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Search results for: steroid estrogens
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STEROIDS
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Simultaneous determination of non-steroidal anti-inflammatory drugs and natural estrogens in the mussels Mytilus edulis trossulus
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Evidence for sex steroid receptors in feline brainstem
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Cyanogenic Compounds and Estrogen Disruptors
PublicationBalanced diet consists largely of plants containing cyanogenic compounds in the form of the more common cyanogenic glycosides and sometimes lipids. Maize, wheat, rye, apples, barley, oats, sugar cane and yet many other plants consumed by humans contain cyanogenic compounds. However the risk of poisoning is negligible as it is very easy to remove the toxic HCN by grinding and drying in air or soaking in water and an additional...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublicationBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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SOCS3 is epigenetically up-regulated in steroid resistant nephrotic children.
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Analytical challenges and recent advances in the determination of estrogens in water environments.
PublicationW artykule przedstawiono analizę i syntezę danych literaturowych związanych z występowaniem i oznaczaniem zwiazków endogennych w próbkach wody.Przedstawiono najważniejsze wyzwania związane z wykrywaniem i oznaczaniem śladowych ilości tego typu związków w próbkach środowiskowych.Omówiono również najnowsze rozwiązania metodyczne w zakresie:-przygotowania próbek do analizy (konserwacja, derywatyzacja, izolazja i wzbogacanie analitów)-oznaczania...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Estrogen Receptors in Cell Membranes: Regulation and Signaling
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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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Simultaneous analysis of non-steroidal anti-inflammatory drugs and estrogenic hormones in water and wastewater samples using gas chromatography–mass spectrometry and gas chromatography with electron capture detection
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The triple-sorbents solid-phase extraction for pharmaceuticals and estrogens determination in wastewater samples
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Chemometric Evaluation of Urinary Steroid Hormone Levels as Potential Biomarkers of Neuroendocrine Tumors
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...
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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates
PublicationA series of phosphate and thiophosphate analogs based on the frameworks of N-alkanoyl tyramines have been synthesized and biologically evaluated. Their binding modes have been modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from the human placenta as well as the MCF-7, MDA-MB-231 and SkBr3 cancer cell lines. Most of the new STS inhibitors possessed potent activity...
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Geometry optimization of steroid sulfatase inhibitors - the influence on the free binding energy with STS
PublicationIn the paper we review the application of two techniques (molecular mechanics and quantum mechanics) to study the influence of geometry optimization of the steroid sulfatase inhibitors on the values of descriptors coded their chemical structure and their free binding energy with the STS protein. We selected 22 STS-inhibitors and compared their structures optimized with MM+, PM7 and DFT B3LYP/6–31++G* approaches considering separately...
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Estrogen Receptor 2 Gene Polymorphism in Idiopathic Scoliosis
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Towards β-selectivity in functional estrogen receptor antagonists
PublicationBased on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...
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Expression of α and β Estrogen Receptors in the Chicken Ovary
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New clicked full agonists of the estrogen receptor β
PublicationA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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A mechanistic model for fate and removal of estrogens in biological nutrient removal activated sludge systems
PublicationTwo estrogen fate and transformation models were integrated with a comprehensive activated sludge model (ASM) to predict estrogen removal based on biomass and solids production. Model predictions were evaluated against published full-scale plant data as well as results from a laboratory-scale sequencing batch reactor (SBR) fed synthetic wastewater. The estrogen fate model relating the rate of total estrogen degradation to soluble...
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Dynamics of Oxidative Damage at Early Stages of Estrogen-dependant Carcinogenesis
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Estrogen receptors genes polymorphisms and age at menarche in idiopathic scoliosis
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The PolarScreen™ Estrogen Receptor Competitor Assays for determination of estradiol equivalent concentrations (EEQs) in sewage and drinking water samples.
Open Research DataMunicipal waste waters are one of the main sources of estrogenic compounds in aquatic environments. Feminization of fish downstream of Waste Water Treatment Plants (WWTPs) discharges has been observed worldwide. Some estrogenic chemicals, particularly steroid estrogens, are known to cause disruption of the endocrine system of fishes and abnormalities...
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SOCS3 and SOCS5 mRNA expressions may predict initial steroid response in nephrotic syndrome children
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Estrogen receptors 1 and 2 genotypes and age at menarche in idiopathic scoliosis
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Comparison of High Performance Liquid Chromatography Methods with Different Detectors for Determination of Steroid Hormones in Aqueous Matrices
PublicationThis paper presents the development and comparison of procedures for the qualitative and quantitative determination of five estrogenic compounds (17-a-ethynylestradiol, estrone, estradiol, estriol, and progesterone) in drinking water and wastewater samples. Five extraction columns and two disks were tested for their efficiency. The C18 columns were superior on the basis of cost for solid phase extraction of drinking water or sewage....
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublicationThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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Expression of estrogen receptors, PELP1, and SRC in human spermatozoa and their associations with semen quality
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Expression Profile of Genes Regulating Steroid Biosynthesis and Metabolism in Human Ovarian Granulosa Cells—A Primary Culture Approach
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Study of the chromatographic behavior of selected steroid hormones on aluminum oxide plates based on quantitative structure-retention relationships
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors. Their binding modes were modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta. All of the newly synthesised coumarin derivatives were...
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Comparative molecular modelling of biologically active sterols
PublicationMembrane sterols are targets for a clinically important antifungal agent – amphotericin B. The relatively specific antifungal action of the drug is based on a stronger interaction of amphotericin B with fungal ergosterol than with mammalian cholesterol. Conformational space occupied by six sterols has been defined using the molecular dynamics method to establish if the conformational features correspond to the preferential interaction...
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PELP1 and SRC kinase as important molecules in the estrogen-mediated pathway in human testis and epididymis
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Transcriptomic Effects of Estrogen Starvation and Induction in the MCF7 Cells. The Meta-analysis of Microarray Results
PublicationEstrogen is one of the most important signaling molecules which targets a number of genes. Estrogen levels regulate cell proliferation and a plethora of metabolic processes, which may interfere with a range of medical conditions and drug metabolism. The MCF7 breast cancer cell line, expressing the estrogen receptor α, is a well-studied model of cellular answer to estrogen. The aim of this study was to characterize transcriptomic...
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Relationships between biomarkers of inflammation, ovarian steroids, and age at menarche in a rural polish sample
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Determination of estrogenic endocrine disruptors in environmental samples - a review of chromatographic methods
PublicationWśród związków endokrynnych to estrogeny zarówno naturalne jak i syntetyczne zostały wskazane i opisane jako związki niosące ze sobą największy potencjał aktywności estrogennej. Wysoki potencjał estrogenny jaki posiadają związki z grupy hormonów płciowych potwierdziły badania przeprowadzone zarówno in vitro jak i in vivo. W dużej części (50-95%) próbek ścieków pochodzących z oczyszczalni ścieków zostały wykryte związki z grupy...
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Expression and cellular distribution of estrogen and progesterone receptors and the real-time proliferation of porcine cumulus cells
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Methylation of estrogen receptor 2 (ESR2) in deep paravertebral muscles and its association with idiopathic scoliosis
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Steroid profiles as potential biomarkers in patients with urogenital tract cancer for diagnostic investigations analyzed by liquid chromatography coupled to mass spectrometry
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Replication study of estrogen receptor 1 XbaI polymorphism in adolescent idiopathic scoliosis (AIS) Caucasian population
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A Potential Relationship Between Estrogen Receptors Polymorphisms, Sperm Function and in vitro Fertilization Success: A Preliminary Study*
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Clinical and Biological Significance of ESR1 Gene Alteration and Estrogen Receptors Isoforms Expression in Breast Cancer Patients
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Molecular modelling of membrane sterols with the use of the GROMOS 96 forcefield
PublicationPodstawowym zadaniem tego projektu było udowodnienie zasadności stosowania pola siłowego GROMOS 96 do symulacji steroli błonowych metodą dynamiki molekularnej. Uzyskane wyniki jasno wskazują, że to pole siłowe bardzo dobrze nadaje się do symulacji silnie lipofilowych układów.
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Quantitative structure—retention relationships of some steroid and phenanthrene derivatives on cyano-, reversed-phase, and normal-phase thin-layer chromatography stationary phases
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