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

BMC Complementary and Alternative Medicine

Eliana A Varanda³  Osmany Cuesta-Rubio¹  Wagner Vilegas²  Nicolás Olea⁴  José Manuel Molina-Molina⁴  Mariana F Fernández⁴  Cassia RP Cardoso³  Paula K Boldrin³  Flavia A Resende³  Aline M Prieto³  Mariana S Camargo³ 

[1] Instituto de Farmacia y Alimentos (IFAL), Universidad de La Habana, La Habana, Cuba;UNESP- Univ. Estadual Paulista, Campus do Litoral Paulista, Unidade São Vicente, CEP 11330-900 São Vicente, São Paulo, Brazil;UNESP- Univ. Estadual Paulista, Faculty of Pharmaceutical Sciencies of Araraquara-Department of Biological Sciences, Rodovia Araraquara-Jaú, Km 1, 14801-902 Araraquara, São Paulo, Brazil;School of Pharmacy, University of Granada, Granada, Spain

关键词: Genotoxicity;    Estrogenicity;    Propolis;    Clusia rosea;    Nemorosone;   

Others  :  1221045
DOI  :  10.1186/1472-6882-13-201

 received in 2013-05-07, accepted in 2013-07-25,  发布年份 2013

【 摘 要 】

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.

【 授权许可】

   
2013 Camargo et al.; licensee BioMed Central Ltd.

【 图 表 】

Figure 1.

Figure 2.

Figure 3.

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