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Search results for: steroid estrogens
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XbaI and PvuII Polymorphisms of Estrogen Receptor 1 Gene in Females with Idiopathic Scoliosis: No Association with Occurrence or Clinical Form
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Methylation level of the regulatory regions of the estrogen receptor type 1 gene in paravertebral muscles of girls with idiopathic scoliosis
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Methylation of Estrogen Receptor 1 Gene in the Paraspinal Muscles of Girls with Idiopathic Scoliosis and Its Association with Disease Severity
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Glioblastoma-derived spheroid cultures as an experimental model for analysis of EGFR anomalies
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublicationIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Development of Sulfamoylated 4‑(1-Phenyl‑1H‑1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer
PublicationWe present here the advances achieved in the development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer. Prompted by promising biological results and in silico analysis, the initial series of similar compounds were extended, appending a variety of m-substituents at the outer phenyl ring. The inhibition profiles of the newly...
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Optical activity of the guest azobenzene molecule generated by inclusion complexation with steroidal bile acids.
PublicationZsyntetyzowano krystaliczne kompleksy inkluzyjne azobenzenu z kwasami cholowym i deoksycholowym. Otrzymane związki inkluzyjne poddano badaniom przy wykorzystaniu spektroskopii dichroizmu kołowego w fazie stałej (KBr). Dodatni efekt Cottona, odpowiadający niskoenergetycznemu przejściu elektronowemu n-pi*, skorelowano z helikalnością M,M skręconej cząsteczki azobenzenu. Ponadto w celach porównawczych zmierzono dichroizm kołowy w...
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Fulminant hepatic failure in woman with iron and non-steroidal anti-inflammatory drug intoxication
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Non-steroidal anti-inflammatory drugs are safe with respect to the transcriptome of human dermal fibroblasts
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Estrogen Receptor Type 1 and Type 2 Presence in Paravertebral Skeletal Muscles: Expression Level and Relation to Phenotype in Children with Idiopathic Scoliosis
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Expression of Estrogen Receptor Coactivator Proline-, Glutamic Acid- and Leucine-Rich Protein 1 within Paraspinal Muscles in Adolescents with Idiopathic Scoliosis
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A new silylation reagent dimethyl(3,3,3-trifluoropropyl)silyldiethylamine for the analysis of estrogenic compounds by gas chromatography–mass spectrometry
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The Effect of Sterols on Amphotericin B Self-Aggregation in a Lipid Bilayer as Revealed by Free Energy Simulations
PublicationAmphotericin B (AmB) is an effective but toxic antifungal drug, known to increase the permeability of the cell membrane, presumably by assembling into transmembrane pores in a sterol-dependent manner. The aggregation of AmB molecules in a phospholipid bilayer is, thus, crucial for the drug’s activity. To provide an insight into the molecular nature of this process, here, we report an atomistic molecular dynamics simulation study...
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Simultaneous determination of non-steroidal anti-inflammatory drugs and oestrogenic hormones in environmental solid samples
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From the pills to environment – Prediction and tracking of non-steroidal anti-inflammatory drug concentrations in wastewater
PublicationThe extend of environment pollution by pharmaceuticals is in a stage that required more automatic and integrated solutions. The non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most popular pharmaceutical in the world and emerging pollutants of natural waters. The aim of the paper was to check the correlation of the sales data of selected NSAIDs (ibuprofen, naproxen, diclofenac) and their concentration in the WWTP...
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JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
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Characteristics of hybrid chitosan/phospholipid-sterol, peptide coatings on plasma activated PEEK polymer
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Steroidal Molecular Rotors with 1,4-Diethynylphenylene Rotators: Experimental and Theoretical Investigations Toward Seeking Efficient Properties
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Membrane Sterols Modulate the Binding Mode of Amphotericin B without Affecting Its Affinity for a Lipid Bilayer
PublicationMembrane-active antibiotics are known to selectively target certain pathogens based on cell membrane properties, such as fluidity, lipid ordering, and phase behavior. These are in turn modulated by the composition of a lipid bilayer and in particular by the presence and type of membrane sterols. Amphotericin B (AmB), the golden standard of antifungal treatment, exhibits higher activity toward ergosterol-rich fungal membranes, which...
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Influence of Estradiol-17beta on Progesterone and Estrogen Receptor mRNA Expression in Porcine Follicular Granulosa Cells during Short-Term, In Vitro Real-Time Cell Proliferation
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Antibiotic-sterol interactions provide insight into the selectivity of natural aromatic analogues of amphotericin B and their photoisomers
PublicationAromatic heptaene macrolides (AHMs) belong to the group of polyene macrolide antifungal antibiotics. Members of this group were the first to be used in the treatment of systemic fungal infections. Amphotericin B (AmB), a non-aromatic representative of heptaene macrolides, is of significant clinical importance in the treatment of internal mycoses. It includes the all-trans heptaene chromophore, whereas the native AHMs contain two...
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Longitudinal drug synergy assessment using convolutional neural network image-decoding of glioblastoma single-spheroid cultures
PublicationAbstract Background In recent years, drug combinations have become increasingly popular to improve therapeutic outcomes in various diseases, including difficult to cure cancers such as the brain cancer glioblastoma. Assessing the interaction between drugs over time is critical for predicting drug combination effectiveness and minimizing the risk of therapy resistance. However, as viability readouts of drug combination experiments...
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How do sterols determine the antufungal activitiy of amphotericin B? Free energy of binding between the drug and its membrane targets.
PublicationAmphotericin B (AmB) is a well-known polyene antibiotic used to treat systemic fungal infections. It is commonly accepted that the presence of sterols in the membrane is essential for the AmB biological activity, that is, for the formation of transmembrane ion channels. The selective toxicity of AmB for fungal cells is attributed to the fact that it is more potent against fungal cell membranes containing ergosterol than against...
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CYP19 mRNA and protein levels in nontumorogenic breast epithelial cells (MCF10A) treated with active components of cabbage juices
PublicationZbadano wpływ soków z kapusty na poziom ekspresji genu CYP19 w nietumorogennych komórkach nabłonka gruczołu mlekowego MCF10A kodującego enzym aromatazę uczestniczący w biosyntezie estrogenów i w związku z tym wpływający na zagrożenie rakiem piersi. Soki z kapusty oraz bioaktywne związki w nich występujące stosowane w niskich dawkach obniżały poziom ekspresji tego genu, a zatem miały działanie chemoprewencyjne. Wyższe dawki zarowno...
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Is sequential batch reactor an efficient technology to protect recipient against non-steroidal anti-inflammatory drugs and paracetamol in treated wastewater?
PublicationThe tested facility was a wastewater treatment plant (WWTP) in Swarzewo, where the wastewater treatment takes place in aeration chambers with activated sludge using sequential batch reactors (SBRs). The concentration of the following pharmaceuticals: ibuprofen, paracetamol, flurbiprofen, naproxen, diclofenac, and its metabolites 5OH-diclofenac and 4OH-diclofenac was tested in influents and effluents. Simultaneously, the conventional...
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublicationHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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On the Possibility of the Amphotericin B-Sterol Complex Formation in Cholesterol- and Ergosterol-Containing Lipid Bilayers: A Molecular Dynamics Study
PublicationAmphotericin B (AmB) is a well-known membrane-active antibiotic that has been used to treat systemicfungal infections for more than 45 years. Therapeutic application of AmB is based on the fact that it is moreactive against ergosterol-containing membranes of fungal cells than against mammalian membranes withcholesterol. In this paper, we examine the hypothesis according to which the selectivity of the AmB's membraneaction originates...
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Metal ion directed template synthesis using 2-acetyl-1,3-indandione and ethylenediamine: steric and electronic restrictions
PublicationA template synthesis using 2-acetyl-1,3-indandione and ethylenediamine results in formation of octahedral Ni complex, whose crystal structure has been resolved using single crystal X-ray diffraction. The structure indicates that only exocyclic enolic oxygen atom of the triketone takes part in the condensation with ethylenediamine.
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Stone cutting industry waste-supported zinc oxide nanostructures for ultrasonic assisted decomposition of an anti-inflammatory non-steroidal pharmaceutical compound
PublicationPowdered stone waste (PSW) obtained from a stone cutting industrial unit was applied as support for the immobilization of nano-sized ZnO to be utilized as an effective catalyst for the catalytic conversion of acetaminophen (ACE) under ultrasonication. The incorporation of ZnO nanostructures into PSW structure enhanced the specific surface area and pore volume of the as-prepared nanocompound. The change in the value of zero point...
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Aryl-perfluoroaryl stacking interactions: hydrogen bonding and steric effects in controlling the structure of supramolecular assemblies of N,N'-diaryloxalamides
PublicationOtrzymano kilka struktur supramolekularnych N,N'-diarylooksamidów z silnymi donorami protonów tj. pentafluorofenolem (pfp) i kwasem pentafluorobenzoesowym (pfba), w celu zilustrowania roli współdziałania wiązań wodorowych i oddziaływań pi-elektronowych w tworzeniu uporządkowanych faz stałych. Wprowadzenie do struktury oksamidów objętościowych podstawników arylowych utrudniało tworzenie występujących pomiędzy cząsteczkami oksamidów...
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Determination of hormones in water samples using liquid chromatography coupled with tandem mass spectrometry
PublicationOver the past few years, many synthetic (ethinylestradiol) and natural (estradiol,estriol, estrone) compounds present in the environment have been affecting the hormonalbalance of humans and animals. Steroid hormones are very often used for medical purposesand have high estrogenic activity what makes them endocrine disrupters. Most hormonalcompounds are released into the water as a result of their incomplete removal in wastewatertreatment...
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Determination of non-steroidal anti-inflammatory drugs in natural waters using off-line and on-line SPE followed by LC coupled with DAD-MS
PublicationOpisano dwie metody pozwalające na jednoczesne oznaczanie zawartości niesterydowych leków przeciwzapalnych (difluisal, diklofenak, naproksen, tolmetin, fenoprofen, ibuprofen) w próbkach wodnych. Próbki przygotowywano do analizy z użyciem techniki ekstrakcji do fazy stałej (off-line i on-line). Natomiast oznaczeń końcowych dokonano z użyciem LC-DAD-MS. Sprawdzono kilka różnych kolumienek ekstrakcyjnych i wybrano RP-18 jako najlepsze...
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Screening of 17α-ethynylestradiol and non-steroidal anti-inflammatory pharmaceuticals accumulation in Mytilus edulis trossulus (Gould, 1890) collected from the Gulf of Gdańsk
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The Influence of Alkyl Chain Length and Steric Effect on the Stability Constants and Extractability of Co(II) Complexes with 1-Alkyl-2-Methylimidazoles
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Modulation of CYP1A1, CYP1A2 and CYP1B1 expression by cabbage juices and indoles in human breast cell lines
PublicationEpidemiological studies have shown that consumption of cab- bage and sauerkraut is connected with significant reduction of breast cancer incidences. Estrogens are considered a major breast cancer risk factor and their metabolism by P450 enzymes substan- tially contributes to carcinogenic activity. The aim of this study was to investigate the effect of cabbage and sauerkraut juices of differ- ent origin on the expression profile...
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Phytoecdysteroid containing plants – a source of bioactive compounds with potential anticarcinogenic effects
PublicationEcdysteroids are a group of steroids synthesized in inver- tebrates as molting hormones and also in some plants as secondary metabolites acting as a defense against parasites. These compounds do not naturally occur in mammals and are not structurally related to mammalian steroid hor- mones, consequently do not activate mammalian hormone receptors. Ecdysteroids exhibit very low toxicity to mam- mals and to date no serious side effects...
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A new silylating reagent – dimethyl(3,3,3-trifluoropropyl)silyldiethylamine – for the derivatisation of non-steroidal anti-inflammatory drugs prior to gas chromatography–mass spectrometry analysis
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Projektowanie, synteza oraz badanie aktywności biologicznej amidosiarczanowych inhibitorów sulfatazy steroidowej zawierających w swojej konstytucji ugrupowania fosforowe lub wiązania C-F
PublicationWedług Światowej Organizacji Zdrowia (WHO) estrogeny są jednymi z głównych czynników stymulujących wzrost nowotworów hormonozależnych. Dlatego też, projektowanie oraz synteza nowych, skuteczniejszych środków wpływających na biosyntezę estrogenów stanowi ogromne wyzwanie dla współczesnej medycyny. W ostatnich latach liczne ośrodki naukowe na całym świecie prowadzą intensywne badania związane z poszukiwaniem nowych, skutecznych inhibitorów...
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Hormony płciowe w środowisku - zagrożenia jakie niosą ze sobą
PublicationSpośród dużej ilości i różnorodności związków chemicznych dostających się do środowiska coraz większą uwagę i szczególne zainteresowanie poświęca się związkom endokrynnym (ang. Endocrine Disrupting Coumpounds - EDCs). Wśród związków endokrynnych to estrogeny zarówno naturalne jak i syntetyczne zostały wskazane i opisane jako związki niosące ze sobą największy potencjał aktywności estrogennej. Jednym z głównych źródeł estrogenów...
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Determination of sex hormone concentration in wastewater samples.
Open Research DataConcentration levels of five selected steroid hormones in influent and effluent waters from wastewater treatment plant were determined using SPE(C18)-HPLC-ESI/MS/MS method. Sex hormones like: estradiol, estriol, estrone, 17-α-ethynyloestradiol, progesterone were present in all influent wastwater samples.
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Adipokine and cytokine levels in patients with adrenocortical cancer, subclinical Cushing's syndrome and healthy controls
PublicationIntroduction In recent years researchers have focused at hormonal activity in Cushing’s syndrome (CS) in connection with metabolic disorders and the role of adipokines and cytokines secreted by the adipose tissue. The aim of the study was to investigate levels of adipokines and cytokines in patients with: subclinical CS (SCS) – in relation to hormonal parameters of hypercortisolemia, and, adrenocortical cancer (ACC). Materials...
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Photo-conversion of two epimers (20R and 20S) of pregna-5,7-diene-3β, 17α, 20-triol and their bioactivity in melanoma cells
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Vitamin D derivatives enhance cytotoxic effects of H2O2 or cisplatin on human keratinocytes
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Synthesis and photochemical transformation of 3β,21-dihydroxypregna-5,7-dien-20-one to novel secosteroids that show anti-melanoma activity
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Synthesis and comprehensive structural and physicochemical characterization of dutasteride hydrochloride hydrate solvates
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Modulation of CYP19 expression by cabbage juices and their active components: indole-3-carbinol and 3,30-diindolylmethene in human breast epithelial cell lines
PublicationThe aim of this study was to evaluate the effect of white cabbage and sauerkraut juices of different origin and indole-3-carbinol (I3C) and diindolylmethane (DIM) on expression of CYP19 gene encoding aromatase, the key enzyme of estrogen synthesis.Remarkable differences in the effect on CYP19 transcript and protein level were found between the cab- bage juices (in 2.5-25 mL/L concentrations) and indoles (in 2.5-50 lM doses) in...
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Self-assembly, stability and conductance of amphotericin B channels: bridging the gap between structure and function
PublicationAmphotericin B (AmB), one of the most powerful but also toxic drugs used to treat systemic mycoses, is believed to selectively permeabilize fungal cell membranes to ions in a sterol-dependent manner. Unfortunately, the structure of the biologically active AmB channels has long eluded researchers, obstructing the design of safer alternatives. Here, we investigate the structural and thermodynamic aspects of channel formation, stability,...
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Naturalne związki organiczne
PublicationKsiążka zawiera dwanaście rozdziałów merytorycznych, w których omówiono występowanie, właściwości, otrzymywanie i zastosowanie następujących naturalnych organicznych: aminokwasy, peptydy, białka, cukry, lipidy, alkaloidy, steroidy, kwasy nukleinowe, polifenole i flawonoidy, hormony owadzie i roślinne, terpenoidy i izoterpenoidy oraz związki sygnałowe (feromony).
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2-Methoxyestradiol and Hydrogen Peroxide as Promising Biomarkers in Parkinson’s Disease
PublicationEstrogens function in numerous physiological processes including controlling brain cell growth and differentiation. 2-Meth- oxestradiol (2-ME2), a 17β-estradiol (E2) metabolite, is known for its anticancer effects as observed both in vivo and in vitro. 2-ME2 affects all actively dividing cells, including neurons. The study aimed to determine whether 2-ME2 is a potentially cancer-protective or rather neurodegenerative agent in a...