Document Detail

Anti-implantation effect of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H-benzo(b)pyran, a potent antiestrogenic agent in rats.
MedLine Citation:
PMID:  20674906     Owner:  NLM     Status:  In-Data-Review    
OBJECTIVE: To investigate the anti-implantation effect and hormonal profile of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H-benzo(b)pyran (K-1) in rats.
DESIGN: In vivo assays for anti-implantation activity were performed in pregnant rats. Assays for estrogenicity/antiesrogenicity were performed in immature ovariectomized female rats. In vitro competitive binding of K-1 to human recombinant ERα, transient transfection assay using ERE-luciferase reporter, and alkaline phosphatase (ALP) activity as a measure of estrogenicity and/antiestrogenicity in human endometrial carcinoma cells were performed.
SETTING: Research laboratory.
ANIMAL(S): Adult female rats for anti-implantation activity, immature ovariectomized female rats, and immature castrated/intact male rats.
MAIN OUTCOME MEASURE(S): Number of implantations, uterine growth, luciferase reporter activity, ER binding affinity, and ALP activity.
RESULT(S): Compound K-1 given orally for 1-7 days post coitum at the dose of 100 μg/kg body weight prevented pregnancy in 100% of rats. K-1 was a potent antiestrogenic, and at 50 μg/kg, it could inhibit the effect of 1 μg E(2) in immature rats. Compound was devoid of uterotrophic, androgenic, or antigonadotropic activity. A high affinity binding to ERα was displayed by K-1, with a relative binding affinity of 5% of E(2). In human endometrial carcinoma cells, K-1 did not induce ERα-mediated transcriptional activation that is measured as luciferase reporter activity. K-1 antagonized the E-induced transcriptional activation significantly. K-1 also antagonized E-induced ALP activity in human endometrial cells.
CONCLUSION(S): K-1 appeared to exert its antifertility action by virtue of its strong antiestrogenic activity.
Geetika Kharkwal; Iram Fatima; Shakti Kitchlu; Bishambhar Singh; Kanchan Hajela; Anila Dwivedi
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Publication Detail:
Type:  Journal Article     Date:  2010-08-01
Journal Detail:
Title:  Fertility and sterility     Volume:  95     ISSN:  1556-5653     ISO Abbreviation:  Fertil. Steril.     Publication Date:  2011 Mar 
Date Detail:
Created Date:  2011-03-07     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0372772     Medline TA:  Fertil Steril     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1322-7     Citation Subset:  IM    
Copyright Information:
Copyright © 2011 American Society for Reproductive Medicine. Published by Elsevier Inc. All rights reserved.
Division of Endocrinology, Central Drug Research Institute, Central Drug Research Institute, Council of Scientific and Industrial Research, Lucknow, Uttar Pradesh, India.
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