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

机译:评价nemorosone(在棕色古巴蜂胶中发现的主要化合物)的雌激素,抗雌激素和遗传毒性活性

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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. © 2013 Camargo et al.; licensee BioMed Central Ltd.
机译:背景:棕色蜂胶是古巴发现的主要蜂胶。它的主要成分是Nemorosone,它是Clusia rosea花卉树脂的主要成分。 Nemorosone由于其强大的体外抗癌作用而受到越来越多的关注。据报道,nemorosone在几种人类癌细胞系中均具有毒性,并与它对雌激素受体(ER)的直接作用有关。可以用靶向雌激素介导的信号传导剂(例如抗雌激素)治疗乳腺癌。植物雌激素可以模拟或调节内源性雌激素的作用,并且由于植物雌激素已显示出抗癌活性,因此用植物雌激素治疗乳腺癌可能是一种有效策略。方法:本研究的目的是评估新孕酮与新孕酮相互作用的能力。 ERs,重组酵母测定(RYA)和E-screen测定以及通过彗星测定确定化合物是否导致肿瘤和非肿瘤乳腺细胞中的DNA损伤。结果:Nemorosone不具有雌激素活性,但是,当两种方法都使用时,它抑制了17-β-雌二醇(E2)的作用,显示了它们的抗雌激素性。二苯甲酮在癌症和正常乳腺细胞中引起的DNA损伤呈阴性结果。结论:这些发现表明,新孕酮可能在乳腺癌的治疗中具有治疗作用。 ©2013 Camargo等;被许可人BioMed Central Ltd.

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