• MeSH
• dítě MeSH
• dospělí MeSH
• estradiol krev   MeSH
• lidé MeSH
• mladiství MeSH
• předškolní dítě MeSH
• puberta * MeSH
• věkové faktory MeSH
• Check Tag
• dítě MeSH
• dospělí MeSH
• lidé MeSH
• mladiství MeSH
• předškolní dítě MeSH
• ženské pohlaví MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• estradiol MeSH

In the introduction of the paper the authors explain that it is essential to adopt effective preventive provisions to prevent the loss of osseous tissue in women after the menopause and to prevent osteoporotic fractures. In Bohemia and Moravia during the last 20 years the incidence of these frequently fatal or invalidating fractures of the proximal femur has increased substantially and in view of the ageing of the population it may be assumed that this trend will proceed further. Among possible preventive provisions, in order to eliminate undesirable metabolic side-effects of long-term hormonal substitution treatment, it seems best to administer by the parenteral route natural oestradiol by using the transdermal therapeutic Estraderm TTS system. Its effectiveness in suppressing menopause-induced enhanced bone resorption was tested in 11 women where on average within three months after bilateral ovariectomy increased bone resorption was found. In all women in the course of four months treatment all biochemical indicators of bone remodelling became normal - urinary excretion of hydroxyproline, acid plasma phosphatase activity, serum alkaline phosphatase isoenzyme, and serum osteocalcin. The dynamics of indicators of osteoresorption were similar as in women treated with oral synthetic oestrogen, which may produce, however, serious metabolic side-effects. Substitution treatment with Estraderm improves significantly also other manifestations of the climacteric oestrogen deficiency syndrome. Its safety is further enhanced by combination with progesterone.

• MeSH
• aplikace kožní MeSH
• dospělí MeSH
• estradiol aplikace a dávkování   MeSH
• estrogenní substituční terapie * MeSH
• lidé středního věku MeSH
• lidé MeSH
• ovarektomie MeSH
• postmenopauzální osteoporóza prevence a kontrola   MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• ženské pohlaví MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• estradiol MeSH

The levels of oestradiol-17 beta (E2) in the blood plasma were evaluated in 15 boars exhibiting signs of sexual potency disorders and in 20 boars with no such disorders before and after i. v. administration of chorion gonadotropin (HCG). No significant difference (P greater than 0.05) was found in the E2 levels in the blood plasma of the boars of the two groups before HCG administration. Two hours after the i. v. injection of 500 I. U. of HCG, an insignificant increase in the basal levels of E2 was recorded, reaching on the average 28.9% in the boars with potency disorders and 38.8% in those with no potency changes. Neither were there any significant differences in the E2 levels determined after HCG treatment between the boars with and without sexual potency disorders. It is inferred from the results that deviations in E2 concentration in the blood obviously do not contribute significantly to disorders in the sexual potency of boars.

• MeSH
• choriogonadotropin terapeutické užití   MeSH
• erektilní dysfunkce krev   farmakoterapie   veterinární   MeSH
• estradiol krev   MeSH
• nemoci prasat krev   farmakoterapie   MeSH
• prasata MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• choriogonadotropin MeSH
• estradiol MeSH

Novel BODIPY-estradiol conjugates have been synthesized by selecting position C-3-O for labeling. The conjugation strategy was based on Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) or etherification. Estradiol derivatives used as azide partners bearing an ω-azidoalkyl function through C4-C8-long linkers have been prepared. CuAAC reactions of estradiol azides with BODIPY alkyne furnished fluorescent 3-O-labeled conjugates bearing the triazole ring as a coupling moiety. Williamson etherifications of 3-O-(ω-bromoalkyl)-17β-estradiol derivatives with BODIPY-OH resulted in labeled conjugates connected with an ether moiety. Interactions of the conjugates with estrogen receptor (ER) were investigated using molecular docking calculations in comparison with estradiol. The conjugates occupied both the classical and alternative binding sites on human ERα, with slightly lower binding affinity to references estradiol and diethystilbestrol. All compounds have displayed reasonable estrogenic activity. They increased the proliferation of ER-positive breast cancer cell line MCF7 contrary to ER-negative SKBR-3 cell line. The most potent compound 13a induced the transcriptional activity of ER in dose-dependent manner in dual luciferase recombinant reporter model and increased progesterone receptor's expression, proving the retained estrogenic activity. The fluorescence of candidate compound 13a co-localised with the ERα. The newly synthesized labeled compounds might serve as good starting point for further development of fluorescent probes for modern biological applications. In addition to studying steroid uptake and transport in cells, e.g. in the processes of biodegradation of estrogen-hormones micropollutants, they could also be utilized in examination of estrogen-binding proteins.

• Klíčová slova
• 17β-estradiol, BODIPY, CuAAC, Estrogenic activity, Human estrogen receptor alpha,
• MeSH
• alfa receptor estrogenů * metabolismus   chemie   MeSH
• azidy chemie   MeSH
• estradiol * chemie   farmakologie   MeSH
• estrogeny chemie   MeSH
• fluorescenční barviva chemie   MeSH
• lidé MeSH
• MFC-7 buňky MeSH
• nádorové buněčné linie MeSH
• proliferace buněk účinky léků   MeSH
• simulace molekulového dockingu * MeSH
• sloučeniny boru * chemie   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene MeSH Prohlížeč
• alfa receptor estrogenů * MeSH
• azidy MeSH
• ESR1 protein, human MeSH Prohlížeč
• estradiol * MeSH
• estrogeny MeSH
• fluorescenční barviva MeSH
• sloučeniny boru * MeSH

Intracerebroventricular (ICV) administration of estradiol benzoate (E2B) and progesterone (P) induces intense lordosis behavior in ovariectomized rats primed peripherally with E2B. The present study tested the hypothesis that the Kisspeptin (Kiss) and melanin-concentrating hormone (MCH) pathways regulate female sexual behavior induced by these steroid hormones. In Experiment 1, we tested the relevance of the Kiss pathway by ICV infusion of its inhibitor, kiss-234, before administration of E2B or P in estrogen-primed rats. Lordosis induced by E2B alone or with the addition of P was reduced significantly at 30, 120, and 240 min. In Experiment 2, ICV infusion of MCH 30 min before E2B or P significantly reduced lordosis in rats primed with E2B alone. These data support the hypothesis that the Kiss and MCH pathways, which can release or modulate gonadotropin-releasing hormone (GnRH), are involved in E2B- and P-induced lordosis.

• Klíčová slova
• Estradiol, Kisspeptin, Lordosis, Melanin-concentrating hormone, Progesterone,
• MeSH
• estradiol farmakologie   MeSH
• hormon uvolňující gonadotropiny farmakologie   MeSH
• kisspeptiny farmakologie   MeSH
• krysa rodu Rattus MeSH
• lordóza * chemicky indukované   MeSH
• ovarektomie MeSH
• progesteron * farmakologie   MeSH
• sexuální chování zvířat fyziologie   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• estradiol 3-benzoate MeSH Prohlížeč
• estradiol MeSH
• hormon uvolňující gonadotropiny MeSH
• kisspeptiny MeSH
• melanin-concentrating hormone MeSH Prohlížeč
• progesteron * MeSH

The effect of current 48-hour infusion of estradiol benzoate (EB) on the dynamics of the concentration of progesterone (P) and thyroxine (T4) was studied in four heifers in the luteal stage of their cycle. The parameters were evaluated in three intervals: infusion (A), post-infusion (B) and "uninfluenced" interval (C). In the course of infusion the concentrations of P in three animals had a markedly descending tendency. The P concentration increase in the 36th hour of infusion was maintained also during the post-infusion interval. The decrease in P in the third, "uninfluenced", interval was replaced by a new rise towards the end. One heifer showed an increase in P concentrations at the beginning of EB infusion. A decrease was recorded towards the end of the interval. The concentration decreased in the post-infusion period. A comparatively high concentration of P in the "uninfluenced" interval was again replaced by a drop towards the end in the 286th hour. The concentration of T4 in three heifers had a descending tendency in the infusion and post-infusion intervals. The decrease in the infusion interval was more pronounced. In the "uninfluenced" interval the T4 concentrations increased step by step. In one heifer the concentration of T4 slightly increased during infusion. A decrease was recorded in the post-infusion and "uninfluenced" interval. Rectal examination in the 172nd hour revealed the original corpus luteum in three animals and the production of the corpus luteum in the same ovary was found in this period in one heifer. In the 88th hour this animal showed clinical manifestations of oestrus. On the basis of the dynamics of the studied hormones and clinical studies, the thyroid hormones can be regarded as an important secondary factor involved in the permanent cyclic changes in reproduction process.

• MeSH
• estradiol farmakologie   MeSH
• luteální fáze * MeSH
• menstruace * MeSH
• progesteron krev   MeSH
• skot krev   MeSH
• thyroxin krev   MeSH
• zvířata MeSH
• Check Tag
• skot krev   MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• estradiol MeSH
• progesteron MeSH
• thyroxin MeSH

17α-Estradiol (αE2) is a natural diastereoisomer of 17β-estradiol (E2). It is well known that αE2 can bind to estrogen receptors. However, its biological activity is less than that of E2 and is species and tissue specific. The goal of our study was to propose the mechanism of αE2 hormonal response in rat sperm during their capacitation in vitro and compare it with a previously studied mouse model. Concentration changes in externally added αE2 during capacitation of rat sperm were monitored by the high-performance liquid chromatographic method with tandem mass spectrometric detection (HPLC-MS/MS). The calculated values of relative concentrations Bt were subjected to kinetic analysis. The findings indicated that αE2 in rat sperm did not trigger autocatalytic reaction, in contrast to the mouse sperm, and that the initiation of the hormone penetration through the sperm plasma membrane was substantially faster in rats.

• Klíčová slova
• 17α-estradiol, HPLC MS/MS, capacitation, estrogen receptors, kinetics, rat, sperm,
• MeSH
• estradiol * chemie   MeSH
• kapacitace spermií * fyziologie   MeSH
• kinetika MeSH
• krysa rodu Rattus MeSH
• myši MeSH
• sperma metabolismus   MeSH
• tandemová hmotnostní spektrometrie MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• estradiol * MeSH

Microtubule dynamics is one of the major targets for new chemotherapeutic agents. This communication presents the synthesis and biological profiling of steroidal dimers based on estradiol, testosterone and pregnenolone bridged by 2,6-bis(azidomethyl)pyridine between D rings. The biological profiling revealed unique properties of the estradiol dimer including cytotoxic activities on a panel of 11 human cell lines, ability to arrest in the G2/M phase of the cell cycle accompanied with the attenuation of DNA/RNA synthesis. Thorough investigation precluded a genomic mechanism of action and revealed that the estradiol dimer acts at the cytoskeletal level by inhibiting tubulin polymerization. Further studies showed that estradiol dimer, but none of the other structurally related dimeric steroids, inhibited assembly of purified tubulin (IC50, 3.6 μM). The estradiol dimer was more potent than 2-methoxyestradiol, an endogenous metabolite of 17β-estradiol and well-studied microtubule polymerization inhibitor with antitumor effects that was evaluated in clinical trials. Further, it was equipotent to nocodazole (IC50, 1.5 μM), an antimitotic small molecule of natural origin. Both estradiol dimer and nocodazole completely and reversibly depolymerized microtubules in interphase U2OS cells at 2.5 μM concentration. At lower concentrations (50 nM), estradiol dimer decreased the microtubule dynamics and growth life-time and produced comparable effect to nocodazole on the microtubule dynamicity. In silico modeling predicted that estradiol dimer binds to the colchicine-binding site in the tubulin dimer. Finally, dimerization of the steroids abolished their ability to induce transactivation by estrogen receptor α and androgen receptors. Although other steroids were reported to interact with microtubules, the estradiol dimer represents a new structural type of steroid inhibitor of tubulin polymerization and microtubule dynamics, bearing antimitotic and cytotoxic activity in cancer cell lines.

• Klíčová slova
• 17β-Estradiol (E2) (PubChem CID: 5757), 2-Methoxyestradiol (2-ME) (PubChem CID: 66414), Antimitotic activity, Dihydrotestosterone (DHT) (PubChem CID: 10635), Luciferase reporter assay, Microtubule dynamics, Microtubules, Molecular dynamics simulation, Nocodazole (PubChem CID: 4122), Paclitaxel (PubChem CID: 36314), Steroid dimer, Steroid receptor, Tubulin assembly,
• MeSH
• buněčný cyklus MeSH
• estradiol chemie   farmakologie   MeSH
• estrogeny chemie   farmakologie   MeSH
• lidé MeSH
• mikrotubuly účinky léků   fyziologie   MeSH
• modulátory tubulinu chemie   farmakologie   MeSH
• nádorové buňky kultivované MeSH
• nádory farmakoterapie   metabolismus   patologie   MeSH
• polymerizace MeSH
• proliferace buněk MeSH
• tubulin chemie   účinky léků   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• estradiol MeSH
• estrogeny MeSH
• modulátory tubulinu MeSH
• tubulin MeSH

A novel HPLC method for simultaneous determination of estradiol and its seven degradation products in topical gel was developed. Zorbax SB-CN (150 mm x 4.6 mm, 5 microm) analytical column and mobile phase composed of acetonitrile, phosphoric acid 0.085%, and tetrahydrofurane (27:63:10, v/v/v) at flow-rate 1.0 ml min(-1) were used for the chromatographic separation using UV detection at 225 nm. The active substance estradiol was separated from all its known degradation products successfully. Two degradation products estrone and Delta(9(11))-estrone were not separated sufficiently, their peaks were evaluated as a sum of two components. The method was validated according to ICH guideline recommendations and thereafter it was successfully applied for stability tests of topical cream Estrogel HBF in the quality control laboratory. Limits of detection for degradation products ranged from 1.03 x 10(-5) to 1.14 x 10(-4) mg ml(-1), limits of quantitation for degradation products were in the range 3.43 x 10(-5) to 3.81 x 10(-4) mg ml(-1). The developed method is selective, precise, accurate and sensitive enough for determination of estradiol and its known degradation products.

• MeSH
• estradiol analogy a deriváty   analýza   izolace a purifikace   MeSH
• estron analýza   MeSH
• ethinylestradiol analýza   MeSH
• vysokoúčinná kapalinová chromatografie metody   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• validační studie MeSH
• Názvy látek
• estradiol-17 beta-3-methyl ether MeSH Prohlížeč
• estradiol MeSH
• estron MeSH
• ethinylestradiol MeSH

• MeSH
• dialýza ledvin škodlivé účinky   MeSH
• estradiol krev   MeSH
• gynekomastie krev   etiologie   MeSH
• lidé středního věku MeSH
• lidé MeSH
• senioři MeSH
• testosteron krev   MeSH
• Check Tag
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• senioři MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• estradiol MeSH
• testosteron MeSH