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Cytotoxic activity of nemorosone in human MCF-7 breast cancer cells.

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.

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  • Authors+Show Affiliations

    ,

    Department of Pharmaceutical Sciences, University of Salerno, Fisciano, Italy. apopolo@unisa.it

    , , , , , ,

    Source

    MeSH

    Antineoplastic Agents, Phytogenic
    Benzophenones
    Breast Neoplasms
    Calcium Signaling
    Cell Line, Tumor
    Cell Survival
    Clusia
    Cytotoxins
    Female
    Humans
    Plant Extracts

    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 -