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Cytotoxic activity of nemorosone in human MCF-7 breast cancer cells.
Can J Physiol Pharmacol 2011; 89(1):50-7CJ

Abstract

Estrogen receptor (ER) antagonists have been widely used for breast cancer treatment; however, patients have increasingly shown resistance and sensitivity to the high toxicity of these drugs, and identification of novel targeted therapies is therefore required. To determine whether nemorosone, a polycyclic polyisoprenylated benzophenone isolated from floral resins of Clusia rosea Jacq. and Cuban propolis samples, exerts anticancer effects on human breast cancer cells, estrogen receptor positive (ERα+) MCF-7 and estrogen receptor negative (ERα-) MDA-MB-231 and LNCaP cells were used. Cells were treated with nemorosone alone or in association with 17β-estradiol (E2) or an ER antagonist, ICI 182,780, a selective ER downregulator that completely abrogates estrogen-sensitive gene transcription. Nemorosone inhibited the cell viability of ERα+ but not of ERα- cells. In MCF-7, nemorosone induced inhibition of cell growth by blocking the cell cycle in the G₀/G₁ phase. Moreover, the expression of pERK1/2 and pAkt, considered to be hallmarks of the nongenomic estrogen signalling pathway, were reduced in MCF-7 cells treated with nemorosone. All these effects were enhanced by ICI 182,780. However, nemorosone was not able to interfere with E2-induced Ca²(+) release. These findings suggest that nemorosone may have therapeutic application in the treatment of breast cancer because of its activity on ERα.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, University of Salerno, Fisciano, Italy. apopolo@unisa.itNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21186377

Citation

Popolo, Ada, et al. "Cytotoxic Activity of Nemorosone in Human MCF-7 Breast Cancer Cells." Canadian Journal of Physiology and Pharmacology, vol. 89, no. 1, 2011, pp. 50-7.
Popolo A, Piccinelli AL, Morello S, et al. Cytotoxic activity of nemorosone in human MCF-7 breast cancer cells. Can J Physiol Pharmacol. 2011;89(1):50-7.
Popolo, A., Piccinelli, A. L., Morello, S., Sorrentino, R., Osmany, C. R., Rastrelli, L., ... Aldo, P. (2011). Cytotoxic activity of nemorosone in human MCF-7 breast cancer cells. Canadian Journal of Physiology and Pharmacology, 89(1), pp. 50-7. doi:10.1139/y10-100.
Popolo A, et al. Cytotoxic Activity of Nemorosone in Human MCF-7 Breast Cancer Cells. Can J Physiol Pharmacol. 2011;89(1):50-7. PubMed PMID: 21186377.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Cytotoxic activity of nemorosone in human MCF-7 breast cancer cells. AU - Popolo,Ada, AU - Piccinelli,Anna Lisa, AU - Morello,Silvana, AU - Sorrentino,Rosalinda, AU - Osmany,Cuesta Rubio, AU - Rastrelli,Luca, AU - Pinto,Aldo, AU - Aldo,Pinto, PY - 2010/12/28/entrez PY - 2010/12/28/pubmed PY - 2011/12/14/medline SP - 50 EP - 7 JF - Canadian journal of physiology and pharmacology JO - Can. J. Physiol. Pharmacol. VL - 89 IS - 1 N2 - Estrogen receptor (ER) antagonists have been widely used for breast cancer treatment; however, patients have increasingly shown resistance and sensitivity to the high toxicity of these drugs, and identification of novel targeted therapies is therefore required. To determine whether nemorosone, a polycyclic polyisoprenylated benzophenone isolated from floral resins of Clusia rosea Jacq. and Cuban propolis samples, exerts anticancer effects on human breast cancer cells, estrogen receptor positive (ERα+) MCF-7 and estrogen receptor negative (ERα-) MDA-MB-231 and LNCaP cells were used. Cells were treated with nemorosone alone or in association with 17β-estradiol (E2) or an ER antagonist, ICI 182,780, a selective ER downregulator that completely abrogates estrogen-sensitive gene transcription. Nemorosone inhibited the cell viability of ERα+ but not of ERα- cells. In MCF-7, nemorosone induced inhibition of cell growth by blocking the cell cycle in the G₀/G₁ phase. Moreover, the expression of pERK1/2 and pAkt, considered to be hallmarks of the nongenomic estrogen signalling pathway, were reduced in MCF-7 cells treated with nemorosone. All these effects were enhanced by ICI 182,780. However, nemorosone was not able to interfere with E2-induced Ca²(+) release. These findings suggest that nemorosone may have therapeutic application in the treatment of breast cancer because of its activity on ERα. SN - 1205-7541 UR - https://www.unboundmedicine.com/medline/citation/21186377/Cytotoxic_activity_of_nemorosone_in_human_MCF_7_breast_cancer_cells_ L2 - http://www.nrcresearchpress.com/doi/full/10.1139/y10-100?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -