Evaluation of the suitability of recombinant yeast-based estrogenicity assays as a pre-screening tool in environmental samples

Brix, Rikke; Noguerol, Tania-Noelia; Piña, Benjamı́n; Balaam, Jan; Nilsen, Anja Julie; Tollefsen, Knut Erik; Levy, Walkiria; Schramm, Karl‐Werner; Barceló, Damià

doi:10.1016/j.envint.2010.02.004

Cited by 24 publications

(8 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The estrogenic activity of nemorosone, evaluated by the recombinant yeast assay (RYA) based on vertebrate estrogen receptors, is a convenient measure of the potential for endocrine disruption of a substance or an environmental sample (Garcia-Reyero et al, 2005;Brix et al, 2010). This assay makes use of an engineered yeast strain that harbors two foreign genetic elements: a vertebrate receptor, in this case, a human estrogen receptor, ER, and a reporter gene whose expression is made dependent on the presence of estrogens and whose final product concentration is easy to measure.…”

Section: Resultsmentioning

confidence: 99%

“…In recent years, endocrine disrupting chemicals (EDC) have become a major issue in the field of environmental science, owing to their ability to interact with human estrogen receptors, thus interfering with the endocrine system (Crews et al, 2000;Brix et al, 2010). Epidemiological studies and animal experiments have shown that estrogen can have carcinogenic properties.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Assessment of estrogenic, mutagenic and antimutagenic activity of nemorosone

Camargo¹,

Varela²,

Oliveira³

et al. 2011

Rev. bras. farmacogn.

View full text Add to dashboard Cite

Currently, a wide range of research involving natural products is focused on the discovery of new drugs in many different therapeutic areas. A great number of the synthetic compounds on the market were derived from natural products, especially plants. Nemorosone is the major constituent of the floral resin of Clusia rosea Jacq., Clusiaceae, and in Cuban propolis. In vitro studies have shown cytotoxic activity in this substance against various tumor cell lines, including those resistant to various cytotoxic drugs, whereas it has low cytotoxicity to non-tumoral cells. Therefore, in order to characterize the biological activity of nemorosone, a substance with potential antitumor activity, and in view of preclinical testing of the toxicity of drug candidate compounds, the main aim of this study was to determine the mutagenic and antimutagenic activity of nemorosone by the Ames test, using the strains TA97a, TA98, TA100 and TA102 of Salmonella typhimurium. Secondly, to characterize the estrogenic activity in an experimental recombinant yeast model (Recombinant Yeast Assay) mutagenic activity was observed at in any of the concentrations in any of the test strains. To evaluate the antimutagenic potential, direct and indirect mutagenic agents were used: 4 nitro-o-phenylenediamine (NPD), mitomycin C (MMC) and aflatoxin B1 (AFL). Nemorosone showed moderate antimutagenic activity (inhibition level 31%), in strain TA100 in the presence of AFL, and strong antimutagenic activity in TA102 against MMC (inhibition level 53%). Estrogenic activity was observed, with an EEq of 0.41±0.16 nM at various tested concentrations.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Assessment of estrogenic, mutagenic and antimutagenic activity of nemorosone

Camargo¹,

Varela²,

Oliveira³

et al. 2011

Rev. bras. farmacogn.

View full text Add to dashboard Cite

show abstract

“…Apparent EC 50 values for each sample (a minimum of two replicas with at least four points each) were calculated using standard non-linear regression methods. These values were converted to EEQ by assuming they correspond to the EC 50 of estradiol [22], 7.29 × 10 -9 g/mL in our assay. Three independent experiments were done with the compounds, all of them in triplicate.…”

Section: Methodsmentioning

confidence: 99%

Estrogenic and mutagenic activities of Crotalaria pallida measured by recombinant yeast assay and Ames test

Boldrin

Resende

Höhne

et al. 2013

BMC Complement Altern Med

View full text Add to dashboard Cite

BackgroundCrotalaria pallida Ailton is a plant belonging to the Fabaceae family, popularly known as “rattle or rattlesnake” and used in traditional medicine to treat swelling of the joints and as a vermifuge. Previous pharmacological studies have also reported anti-inflammatory, antimicrobial and antifungal activities. Nevertheless, scientific information regarding this species is scarce, and there are no reports related to its possible estrogenic and mutagenic effects. Thus, the purpose of the present study was to investigate the estrogenic potential of C. pallida leaves by means of the Recombinant Yeast Assay (RYA), seeking an alternative for estrogen replacement therapy during menopause; and to reflect on the safe use of natural products to assess the mutagenic activity of the crude extract from C. pallida leaves, the dichloromethane fraction and stigmasterol by means of the Ames test.MethodsThe recombinant yeast assay with the strain BY4741 of Saccharomyces cerevisiae, was performed with the ethanolic extract, dichloromethane fraction and stigmasterol isolated from the leaves of C. pallida. Mutagenic activity was evaluated by the Salmonella/microsome assay (Ames test), using the Salmonella typhimurium tester strains TA100, TA98, TA97 and TA102, with (+S9) and without (-S9) metabolization, by the preincubation method.ResultsAll samples showed estrogenic activity, mainly stigmasterol. The ethanolic extract from C. pallida leaves showed mutagenic activity in the TA98 strain (-S9), whereas dichloromethane fraction and stigmasterol were found devoid of activity.ConclusionConsidering the excellent estrogenic activity performed by stigmasterol in the RYA associated with the absence of mutagenic activity when evaluated by the Ames test, stigmasterol becomes a strong candidate to be used in hormone replacement therapy during menopause.

show abstract

“…This is an especially harmful effect of chemical pollution that occurs when a chemical accumulates in an animal (or human) and affects its endocrine system. Given the multiple functions of hormones in the body, this alteration can lead to a variety of adverse effects, including hermaphroditism in fish and reproductive deficiencies in humans [1], [2].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Estrogenic Potential of Flavonoids Using a Recombinant Yeast Strain and MCF7/BUS Cell Proliferation Assay

et al. 2013

View full text Add to dashboard Cite

Phytoestrogens are of interest because of their reported beneficial effects on many human maladies including cancer, neurodegeneration, cardiovascular disease and diabetes. Furthermore, there is a search for compounds with estrogenic activity that can replace estrogen in hormone replacement therapy during menopause, without the undesirable effects of estrogen, such as the elevation of breast cancer occurrence. Thus, the principal objective of this study was to assess the estrogenic activity of flavonoids with different hydroxylation patterns: quercetin, kaempferol, luteolin, fisetin, chrysin, galangin, flavone, 3-hydroxyflavone, 5-hydroxyflavone and 7-hydroxyflavone via two different in vitro assays, the recombinant yeast assay (RYA) and the MCF-7 proliferation assay (E-screen), since the most potent phytoestrogens are members of the flavonoid family. In these assays, kaempferol was the only compound that showed ERα-dependent transcriptional activation activity by RYA, showing 6.74±1.7 nM EEQ, besides acting as a full agonist for the stimulation of proliferation of MCF-7/BUS cells. The other compounds did not show detectable levels of interaction with ER under the conditions used in the RYA. However, in the E-screen assay, compounds such as galangin, luteolin and fisetin also stimulated the proliferation of MCF-7/BUS cells, acting as partial agonists. In the evaluation of antiestrogenicity, the compounds quercetin, chrysin and 3-hydroxyflavone significantly inhibited the cell proliferation induced by 17-β-estradiol in the E-screen assay, indicating that these compounds may act as estrogen receptor antagonists. Overall, it became clear in the assay results that the estrogenic activity of flavonoids was affected by small structural differences such as the number of hydroxyl groups, especially those on the B ring of the flavonoid.

show abstract

Evaluation of the suitability of recombinant yeast-based estrogenicity assays as a pre-screening tool in environmental samples

Cited by 24 publications

References 33 publications

Assessment of estrogenic, mutagenic and antimutagenic activity of nemorosone

Assessment of estrogenic, mutagenic and antimutagenic activity of nemorosone

Estrogenic and mutagenic activities of Crotalaria pallida measured by recombinant yeast assay and Ames test

Evaluation of Estrogenic Potential of Flavonoids Using a Recombinant Yeast Strain and MCF7/BUS Cell Proliferation Assay

Contact Info

Product

Resources

About