| Anti-implantation effect of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H-benzo(b)pyran, a potent antiestrogenic agent in rats. | |
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MedLine Citation:
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PMID: 20674906 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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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. INTERVENTION(S): None. 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. |
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Authors:
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Geetika Kharkwal; Iram Fatima; Shakti Kitchlu; Bishambhar Singh; Kanchan Hajela; Anila Dwivedi |
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Publication Detail:
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Type: Journal Article Date: 2010-08-01 |
Journal Detail:
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Title: Fertility and sterility Volume: 95 ISSN: 1556-5653 ISO Abbreviation: Fertil. Steril. Publication Date: 2011 Mar |
Date Detail:
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Created Date: 2011-03-07 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0372772 Medline TA: Fertil Steril Country: United States |
Other Details:
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Languages: eng Pagination: 1322-7 Citation Subset: IM |
Copyright Information:
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Copyright © 2011 American Society for Reproductive Medicine. Published by Elsevier Inc. All rights reserved. |
Affiliation:
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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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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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