for antagonistic activity. Ishikawa cells were cotransfected with expression vectors for ERα and luciferase reporter gene and incubated with various concentrations of compounds for 24 hours. Details are given in the Materials and Methods section. Normalized relative luciferase unit (RLU) values are expressed as a percentage of ERα in response to E2. Values represent the mean ± SE of three or more independent experiments. P-values vs. control: (a) P<.001; (b) P>.05. (C and D) Effect of K-1 on ALP stimulation by K-1. Ishikawa cells were incubated with 10 nM E2 or compound K-1 at various doses (C) and E2 + compound K-1 at various doses (D) for 48 hours. Details are given in the Materials and Methods section. The results are mean ± SE of four replicates. P-values vs. control: (a) P<.001; (b) P<.01; (c) P<.05; (d) P>.05. Fertility and Sterility  , DOI: ( /j.fertnstert ) Copyright © 2011 American Society for Reproductive Medicine Terms and Conditions


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