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Mamta Tripathy, Umesh Rai
The current study in Indian wall lizard Hemidactylus flaviviridis for the first time demonstrates the reproductive phase-dependent expression pattern of aromatase (cyp19) and estrogen receptor subtypes (er-α and er-β) as well as their gonadotropic regulation in the ovary of a squamate. The expression of cyp19 remained low during regressed phase, increased markedly in recrudescent and declined sharply in breeding phase. Further, temporal profile of plasma estradiol 17-β (E2) was found to be relatively parallel to the expression pattern of ovarian cyp19...
October 14, 2017: Steroids
Amal Al-Aboudi, Belal Muneeb Kana'an, Musa Abu Zarga, Saira Bano, Atia-Tul-Wahab, Kulsoom Javed, M Iqbal Choudhary
Fungal cells were used for the first time to synthesize derivatives of spironolactone (1), a diuretic and antihypertensive drug. Ten different fungi were screened for their ability to biotransform 1, four of which were able to produce metabolites 2-8. Gibberella fujikuroi produced canrenone (2), 1-dehydrocanrenone (3), Curvularia lunuta provided compound 2, and 7α-thio-spironolactone (4), Fusarium lini yielded compounds 2, 3, 1β-hydroxycanrenone (5), 1α-hydroxycanrenone (6), 1-dehydro-15α-hydroxycanrenone (7), and 15α-hydroxycanrenone (8), while Aspergillus alliaceus was able to produce all the seven metabolites...
October 13, 2017: Steroids
Xiufang Shi, Zhihao Wang, Feng Xu, Xiang Lu, Haifeng Yao, Dandan Wu, Shuaijun Sun, Ruifang Nie, Shuo Gao, Panpan Li, Liwen Xia, Zhenzhong Zhang, Cong Wang
A series of 17β-amide-2-methoxyestradiol compounds were synthesized with an aim to enhance the antiproliferative effect of 2-methoxyestradiol. The antiproliferative activity of 2-methoxyestradiol analogs against human cancer cells was investigated. 2-methoxy-3-benzyloxy-17β-chloroacetamide-1,3,5(10)-triene (5e) and 2-methoxy-3-hydroxy-17β-butyramide-1,3,5(10)-triene (6c) had comparable or better antitumor activity than 2-methoxyestradiol. The elimination half-life of 6c (t1/2β = 240.93 min) is ten times longer than 2-ME and the area under the curve was seven times (AUC0-tmin =2068...
October 12, 2017: Steroids
Maria Filek, Elżbieta Rudolphi-Skórska, Apolonia Sieprawska, Miroslav Kvasnica, Anna Janeczko
Steroids constitute one of the most important groups of compounds of regulatory properties both in the animal and plant kingdom. In plants, steroids such as brassinosteroids or progesterone, by binding to protein receptors in cell membranes, regulate growth and initiate processes leading to increased tolerance to stress conditions. Due to their structural similarities to sterols, these steroids may also directly interact with cellular membranes. Our aim was to determine the changes of the structural parameters of lipid membranes under the influence of hydrophobic steroid compounds, i...
October 10, 2017: Steroids
Katherine Vargas-Romero, Oscar Alberto, Marcos Flores-Álamo, Martín A Iglesias-Arteaga
Treatment of steroid sapogenins with H2O2 in CF3COOH for 15min followed by reflux in CH3OH/H2O afforded good yields of pregnan-3β,16β,20-triol 3-monoacetates. When the hydrolysis step was carried out with KOH in refluxing methanol excellent yields pregnantriols were obtained. The resulting compounds were characterized by their melting points and NMR spectral data. An X-ray diffraction analysis of compound 3a confirmed the proposed structure and provided detailed information about the bond lengths, bond angles and conformation...
October 10, 2017: Steroids
Linzhao Li, Guang Yang, Guangneng Liao, Jie Mei, Lan Li, Chengshi Wang, Yujia Yuan, Yujun Shi, Jingping Liu, Zhihui Zhong, Jingqiu Cheng, Yanrong Lu, Iain J Clarke, Younan Chen
Metabolic syndrome (MetS) is characterized by a cluster of key features, which include abdominal obesity, insulin resistance, hypertension, and dyslipidemia. The aim of this study was to assess the impact of elevated glucocorticoid levels on the development of MetS in middle-aged female rhesus monkeys (Macaca Mulatta) after ovariectomy. Six female ovariectomized rhesus monkeys (9-13 years) were randomly assigned to either a control group (normal diet, n=3) or a group in which MetS was facilitated (n=3). The MetS group fed with HFD (15% fat) and received oral prednisone acetate treatment (50 mg/day)...
October 4, 2017: Steroids
John Meitzen, Kyla A Britson, Krista Tuomela, Paul G Mermelstein
17β-estradiol can rapidly modulate neuron function via membrane estrogen receptors (ERs) in a sex-specific manner. For example, female rat hippocampal neurons express palmitoylated versions of ERα and ERβ that associate with the plasma membrane. These membrane-associated ERs are organized by caveolin proteins into functional signaling microdomains with metabotropic glutamate receptors (mGluRs). ER/mGluR signaling mediates several sex-specific estradiol actions on hippocampal neuron function. An important unanswered question regards the mechanism by which sex-specific membrane-associated ER signaling is generated, especially since it has been previously demonstrated that mGluR action is not sex-specific...
September 28, 2017: Steroids
Shan Huang, Jiangning Xie, Jianguo Cui, Liang Liu, Yu Liang, Yi Liu, Qi Xiao
Steroidal compounds have attracted great attentions in biomedical and pharmacological areas. The investigation of structural influences during protein-compound interactions helps in understanding both the biological effects and the mechanism behind bioactivities of steroidal compounds. Herein, the structural influences of three steroidal complexes were investigated based on their binding interactions with human serum albumin (HSA) by multispectroscopic methods and molecular modeling techniques. Three steroidal compounds bonded with HSA to form three HSA-compound complexes, and van der Waals force and hydrogen bond played major roles in stabilizing these complexes...
September 26, 2017: Steroids
Rodewald Andrea, Mills Daniel, M Veronika Gebhart, Gustav F Jirikowski
Steroids are important olfactory signals in most mammalian species. The vomeronasal organ has been suspected to be the primary target of pheromones. In rat vomeronasal sensory neurons express steroid binding proteins and nuclear receptors. Some binding globulins were found also in single ciliated cells of the non-sensory vomeronasal epithelium. Immunoelectron microscopy revealed VDR in olfactory microvilli and DPB in apical membrane protrusions of supporting sells within the sensory epithelium. Pilot behavioral studies with dogs showed increased sniffing duration upon exposure to low concentrations of vitamin D while higher concentrations were less effective...
September 26, 2017: Steroids
Luca F Castelnovo, Valerio Magnaghi, Peter Thomas
The role played by progestogens in modulating Schwann cell pathophysiology is well established. Progestogens exert their effects in these cells through both classical genomic and non-genomic mechanisms, the latter mediated by the GABA-A receptor. However, there is evidence that other receptors may be involved. Membrane progesterone receptors (mPRs) are novel 7-transmembrane receptors coupled to G proteins that have been characterized in different tissues and cells, including the central nervous system (CNS)...
September 26, 2017: Steroids
Su Yi Loh, Nelli Giribabu, Naguib Salleh
We hypothesized that testosterone-induced increase in blood pressure involve changes in aldosterone levels and expression of epithelial sodium channel (ENaC) in the kidneys. METHODS: Ovariectomized female normotensive Wistar Kyoto (WKY) and Spontaneous hypertensive (SHR) rats were given six weeks treatment with testosterone via subcutaneous silastic implant. The rats were anesthetized and mean arterial pressure (MAP) was measured via direct cannulation of the carotid artery. Animals were sacrificed and kidneys were removed and subjected for α, β and γ-ENaC protein and mRNA expression analyses by Western blotting and Real-time polymerase chain reaction (qPCR), respectively...
September 24, 2017: Steroids
Balbina J Plotkin, Monika I Konakieva
Upon entering the human host, Staphylococcus aureus is exposed to endogenous steroid hormones. The interaction between S. aureus and dehydroepiandosterone (DHEA) results in an increased resistance to the host cationic defense peptide, β-1 defensin, as well as vancomycin and other antibiotics that have a positive charge. The increased resistance to vancomycin is phenotypic and appears to correlate with a DHEA-mediated alteration in cell surface architecture. DHEA-mediated cell surface changes include alterations in: cell surface charge, surface hydrophobicity, capsule production, and carotenoid production...
September 23, 2017: Steroids
Lanlan Chen, Xiaomin Chen, Xiaozhen Chen, Zhiyan Hu, Xiaoheng Li, Ying Su, Xingwang Li, Ren-Shan Ge
Placenta produces progesterone and estradiol for maintaining pregnancy. Two critical enzymes are responsible for their production: 3β-hydroxysteroid dehydrogenase 1 (HSD3B1) that catalyzes the formation of progesterone from pregnenolone and aromatase that catalyzes the production of estradiol from testosterone. Fungicide ziram may disrupt the placental steroid production. In the present study, we investigated the effects of ziram on steroid formation in human placental cell line JEG-3 cells and on HSD3B1 and aromatase in the human placenta...
September 23, 2017: Steroids
Grant L Weiss, Jennifer R Rainville, Qi Zhao, Jeffrey G Tasker
Cellular effects of glucocorticoids can be separated into classical transcriptional regulation via activation of the canonical nuclear glucocorticoid receptor and rapid actions mediated by activation of one or more putative membrane-associated glucocorticoid receptors that regulate both transcriptional and non-transcriptional signaling. Dexamethasone-bovine serum albumin (Dex-BSA), is one of several membrane-limited steroid receptor agonists. Dex-BSA and other steroid conjugates such as corticosterone-, estradiol- and testosterone-BSA have been used to study rapid steroid effects initiated by a putative membrane receptor...
September 19, 2017: Steroids
Patrizia Ferraboschi, Maria Chiara Sala, Riccardo Stradi, Laura Ragonesi, Clarissa Gagliardi, Paolo Lanzarotti, Enzio M Ragg, Matteo Mori, Fiorella Meneghetti
Cortexolone-17α-propionate (CP) is a topically active antiandrogen useful in the treatment of skin disorders. In the solid state, three anhydrous forms of this drug (CPI, CPII and CPIII) occurr, together with one hydrated crystal (CPW). The single crystal structure of the monohydrated phase, CPW, compared with that of the anhydrous form CPIII, shows a markedly different solid state behavior. These latter pseudopolymorphic forms have also been fully characterized by spectroscopic methods.
September 15, 2017: Steroids
Xinliang Liu, Dehong Sun, Xiaosong Ma, Chuansheng Li, Jie Ying, Youde Yan
The efficacy, safety and health-economic outcomes were compared between corticosteroid and non-corticosteroid treatments in acute gout patients. All electronic literatures comparing the curative effects or full economic evaluations of corticosteroids versus non-corticosteroids on acute pain in acute gout patients and published until June 30, 2017 in any language were searched through PubMed, EMBASE, Web of Science, and Cochrane Central Register of Controlled Trials. Pooled odds ratios with 95% confidence intervals and standard(or weighted) mean difference were calculated using random-or fixed-effects models according to the I(2) statistic test of heterogeneity...
September 9, 2017: Steroids
Laura V de Vries, Wilhelmina H A de Jong, Daan J Touw, Stefan P Berger, Gerjan Navis, Ido P Kema, Stephan J L Bakker
Chronic prednisolone treatment in renal transplant recipients (RTR) causes metabolic abnormalities, which cluster in the metabolic syndrome (MS). It also suppresses the hypothalamic-pituitaryadrenal (HPA)-axis. We investigated whether HPA-axis suppression, as measured by 24h urinary cortisol excretion, is associated with presence of the MS and its individual components, in outpatient RTR with a functioning graft for >1year. Urinary cortisol was measured in 24h urine, using LC-MS/MS (LOQ 0.30nmol/L). We included 563 RTR (age 51±12years; 54% male) at median 6...
September 8, 2017: Steroids
Takeshi Iwasa, Toshiya Matsuzaki, Mayila Yiliyasi, Kiyohito Yano, Minoru Irahara
Previously, we showed that chronic testosterone administration increased body weight (BW) and food intake (FI), but did not alter fat weight, in young female rats. To examine our hypothesis that the effects of androgens on BW, FI and body composition might be age-dependent, the effects of chronic testosterone administration were evaluated in rats of different ages; i.e., young and middle-aged rats. Although chronic testosterone administration increased BW gain, FI, and feed efficiency in both young and middle-aged rats, it increased visceral fat weight in middle-aged rats, but not in young rats...
September 8, 2017: Steroids
Manuel A Ramos-Enríquez, Katherine Vargas-Romero, Lucie Rárová, Miroslav Strnad, Martín A Iglesias-Arteaga
Benzylidenespirostanols were prepared by two-step synthesis including BF3·Et2O-catalyzed aldol condensation of several acetylated steroid sapogenins with benzaldehyde followed by saponification. The obtained compounds showed moderate cytotoxicity against three cancer cell lines (T-lymphoblastic leukemia cell line CEM, breast carcinoma cell line MCF7 and cervical carcinoma cell line HeLa) and normal human fibroblasts (BJ). The most active of the five tested substances was 3c (lowest IC50 for MCF7 cells 19.9±0...
September 5, 2017: Steroids
Izabella Jastrzebska, Jacek W Morzycki
This article presents new transformations of solasodine - a representative steroid alkaloid sapogenin from the Solanum family. Oxidation of N,O-diacetylated solasodine with either NaNO2/BF3·Et2O or t-BuONO/BF3·Et2O resulted in partial degradation of the side chain to (20S)-3β-acetoxypregn-5-ene-20,16β-carbolactone (vespertilin acetate). The same starting compound when treated with TMSOTf afforded the corresponding pseudosapogenin after aqueous work-up. However, when the crude reaction mixture was directly subjected to purification on a silica gel column, efficient autoxidation to pregna-5,16-dien-3β-ol-20-one acetate was observed...
September 5, 2017: Steroids
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