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At least 235 records · Page 13Linked to original sources
PubMed2000

A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation.

While searching for natural ligands for the peroxisome proliferator-activated receptor (PPAR) gamma, we identified a synthetic compound that binds to this receptor. Bisphenol A diglycidyl ether (BADGE) is a ligand for PPARgamma with a K(d(app)) of 100 microM. This compound has no apparent ability to activate the transcriptional activity of PPARgamma; however, BADGE can antagonize the ability of agonist ligands such as rosiglitazone to activate the transcriptional and adipogenic action of this receptor. BADGE also specifically blocks the ability of natural adipogenic cell lines such as 3T3-L1 and 3T3-F442A cells to undergo hormone-mediated cell differentiation. These results provide the first pharmacological evidence that PPARgamma activity is required for the hormonally induced differentiation of adipogenic cells.

1-Methyl-3-isobutylxanthine↗
PubMed2004

[Preliminary investigation on endocrine disrupting chemicals in a sewage treatment plant of Beijing].

Endocrine disrupting chemicals (EDCs) existed in the water treatment units of Beijing based Sewage Treatment Plant were analyzed by SPE-GC/MSD and GC/ECD. Totally 30 EDCs were detected from the influent, effluent and sludge. The results show that about 70%-99% EDCs in the influent were removed after treatment. Sludge adsorption played an important role in the reduction of EDCs. The range of phenols in sludge was 17-35 mg/kg, the range of PAEs was 25-77 mg/kg and the range of PAHs was 1.33-1.74 mg/kg. Compared with the results in other countries in literature, the existence of EDCs in the Sewage Treatment Plant was not serious.

Benzhydryl Compounds↗
PubMed2003

The leading role and responsibility of the international scientific community in test development.

The possibility that one or more environmental factors may be affecting adversely the endocrine systems of humans and wildlife has been the subject of international study for the past 7 years. Irrespective of which factors are the most important contributors to the perceived problem; the decision has been taken to evaluate synthetic chemicals for such chemical toxicities. This decision requires access to reliable and relevant endocrine disruption (ED) assays. However, few such tests currently exist, albeit many candidate assays are currently under development. Faced with this situation, the US Environmental Protection Agency has taken the lead in supporting the development and validation of appropriate ED assays. Two of these assays, the rodent uterotrophic assay and the Hershberger anti-androgen assay, are in the final stages of validation, a project conducted under the auspices of the Organisation for Economic and Commercial Development. This article describes the particular scientific issues associated with the validation of these two assays and alerts to the continuing need to consider new assay protocols as they become available.

Adenocarcinoma↗
PubMed2002

Kinetic analysis of estrogen receptor/ligand interactions.

Surface plasmon resonance biosensor technology was used to directly measure the binding interactions of small molecules to the ligand-binding domain of human estrogen receptor. In a screening mode, specific ligands of the receptor were easily discerned from nonligands. In a high-resolution mode, the association and dissociation phase binding responses were shown to be reproducible and could be fit globally to a simple interaction model to extract reaction rate constants. On average, antagonist ligands (such as tamoxifen and nafoxidine) were observed to bind to the receptor with association rates that were 500-fold slower than agonists (such as estriol and beta-estradiol). This finding is consistent with these antagonists binding to an altered conformation of the receptor. The biosensor assay also could identify subtle differences in how the same ligand interacted with two different isoforms of the receptor (alpha and beta). The biosensor's ability to determine kinetic rate constants for small molecule/protein interactions provides unique opportunities to understand the mechanisms associated with complex formation as well as new information to drive the optimization of drug candidates.

Antibodies, Monoclonal↗
PubMed1998

Food contamination from epoxy resins and organosols used as can coatings: analysis by gradient NPLC.

Normal phase LC with gradient elution enabled the analysis of a broadened range of oligomers of BADGE (Bisphenol-A diglycidyl ether) and Novolak compounds in canned foods, such as sea foods in oil, meat products and soups. A major component released from Bisphenol-A resins was identified as the cyclo-(Bisphenol-A monoglycidyl ether) dimer and was commonly present in foods at concentrations of around 1 mg/kg. For the epoxy Novolaks, concentrations of the three- to six-ring compounds often far exceeded those of BFDGE (Bisphenol-F diglycidyl ether) and reached 20 mg/kg in foods. A two-step acylation is proposed for the detection of epoxy components.

Benzhydryl Compounds↗
PubMed2004

Plasma vitellogenin levels and gonadal morphology of wild carp (Cyprinus carpio L.) in a receiving rivers downstream of sewage treatment plants.

A field study was carried out in order to assess, in a wild cyprinid fish, the biological effects related to the exposure to estrogenic compounds. The gonadosomic index (GSI), plasma vitellogenin (VTG) level and histological observations of gonads were performed to evaluate the reproductive health in common carp (Cyprinus carpio) from three rivers receiving sewage treatment plant (STP) effluents (Guadarrama, Henares and Jarama rivers, Spain) and from a reference site (Lozoya river). No significative differences in male GSI between sites were described. Only in the 18% of fish from Guadarrama river were elevated plasma VTG levels detected. The presence of oocytes in the testis was not found in any of males examined. The results suggest that the released estrogenic compounds by STPs effluents are not enough capable to adversely affect the gonadal development of the fish studied. Additional studies will be required to assess the risk of estrogenic compounds on fish from other sites of this area.

Animals↗
PubMed1998

Methods for xenoestrogen testing.

Research in our laboratories has focused on development of a battery of in vivo and in vitro bioassays for determining estrogenic activity and potency of different classes of natural and synthetic industrial-derived estrogenic compounds (xenoestrogens) including food/beverage extracts, phytoestrogens, phenolic compounds, organochlorine pesticides and pollutants. For many of the weak estrogenic compounds, their activity as estrogen receptor (ER) agonists or antagonists is dependent on the gene/gene promoter, cell context and expression of ER(alpha) or ER(beta) isoform. For example, extracts of red wine, bound to the ER, exhibited estrogenic activity in T47D, MCF-7 (breast) and Hep G2 (liver) human cancer cell lines, whereas reconstituted organochlorine pesticide residues found in food were active only in Hep G2 cells that transiently expressed ER(alpha) or ER(beta). The relative potencies of red wine extracts versus reconstituted organochlorine pesticides were assay-dependent; however, estrogen equivalent daily intakes from a glass of red wine (approximately 0.5-2 microg estrogen equivalents/day) were at least 10(3) higher than observed for the reconstituted organochlorine pesticide mixtures. Risk assessment of xenoestrogens and other synthetic chemicals which modulate endocrine responses must take into account high dietary levels of natural products in food, drugs and health food store extracts which also modulate endocrine responses.

Animals↗