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评价棕古巴胶中主要化合物Nemorosone 的雌激素、抗雌激素和遗传毒性活性。

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

机构信息

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

出版信息

BMC Complement Altern Med. 2013 Jul 31;13:201. doi: 10.1186/1472-6882-13-201.

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.

摘要

背景

棕褐蜂胶是古巴主要的蜂胶类型,其主要成分为 nemorosone,这是 Clusia rosea 花卉树脂的主要成分。由于其强大的体外抗癌作用,nemorosone 受到了越来越多的关注。已经报道了 nemorosone 在几种人类癌细胞系中的细胞毒性,并与它对雌激素受体 (ER) 的直接作用相关。可以用靶向雌激素介导的信号的药物治疗乳腺癌,例如抗雌激素。植物雌激素可以模拟或调节内源性雌激素的作用,用植物雌激素治疗乳腺癌可能是一种有效的策略,因为它们已经显示出抗癌活性。

方法

本研究的目的是通过重组酵母测定法 (RYA) 和 E-screen 测定法评估 nemorosone 与 ER 相互作用的能力,并通过彗星试验确定该化合物是否会引起肿瘤和非肿瘤乳腺细胞中的 DNA 损伤。

结果

nemorosone 没有表现出雌激素活性,但是当使用这两种方法中的任何一种时,它都抑制了 17-β-雌二醇 (E2) 的作用,显示出其抗雌激素特性。苯并二酮在癌细胞和正常乳腺细胞中诱导的 DNA 损伤呈阴性结果。

结论

这些发现表明,nemorosone 可能在治疗乳腺癌方面具有治疗应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e80/3733937/e3443d063ce0/1472-6882-13-201-1.jpg

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