Abstract
Background: 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. Methods: 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. Results: Cajanus cajan (Fabaceae), Abarema cochliacarpus (Fabaceae), and Borreria verticillata (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, C. cajans exerted the highest positive modulation on TR, causing an activation of 59.9%, while B. verticillata and A. cochliacarpus caused 30.8% and 23.3%, respectively. Conclusions: Our results contribute towards the validation of the traditional use of C. cajans, B. verticillata, and A. cochliacarpus 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.
Highlights
Nuclear receptors (NRs) are proteins that form a superfamily of eukaryotic transcription factors; their function is dependent on ligand binding, and they are evolutionarily correlated
Starting from surveys conducted in both Pataxó indigenous and Salvador communities, Bahia state, Brazil [17,18], this study selected twenty plants indicated for the treatment of metabolic disorders
All ethanol extracts were assessed for the estrogen receptor (ER) activation through the corresponding reporter gene-assay, and only the most active ones were subjected to the thyroid receptor (TR) activation assay
Summary
Nuclear receptors (NRs) are proteins that form a superfamily of eukaryotic transcription factors; their function is dependent on ligand binding, and they are evolutionarily correlated The relevance of this group of proteins in metabolic disease is shown by numerous synthetic ligands used in the clinic or under exploratory development for the treatment of diabetes mellitus, dyslipidemia, hypercholesterolemia, or other metabolic abnormalities [1]. Thyroid hormone receptors (TRs) are disseminated by various organs in the human body They are mainly expressed in the liver, pituitary, inner ear, retina, and several brain areas, playing an important role in growth, development and differentiation, as well as in the regulation of key metabolic processes, such as lipogenesis, lipolysis, and thermogenesis [7,8,9]. Conclusions: Our results contribute towards the validation of the traditional use of
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
