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巴西巴伊亚药用植物对雌激素和甲状腺激素受体的激活作用

Estrogen and Thyroid Hormone Receptor Activation by Medicinal Plants from Bahia, Brazil.

作者信息

Reis Luã Tainã Costa, da Silva Magnus Régios Dias, Costa Silvia Lima, Velozo Eudes da Silva, Batista Ronan, da Cunha Lima Suzana Telles

机构信息

Laboratory of Bioprospection and Biotechnology (LaBBiotec), Institute of Biology, Federal University of Bahia (UFBA), Barão de Jeremoabo Street, 147-Ondina, Salvador, BA 40170-115, Brazil.

Laboratory of Molecular and Translational Endocrinology, Department of Medicine, Federal University of São Paulo (UNIFESP), R. Sena Madureira, 1500-Vila Clementino, São Paulo, SP 04021-001, Brazil.

出版信息

Medicines (Basel). 2018 Jan 15;5(1):8. doi: 10.3390/medicines5010008.

Abstract

: A number of medicinal plants are traditionally used for metabolic disorders in Bahia state, Brazil. The aim of this study was to evaluate the estrogen receptor (ER) and thyroid receptor (TR) activation of crude extracts prepared from 20 plants. : Species were extracted and assayed for receptor activation through both ER and TR gene-reporter assays, using 17β-estradiol and triiodothyronine (T3), respectively, as the positive controls. : (Fabaceae), (Fabaceae), and (Rubiaceae) were able to activate ER as much as the positive control (17β-estradiol). These three plant species were also assayed for TR activation. At the concentration of 50 µg/mL, exerted the highest positive modulation on TR, causing an activation of 59.9%, while and caused 30.8% and 23.3%, respectively. : Our results contribute towards the validation of the traditional use of , , and in the treatment of metabolic disorders related to ER and TR functions. The gene-reporter assay was proven effective in screening crude plant extracts for ER/TR activation, endorsing this methodology as an important tool for future bioprospection studies focused on identifying novel starting molecules for the development of estrogen and thyroid agonists.

摘要

在巴西巴伊亚州,许多药用植物传统上用于治疗代谢紊乱。本研究的目的是评估从20种植物中制备的粗提物对雌激素受体(ER)和甲状腺受体(TR)的激活作用。通过ER和TR基因报告试验分别使用17β-雌二醇和三碘甲状腺原氨酸(T3)作为阳性对照,对植物物种进行提取并检测其受体激活情况。(豆科)、(豆科)和(茜草科)能够与阳性对照(17β-雌二醇)一样激活ER。还对这三种植物物种进行了TR激活检测。在50μg/mL的浓度下,对TR的正向调节作用最强,激活率为59.9%,而和的激活率分别为30.8%和23.3%。我们的结果有助于验证、和在治疗与ER和TR功能相关的代谢紊乱方面的传统用途。基因报告试验被证明可有效筛选植物粗提物的ER/TR激活情况,支持将该方法作为未来生物勘探研究的重要工具,该研究专注于识别用于开发雌激素和甲状腺激动剂的新型起始分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/504c/5874573/da1031afbf37/medicines-05-00008-g001.jpg

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