The major in vivo effect of 17 beta-estradiol (17 beta E-2) on bone is the maintenance of bone mass by decreasing bone resorption, However, whether 17 beta E-2 affects osteoclast differentiation and/or function directly or through its action on osteoblasts is unclear. To investigate this question we examined a human pre-osteoclastic cell line (FLG 29.1) for evidence of functional estrogen receptors (ER), Binding of [H-3] 17 beta E-2 to nuclear ER was steroid-specific with approximately 400 saturable, high affinity (Kd similar to 1 nhl) binding sites per cell nucleus, Pretreatment with 17 beta E-2 induced Specific binding of progesterone to FGL 29.1 cells, In addition, stimulation of these cells with 10 nM and 100 nM of 17 beta E-2 significantly (p<0.005) reduced cell proliferation, These observations clearly indicate the presence of functional estrogen receptors in osteoclast precursors, Moreover using a cell-impermeant and fluorescent estrogen conjugate, 17 beta-estradiol-6-carboxymethyloxime-bovine serum albumin-fluorescein isothiocyanate, we demonstrated the presence of specific plasma membrane binding sites for 17 beta E-2. Stimulation of FLG 29.1 with 17 beta E-2 induced different rapid responses, thus suggesting a nongenomic action of 17 beta E-2 on osteoclast precursors. LY 139478 is a member of the non-steroidal antiestrogens, described to be full estrogen agonists in bone acting via an estrogen receptor mediated mechanism, To investigate the in vitro properties of LY 139478 on osteoclast precursors, the human pre-osteoclastic cell line FLG 29.1 was examined for evidence of bioeffects of this compound, We demonstrated that its mechanism of action is mediated through the binding to the estrogen receptor.

Becherini, L., Frediani, U., Gennari, L., Fiorelli, L., Tanini, A., Brandi, M.L. (1998). Role of estrogenic and antiestrogenic molecules in osteoclastogenesis. ITALIAN JOURNAL OF MINERAL & ELECTROLYTE METABOLISM, 11(1), 1-8.

Role of estrogenic and antiestrogenic molecules in osteoclastogenesis

Gennari L.;
1998-01-01

Abstract

The major in vivo effect of 17 beta-estradiol (17 beta E-2) on bone is the maintenance of bone mass by decreasing bone resorption, However, whether 17 beta E-2 affects osteoclast differentiation and/or function directly or through its action on osteoblasts is unclear. To investigate this question we examined a human pre-osteoclastic cell line (FLG 29.1) for evidence of functional estrogen receptors (ER), Binding of [H-3] 17 beta E-2 to nuclear ER was steroid-specific with approximately 400 saturable, high affinity (Kd similar to 1 nhl) binding sites per cell nucleus, Pretreatment with 17 beta E-2 induced Specific binding of progesterone to FGL 29.1 cells, In addition, stimulation of these cells with 10 nM and 100 nM of 17 beta E-2 significantly (p<0.005) reduced cell proliferation, These observations clearly indicate the presence of functional estrogen receptors in osteoclast precursors, Moreover using a cell-impermeant and fluorescent estrogen conjugate, 17 beta-estradiol-6-carboxymethyloxime-bovine serum albumin-fluorescein isothiocyanate, we demonstrated the presence of specific plasma membrane binding sites for 17 beta E-2. Stimulation of FLG 29.1 with 17 beta E-2 induced different rapid responses, thus suggesting a nongenomic action of 17 beta E-2 on osteoclast precursors. LY 139478 is a member of the non-steroidal antiestrogens, described to be full estrogen agonists in bone acting via an estrogen receptor mediated mechanism, To investigate the in vitro properties of LY 139478 on osteoclast precursors, the human pre-osteoclastic cell line FLG 29.1 was examined for evidence of bioeffects of this compound, We demonstrated that its mechanism of action is mediated through the binding to the estrogen receptor.
1998
Becherini, L., Frediani, U., Gennari, L., Fiorelli, L., Tanini, A., Brandi, M.L. (1998). Role of estrogenic and antiestrogenic molecules in osteoclastogenesis. ITALIAN JOURNAL OF MINERAL & ELECTROLYTE METABOLISM, 11(1), 1-8.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/21081
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