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Evaluation of estrogenic, antiestrogenic and genotoxic activity of nemorosone, the major compound found in brown Cuban propolis.

Abstract

BACKGROUND

Brown propolis is the major type of propolis found in Cuba; its principal component is nemorosone, the major constituent of Clusia rosea floral resins. Nemorosone has received increasing attention due to its strong in vitro anti-cancer action. The citotoxicity of nemorosone in several human cancer cell lines has been reported and correlated to the direct action it has on the estrogen receptor (ER). Breast cancer can be treated with agents that target estrogen-mediated signaling, such as antiestrogens. Phytoestrogen can mimic or modulate the actions of endogenous estrogens and the treatment of breast cancer with phytoestrogens may be a valid strategy, since they have shown anti-cancer activity.

METHODS

The aim of the present investigation was to assess the capacity of nemorosone to interact with ERs, by Recombinant Yeast Assay (RYA) and E-screen assays, and to determine by comet assay, if the compound causes DNA-damaging in tumoral and non-tumoral breast cells.

RESULTS

Nemorosone did not present estrogenic activity, however, it inhibited the 17-β-estradiol (E2) action when either of both methods was used, showing their antiestrogenicity. The DNA damage induced by the benzophenone in cancer and normal breast cells presented negative results.

CONCLUSION

These findings suggest that nemorosone may have therapeutic application in the treatment of breast cancer.

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  • Authors+Show Affiliations

    ,

    UNESP-University Estadual Paulista, Faculty of Pharmaceutical Sciencies of Araraquara-Department of Biological Sciences, Araraquara, São Paulo, Brazil.

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    Source

    MeSH

    Benzophenones
    Cell Line, Tumor
    Cell Proliferation
    Comet Assay
    Cuba
    DNA Damage
    Drug Evaluation, Preclinical
    Estrogen Antagonists
    Estrogens
    Humans
    Mass Spectrometry
    Mutagens
    Plant Extracts
    Propolis

    Pub Type(s)

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

    Language

    eng

    PubMed ID

    23902919

    Citation

    Camargo, Mariana S., et al. "Evaluation of Estrogenic, Antiestrogenic and Genotoxic Activity of Nemorosone, the Major Compound Found in Brown Cuban Propolis." BMC Complementary and Alternative Medicine, vol. 13, 2013, p. 201.
    Camargo MS, Prieto AM, Resende FA, et al. Evaluation of estrogenic, antiestrogenic and genotoxic activity of nemorosone, the major compound found in brown Cuban propolis. BMC Complement Altern Med. 2013;13:201.
    Camargo, M. S., Prieto, A. M., Resende, F. A., Boldrin, P. K., Cardoso, C. R., Fernández, M. F., ... Varanda, E. A. (2013). Evaluation of estrogenic, antiestrogenic and genotoxic activity of nemorosone, the major compound found in brown Cuban propolis. BMC Complementary and Alternative Medicine, 13, p. 201. doi:10.1186/1472-6882-13-201.
    Camargo MS, et al. Evaluation of Estrogenic, Antiestrogenic and Genotoxic Activity of Nemorosone, the Major Compound Found in Brown Cuban Propolis. BMC Complement Altern Med. 2013 Jul 31;13:201. PubMed PMID: 23902919.
    * Article titles in AMA citation format should be in sentence-case
    TY - JOUR T1 - Evaluation of estrogenic, antiestrogenic and genotoxic activity of nemorosone, the major compound found in brown Cuban propolis. AU - Camargo,Mariana S, AU - Prieto,Aline M, AU - Resende,Flavia A, AU - Boldrin,Paula K, AU - Cardoso,Cassia R P, AU - Fernández,Mariana F, AU - Molina-Molina,José Manuel, AU - Olea,Nicolás, AU - Vilegas,Wagner, AU - Cuesta-Rubio,Osmany, AU - Varanda,Eliana A, Y1 - 2013/07/31/ PY - 2013/05/07/received PY - 2013/07/25/accepted PY - 2013/8/2/entrez PY - 2013/8/2/pubmed PY - 2013/9/24/medline SP - 201 EP - 201 JF - BMC complementary and alternative medicine JO - BMC Complement Altern Med VL - 13 N2 - BACKGROUND: Brown propolis is the major type of propolis found in Cuba; its principal component is nemorosone, the major constituent of Clusia rosea floral resins. Nemorosone has received increasing attention due to its strong in vitro anti-cancer action. The citotoxicity of nemorosone in several human cancer cell lines has been reported and correlated to the direct action it has on the estrogen receptor (ER). Breast cancer can be treated with agents that target estrogen-mediated signaling, such as antiestrogens. Phytoestrogen can mimic or modulate the actions of endogenous estrogens and the treatment of breast cancer with phytoestrogens may be a valid strategy, since they have shown anti-cancer activity. METHODS: The aim of the present investigation was to assess the capacity of nemorosone to interact with ERs, by Recombinant Yeast Assay (RYA) and E-screen assays, and to determine by comet assay, if the compound causes DNA-damaging in tumoral and non-tumoral breast cells. RESULTS: Nemorosone did not present estrogenic activity, however, it inhibited the 17-β-estradiol (E2) action when either of both methods was used, showing their antiestrogenicity. The DNA damage induced by the benzophenone in cancer and normal breast cells presented negative results. CONCLUSION: These findings suggest that nemorosone may have therapeutic application in the treatment of breast cancer. SN - 1472-6882 UR - https://www.unboundmedicine.com/medline/citation/23902919/Evaluation_of_estrogenic_antiestrogenic_and_genotoxic_activity_of_nemorosone_the_major_compound_found_in_brown_Cuban_propolis_ L2 - https://bmccomplementalternmed.biomedcentral.com/articles/10.1186/1472-6882-13-201 DB - PRIME DP - Unbound Medicine ER -