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

Oleh:

Kharkwal, Geetika ; Fatima, Iram ; Kitchlu, Shakti ; Singh, Bishambhar ; Hajela, Kanchan ; Dwivedi, Anila

Jenis: Article from Journal - ilmiah internasional
Dalam koleksi: Fertility and Sterility (keterangan: ada di ClinicalKey) vol. 95 no. 04 (Mar. 2011), page 1322-1327.
Topik: Antiestrogen; implantation; estrogen receptor; uterus

Ketersediaan

Perpustakaan FK Nomor Panggil: F02.K.2011.03 Non-tandon: 1 (dapat dipinjam: 0) Tandon: tidak ada

Lihat Detail Induk

Isi artikel

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 ERa, 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 E2 in immature rats. Compound was devoid of uterotrophic, androgenic, or antigonadotropic activity. A high affinity binding to ERa was displayed by K-1, with a relative binding affinity of 5% of E2. In human endometrial carcinoma cells, K-1 did not induce ERa-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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