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Applicability of the OECD 455 in - vitro assay for determination of hERa agonistic activity of isoflavonoidsGramec, Darja, farmacevtka ...The Organisation for Economic Co-operation and Development (OECD)-validated transactivation assay using the human estrogen receptor alpha (hER [alpha]) Hela9903 cell line is used for activity ... evaluation of hER [alpha] agonists and antagonists. Due to many advantages, this assay is broadly used as an initial screening process. However, response significantly higher from that of 17- [beta] estradiol (E2) was observed with phytoestrogens for concentrations commonly above 1- [micro]M in previous studies. The main aim of this study was thus to ascertain the applicability of OECD protocol 455 for evaluation of estrogenic activity of natural flavonoids, including known phytoestrogens. The estrogenic activities of aglycones as well as of O-methylated and glycosylated flavonoids were evaluated. Supra-maximal luciferase activity was seen for most of the flavonoids tested at concentrations even below 1- [micro]M. hER [alpha]-mediated luciferase expression was confirmed with the competition assay specified in OECD protocol 455. However, at concentrations above 1- [micro]M, non-specific interactions were also observed. Instead of EC50 values, which could not be determined for most of the isoflavonoids tested, the concentrations corresponding to 10% (PC10) and 50% (PC50) of the maximum activity of the positive control, E2, were used for quantitative determination of estrogenic activities. Appropriate evaluation of the data obtained with the current OECD protocol 455 validated assay represents a valuable tool for initial screening of natural flavonoids for estrogenic activity.Source: Toxicology and applied pharmacology. - ISSN 0041-008X (Vol. 386, 2020, str. 1-9)Type of material - article, component partPublish date - 2020Language - englishCOBISS.SI-ID - 4851825
Author
Gramec, Darja, farmacevtka |
Tvrdý, Václav |
Kenda, Maša, farmacevtka |
Zega, Anamarija |
Pour, Milan |
Horký, Pavel |
Mladěnka, Přemysl |
Sollner Dolenc, Marija |
Peterlin-Mašič, Lucija
Topics
Flavonoidi |
flavonoid |
endocrine activity |
estrogenic effect |
OECD TG 455 |
endokrina aktivnost |
fitoestrogeni
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Author | Gramec, Darja, farmacevtka ... |
Title | Applicability of the OECD 455 in - vitro assay for determination of hERa agonistic activity of isoflavonoids |
Publication date | 2020-01-01 |
COBISS.SI-ID | 4851825 |
Publication version in repository | Publisher's version |
Publication licence | Unidentified |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Gramec, Darja, farmacevtka | 35432 |
Tvrdý, Václav | ![]() |
Kenda, Maša, farmacevtka | 39201 |
Zega, Anamarija | 18633 |
Pour, Milan | ![]() |
Horký, Pavel | ![]() |
Mladěnka, Přemysl | ![]() |
Sollner Dolenc, Marija | 08519 |
Peterlin-Mašič, Lucija | 19317 |
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