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The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen improve ANP levels and decrease nuclear translocation of NF-kB in estrogen-deficient rats.
Pharmacol Rep. 2017 Aug; 69(4):798-805.PR

Abstract

BACKGROUND

The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are used for the treatment of osteoporosis and cancer, respectively, in women. The impairment of both the Atrial Natriuretic Peptide (ANP) cell signaling system and the translocation of nuclear factor-kappa B (NF-kB) to the cell nucleus are associated with detrimental cardiovascular effects and inflammation. The effects of SERMs on these parameters in the cardiac tissue of estrogen-deficient rats has not been reported.

METHODS

We investigated the effects of raloxifene and tamoxifen on ANP signaling, p65 NF-kB nuclear translocation, cardiac histology and contractility. Female rats were divided into five groups: control (SHAM), ovariectomized (OVX), OVX-treated 17-β-estradiol (E), OVX-treated raloxifene (RLX) and OVX-treated tamoxifen (TAM). The treatments started 21days after ovariectomy and continued for 14days.

RESULTS

Ovariectomy reduced ANP mRNA in the left atrium (LA), decreased the content of ANP protein in the LA and in plasma, and increased the level of p65 NF-kB nuclear translocation in the left ventricle. Both 17-β-estradiol and SERMs were able to reverse these alterations, which were induced by the estrogen deficient state. The hemodynamic and cardiac structural parameters analyzed in the present work were not modified by the interventions.

CONCLUSIONS

Our study demonstrates, for the first time, the additional benefits of raloxifene and tamoxifen in an estrogen-deficient state. These include the normalization of plasmatic and cardiac ANP levels and cardiac p65 NF-kB translocation. Therefore, these treatments promote cardiovascular protection and may contribute to the prevention of cardiac dysfunction observed long-term in postmenopausal women.

Authors+Show Affiliations

Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil.Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil.Biological and Health Sciences, Federal Institute of Espirito Santo, Vila Velha, ES, Brazil.Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil.Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil.Department of Physiology and Biophysics, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil.Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil.Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil.Department of Pharmacy, University of Vila Velha, ES, Brazil.Department of Physiology and Biophysics, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil.Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil; Nucleus of Biotechnology, Federal University of Espirito Santo, Vitoria, ES, Brazil.Department of Physiological Sciences, Federal University of Espirito Santo, Vitória, ES, Brazil. Electronic address: nazarebissoli@gmail.com.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28591668

Citation

Lamas, Aline Z., et al. "The Selective Estrogen Receptor Modulators (SERMs) Raloxifene and Tamoxifen Improve ANP Levels and Decrease Nuclear Translocation of NF-kB in Estrogen-deficient Rats." Pharmacological Reports : PR, vol. 69, no. 4, 2017, pp. 798-805.
Lamas AZ, Nascimento AM, Medeiros ARS, et al. The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen improve ANP levels and decrease nuclear translocation of NF-kB in estrogen-deficient rats. Pharmacol Rep. 2017;69(4):798-805.
Lamas, A. Z., Nascimento, A. M., Medeiros, A. R. S., Caliman, I. F., Dalpiaz, P. L. M., Firmes, L. B., Sousa, G. J., Oliveira, P. W. C., Andrade, T. U., Reis, A. M., Gouvea, S. A., & Bissoli, N. S. (2017). The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen improve ANP levels and decrease nuclear translocation of NF-kB in estrogen-deficient rats. Pharmacological Reports : PR, 69(4), 798-805. https://doi.org/10.1016/j.pharep.2017.03.004
Lamas AZ, et al. The Selective Estrogen Receptor Modulators (SERMs) Raloxifene and Tamoxifen Improve ANP Levels and Decrease Nuclear Translocation of NF-kB in Estrogen-deficient Rats. Pharmacol Rep. 2017;69(4):798-805. PubMed PMID: 28591668.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen improve ANP levels and decrease nuclear translocation of NF-kB in estrogen-deficient rats. AU - Lamas,Aline Z, AU - Nascimento,Andrews M, AU - Medeiros,Ana Raquel S, AU - Caliman,Izabela F, AU - Dalpiaz,Polyana L M, AU - Firmes,Luciana B, AU - Sousa,Glauciene J, AU - Oliveira,Phablo Wendell C, AU - Andrade,Tadeu U, AU - Reis,Adelina M, AU - Gouvea,Sônia A, AU - Bissoli,Nazaré S, Y1 - 2017/03/16/ PY - 2016/10/18/received PY - 2017/01/27/revised PY - 2017/03/09/accepted PY - 2017/6/8/pubmed PY - 2018/5/10/medline PY - 2017/6/8/entrez KW - ANP KW - NF-kB KW - Ovariectomy KW - Raloxifene KW - SERMs KW - Tamoxifen SP - 798 EP - 805 JF - Pharmacological reports : PR JO - Pharmacol Rep VL - 69 IS - 4 N2 - BACKGROUND: The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are used for the treatment of osteoporosis and cancer, respectively, in women. The impairment of both the Atrial Natriuretic Peptide (ANP) cell signaling system and the translocation of nuclear factor-kappa B (NF-kB) to the cell nucleus are associated with detrimental cardiovascular effects and inflammation. The effects of SERMs on these parameters in the cardiac tissue of estrogen-deficient rats has not been reported. METHODS: We investigated the effects of raloxifene and tamoxifen on ANP signaling, p65 NF-kB nuclear translocation, cardiac histology and contractility. Female rats were divided into five groups: control (SHAM), ovariectomized (OVX), OVX-treated 17-β-estradiol (E), OVX-treated raloxifene (RLX) and OVX-treated tamoxifen (TAM). The treatments started 21days after ovariectomy and continued for 14days. RESULTS: Ovariectomy reduced ANP mRNA in the left atrium (LA), decreased the content of ANP protein in the LA and in plasma, and increased the level of p65 NF-kB nuclear translocation in the left ventricle. Both 17-β-estradiol and SERMs were able to reverse these alterations, which were induced by the estrogen deficient state. The hemodynamic and cardiac structural parameters analyzed in the present work were not modified by the interventions. CONCLUSIONS: Our study demonstrates, for the first time, the additional benefits of raloxifene and tamoxifen in an estrogen-deficient state. These include the normalization of plasmatic and cardiac ANP levels and cardiac p65 NF-kB translocation. Therefore, these treatments promote cardiovascular protection and may contribute to the prevention of cardiac dysfunction observed long-term in postmenopausal women. SN - 1734-1140 UR - https://www.unboundmedicine.com/medline/citation/28591668/The_selective_estrogen_receptor_modulators__SERMs__raloxifene_and_tamoxifen_improve_ANP_levels_and_decrease_nuclear_translocation_of_NF_kB_in_estrogen_deficient_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1734-1140(16)30282-1 DB - PRIME DP - Unbound Medicine ER -