小齿兔耳草氯仿提取物调节腔面乳腺癌细胞的雌激素和雄激素受体。

Arrabidaea chica chloroform extract modulates estrogen and androgen receptors on luminal breast cancer cells.

机构信息

Laboratory of Genetics and Biotechnology, Institute of Biotechnology, Federal University of Uberlandia, Rua Major Jerônimo, 566, Sala 601, Patos de Minas, MG, 38700-002, Brazil.

Laboratory of Cytogenetic and Mutagenesis, University Center of Patos de Minas, Patos de Minas, MG, Brazil.

出版信息

BMC Complement Med Ther. 2022 Jan 20;22(1):18. doi: 10.1186/s12906-022-03506-3.

DOI:10.1186/s12906-022-03506-3

PMID:35057779

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8773405/

Abstract

BACKGROUND

Breast Cancer (BC) is the most common cancer in women worldwide and, although 70% of patients are responsive to selective Estrogen Receptor (ER) modulators such as Tamoxifen (Tam), patients' survival is comprised by resistance to endocrine therapy. Brazilian flora, especially the Amazon biome, is one of the richest global sources of native species with potentially bioactive compounds. Arrabidaea chica is a plant native to the Amazon that has been used in the treatment of different diseases. However, its action on BC remains unclear.

METHODS

Herein the biological effects of the chloroform extract of A. chica (CEAC) were evaluated on BC cells and in in vivo model. After confirmation of CEAC antioxidant capacity, cells were treated with CEAC and Tam, alone and with CEAC+Tam. The cell viability was evaluated by MTT and hormone receptor transcripts levels were assessed (ESR1, ESR2 and AR). Finally, anticarcinogenicity of CEAC was recorded in Drosophila melanogaster through Epithelial Tumor Test (ETT).

RESULTS

The study confirmed the antioxidant activity of CEAC. CEAC was selective for MCF-7, downregulating ESR2 and AR transcripts and upregulating ESR2 expression. The modulatory effects of CEAC on ERs did not differ between cells treated with Tam and with CEAC+Tam. Interestingly, previous treatment with CEAC, followed by treatment with Tam promoted a significant decrease in cell viability. The extract also presented anticarcinogenic effect in in vivo assay.

CONCLUSION

The bioassays on breast tumor cells demonstrated the antiproliferative activity of the extract, which modulated the expression of hormone receptors and sensitized luminal tumor cells to Tam. These results suggest that CEAC could be a complementary treatment for BC.

摘要

背景

乳腺癌（BC）是全球女性最常见的癌症，尽管 70%的患者对选择性雌激素受体（ER）调节剂如他莫昔芬（Tam）有反应，但患者的生存仍因内分泌治疗耐药而受到影响。巴西植物群，特别是亚马逊生物群落，是全球具有潜在生物活性化合物的本地物种最丰富的来源之一。Arrabidaea chica 是一种原产于亚马逊的植物，已用于治疗不同的疾病。然而，它对 BC 的作用尚不清楚。

方法

在此，评估了 A. chica 的氯仿提取物（CEAC）对 BC 细胞和体内模型的生物学效应。在确认 CEAC 的抗氧化能力后，用 CEAC 和 Tam 单独和 CEAC+Tam 处理细胞。通过 MTT 评估细胞活力，并评估激素受体转录物水平（ESR1、ESR2 和 AR）。最后，通过上皮肿瘤测试（ETT）在果蝇中记录 CEAC 的抗癌作用。

结果

该研究证实了 CEAC 的抗氧化活性。CEAC 对 MCF-7 具有选择性，下调 ESR2 和 AR 转录物并上调 ESR2 表达。CEAC 对 ER 的调节作用在用 Tam 处理和用 CEAC+Tam 处理的细胞之间没有差异。有趣的是，先用 CEAC 处理，然后用 Tam 处理可显著降低细胞活力。该提取物在体内试验中也表现出抗癌作用。