Simple preparation and analysis of a phytoestrogen-rich extract of Pueraria candollei var. mirifica and its in vitro estrogenic activity

Despite the classical hormonal effect, estrogen has been reported to mediate neuroprotection in the brain, which leads to the searching of estrogen-like substances for treating neurodegenerative diseases. Flavonoids, a group of natural compounds, are well known to possess estrogenic effects and used to substitute estrogen, that is, phytoestrogen. Flavonoid serves as one of the potential targets for the development of natural supplements and therapeutic drugs against different diseases. The neuroprotection activity of flavonoids was chosen for a possible development of anti-Alzheimer's drugs or food supplements. The estrogenic activity of two flavonoids, baicalein and daidzein, were demonstrated by their strong abilities in stimulating estrogen receptor phosphorylation and transcriptional activation of estrogen responsive element in MCF-7 breast cells. The neuroprotection effects of flavonoids againstβ-amyloid (Aβ) were revealed by their inhibition effects onin vitroAβaggregation and Aβ-induced cytotoxicity in PC12 neuronal cells. More importantly, the estrogenic and neuroprotective activities of individual flavonoid could be further enhanced by the cotreatment in the cultures. Taken together, this synergistic effect of baicalein and daidzein might serve as a method to improve the therapeutic efficacy of different flavonoids against Aβ, which might be crucial in developing those flavonoidsin treating Alzheimer's disease in the future.

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In vitro estrogenic activity of representative endocrine disrupting chemicals mixtures at environmentally relevant concentrations

Chemosphere ◽

10.1016/j.chemosphere.2018.10.067 ◽

2019 ◽

Vol 215 ◽

pp. 396-403 ◽

Cited By ~ 10

Author(s):

Hui Yu ◽

Daniel J. Caldwell ◽

Rominder P. Suri

Keyword(s):

Estrogenic Activity ◽

Endocrine Disrupting Chemicals ◽

Endocrine Disrupting

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Evaluation of Estrogenic Activity of Wastewater: Comparison Among In Vitro ERα Reporter Gene Assay, In Vivo Vitellogenin Induction, and Chemical Analysis

Environmental Science & Technology ◽

10.1021/acs.est.5b01027 ◽

2015 ◽

Vol 49 (10) ◽

pp. 6319-6326 ◽

Cited By ~ 25

Author(s):

Masaru Ihara ◽

Tomokazu Kitamura ◽

Vimal Kumar ◽

Chang-Beom Park ◽

Mariko O. Ihara ◽

...

Keyword(s):

Chemical Analysis ◽

Reporter Gene ◽

Estrogenic Activity ◽

Reporter Gene Assay ◽

Gene Assay

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Estrogenic activity of multicyclic aromatic hydrocarbons in rainbow trout (Oncorhynchus mykiss) in vitro assays

Aquatic Toxicology ◽

10.1016/j.aquatox.2018.11.023 ◽

2019 ◽

Vol 207 ◽

pp. 43-51 ◽

Cited By ~ 2

Author(s):

Richard C. Kolanczyk ◽

Jeffrey S. Denny ◽

Barbara R. Sheedy ◽

Patricia K. Schmieder ◽

Mark A. Tapper

Keyword(s):

Rainbow Trout ◽

Oncorhynchus Mykiss ◽

Aromatic Hydrocarbons ◽

Estrogenic Activity ◽

In Vitro Assays ◽

Rainbow Trout Oncorhynchus Mykiss

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Biological Activity of Wastewater Assessed Using in Vitro Cell-Based Assays

10.21203/rs.3.rs-513231/v1 ◽

2021 ◽

Author(s):

Adamo R. Petosa ◽

Monica Nowierski ◽

Viviane Yargeau

Keyword(s):

Wastewater Treatment ◽

Wastewater Treatment Plants ◽

Estrogenic Activity ◽

Solid Phase ◽

Treated Wastewater ◽

Chemical Analyses ◽

Untreated Wastewater ◽

17Β Estradiol ◽

Receiving Waters

Abstract Bioanalytical tools, namely in vitro bioassays, can be employed in tandem with chemical analyses to assess the efficacy of wastewater treatment and the potential for adverse effects from the discharges of wastewater into receiving waters. In the present study, samples of untreated wastewater (i.e. influent) and treated wastewater (i.e. effluent) were collected from two wastewater treatment plants and a wastewater treatment lagoon serving municipalities in southern Ontario, Canada. In addition, grab samples of surface water were collected downstream of the lagoon discharge. After solid phase extraction (SPE) using ion-exchange columns for basic/neutral and acidic compounds, respectively, the extracts were analyzed for a suite of 16 indicator compounds. The two SPE extracts were combined for analysis of biological responses in four in vitro cell-based bioassays. The concentrations of several indicator compounds, including the estrogens, 17β-estradiol and 17α-ethinylestradiol, were below the limits of detection. However, androstenedione and estrone were detected in several influent samples. The concentrations of these steroid hormones and some of the other indicator compounds declined during treatment but acesulfame K, carbamazepine, trimethoprim and DEET persisted in the effluent. The MTS- CellTiter 96® AQueous One Solution Cell Proliferation Assay (MTS) indicated that cell viability was not affected by exposure to the extracts. The Qiagen Nuclear Receptors 10-Pathway Reporter Array indicated that several cellular pathways were upregulated, with the greatest upregulation observed with the estrogen receptor (i.e. induction ratios 12 to 47) and the liver X receptor (i.e. induction ratios 10 to 45). The ERα CALUX assay indicated that estrogenic activity was lower in effluents compared to influents, with the greatest estrogenic activity observed for grab samples of influent from the lagoon (i.e. 56-215 ng L-1 17β-estradiol equivalents). Finally, the results of the Nrf2 Luciferase Luminescence Assay indicated a lower oxidative stress in the effluent samples. Overall, the present study demonstrates that chemical analyses are limited in their ability to predict or explain reductions in the toxicity of treated wastewater. There are thus advantages to using a combination of chemical analyses and in vitro bioassays to monitor the treatment efficiency of wastewater treatment plants and to predict the potential impacts of wastewater discharges into receiving waters.

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Transformation of Pueraria candollei var. mirifica phytoestrogens using immobilized and free β-glucosidase, a technique for enhancing estrogenic activity

RSC Advances ◽

10.1039/d1ra05109a ◽

2021 ◽

Vol 11 (51) ◽

pp. 32067-32076

Author(s):

Fonthip Makkliang ◽

Wipawee Juengsanguanpornsuk ◽

Suppalak Phaisan ◽

Attapon Sakdamas ◽

Waraporn Putalun ◽

...

Keyword(s):

Estrogenic Activity ◽

Pueraria Candollei

Transformation of Pueraria candollei var. mirifica phytoestrogens by β-glucosidase increases estrogenic activity.

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Characterization and validation of fragment antigen-binding (Fab) antibody-based immunoassay for deoxymiroestrol, a potent phytoestrogen from Pueraria candollei

10.22541/au.161270515.50311593/v1 ◽

2021 ◽

Author(s):

Worapol Sae-foo ◽

Supaluk Krittanai ◽

Wipawee Juengsanguanpornsuk ◽

Gorawit Yusakul ◽

Tharita Kitisripanya ◽

...

Keyword(s):

Quantitative Method ◽

Estrogenic Activity ◽

Limit Of Detection ◽

Hormone Replacement ◽

Enzyme Linked Immunosorbent Assay ◽

Antigen Binding ◽

Pueraria Candollei ◽

Specific Determination ◽

Fragment Antigen Binding

Deoxymiroestrol is the most potent phytoestrogen in chromenes group that has been found in Pueraria candollei, Thai name known as Kwao Krua Khao. Several studies reported estrogenic activity of P. candollei in order to using as hormone replacement therapy for postmenopausal women. Previously, specific determination of deoxymiroestrol content by enzyme-linked immunosorbent assay (ELISA) using polyclonal antibody (pAb) have been reported. However, production of pAb has limitation and variability from different batches. Therefore, in this study, we established quantitative method for determination of deoxymiroestrol using fragment antigen-binding (Fab) antibody-based immunoassay. The developed immunoassay has specificity to deoxymiroestrol with a calibration range of 15.6-1000 ng mL-1. Precision including intra-assay and inter-assay are 1.48-7.11 and 0.58-9.31%, respectively. Accuracy of the assay showed in recovery between 99.77-101.61% when spike deoxymiroestrol standard into the samples. The limit of detection (LOD) is 30.80 ng mL-1. Comparation antibody-based immunoassay for determination of deoxymiroestrol using Fab with pAb was represented consistency (R2 = 0.9807) when analysis roots bark of Pueraria candollei from difference areas. Therefore, this development assay can apply to determine deoxymiroestrol content in the plant samples.

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Bisphenol A emission factors from industrial sources and elimination rates in a sewage treatment plant

Water Science & Technology ◽

10.2166/wst.2003.0553 ◽

2003 ◽

Vol 47 (10) ◽

pp. 117-122 ◽

Cited By ~ 23

Author(s):

M. Fuerhacker

Keyword(s):

Bisphenol A ◽

Estrogenic Activity ◽

Animal Experiments ◽

Elimination Rate ◽

Sewage Treatment Plant ◽

Treatment Plant ◽

Emission Factors ◽

Point Sources ◽

In Vitro Test

Bisphenol A (BPA) is widely used for the production of epoxy resins and polycarbonate plastics and is considered an endocrine disruptor. Special in vitro test systems and animal experiments showed a weak estrogenic activity. Aquatic wildlife especially could be endangered by waste water discharges. To manage possible risks arising from BPA emissions the major fluxes need to be investigated and the sources of the contamination of municipal treatment plants need to be determined. In this study, five major industrial point sources, two different household areas and the influent and effluent of the corresponding treatment plant (WWTP) were monitored simultaneously at a plant serving 120,000 population equivalents. A paper producing plant was the major BPA contributor to the influent load of the wastewater treatment plant. All the other emissions from point sources, including the two household areas, were considerably lower. The minimum elimination rate in the WTTP could be determined at 78% with an average of 89% of the total BPA-load. For a possible pollution-forecast, or for a comparison between different point sources, emission factors based on COD-emissions were calculated for industrial and household point sources at BPA/COD-ratios between 1.4 ×10−6-125×10−6 and 1.3×10−6-6.3×10−6, respectively.

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ADME/Tox Properties and Biochemical Interactions of Silybin Congeners: In silico Study

Natural Product Communications ◽

10.1177/1934578x1701200208 ◽

2017 ◽

Vol 12 (2) ◽

pp. 1934578X1701200 ◽

Cited By ~ 2

Author(s):

Antonia Diukendjieva ◽

Merilin Al Sharif ◽

Petko Alov ◽

Tania Pencheva ◽

Ivanka Tsakovska ◽

...

Keyword(s):

In Silico ◽

Estrogen Receptor Alpha ◽

Estrogenic Activity ◽

Qsar Model ◽

Quantitative Structure Activity Relationship ◽

Toxic Effects ◽

Active Constituent ◽

Main Component

Silymarin, the active constituent of Silybum marianum (milk thistle), and its main component, silybin, are products with well-known hepatoprotective, cytoprotective, antioxidant, and chemopreventative properties. Despite substantial in vitro and in vivo investigations of these flavonolignans, their mechanisms of action and potential toxic effects are not fully defined. In this study we explored important ADME/Tox properties and biochemical interactions of selected flavonolignans using in silico methods. A quantitative structure–activity relationship (QSAR) model based on data from a parallel artificial membrane permeability assay (PAMPA) was used to estimate bioavailability after oral administration. Toxic effects and metabolic transformations were predicted using the knowledge-based expert systems Derek Nexus and Meteor Nexus (Lhasa Ltd). Potential estrogenic activity of the studied silybin congeners was outlined. To address further the stereospecificity of this effect the stereoisomeric forms of silybin were docked into the ligand-binding domain of the human estrogen receptor alpha (ERα) (MOE software, CCG). According to our results both stereoisomers can be accommodated into the ERα active site, but different poses and interactions were observed for silybin A and silybin B.

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