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Novel Steroid

Klaudia Barabás, Soma Godó, Ferenc Lengyel, Dávid Ernszt, József Pál, István M Ábrahám
Although rapid effects of steroid hormones on membrane receptors and intracellular signaling molecules have been extensively studied in neurons, we are only beginning to understand the molecular mechanisms behind these non-classical steroid actions. Single molecule tracking (SMT) studies on live cells demonstrated that surface trafficking of membrane receptors determines their ligand binding properties and downstream signaling events. Recent findings suggest that one of the underlying mechanisms of non-classical steroid actions is the alteration of receptor movements on the membrane surface...
May 15, 2018: Hormones and Behavior
B L Youngblood, Y Ueyama, W W Muir, G M Belfort, R H Hammond, J Dai, F G Salituro, A J Robichaud, J J Doherty
BACKGROUND: Different levels of consciousness are required in order to perform different medical procedures. Sedation scales established to objectively define various levels of sedation in humans have not been thoroughly characterized in non-human species. Postural changes in rats or dogs are useful as gross measures of sedation but are inadequate for quantitative assessment since graded levels of sedation are difficult to delineate and obscured by movement abnormalities. NEW METHOD: A new canine sedation scoring (CSS) method was developed based on the modified observer's assessment of alertness and sedation score (MOAA/S) used in humans...
May 14, 2018: Journal of Neuroscience Methods
Nora Al-Kazaale, Phuong T Tran, Farhad Haidari, Eirik Johansson Solum, Sandra Liekens, Peter Vervaeke, Ingebrigt Sylte, Jing-Jy Cheng, Anders Vik, Trond Vidar Hansen
The endogenous steroid 2-methoxyestradiol (1) has attracted a great interest as a lead compound towards the development of new anti-cancer drugs. Herein, the synthesis, molecular modeling, anti-proliferative and anti-angiogenic effects of ten 2-ethyl and four 2-methoxy analogs of estradiol are reported. The ethyl group was introduced to the steroid A-ring using a novel Friedel-Crafts alkylation protocol. Several analogs displayed potent anti-proliferative activity with IC50 -values in the submicromolar range towards the CEM human leukemia cancer cell line...
May 14, 2018: Steroids
Ajeet Kumar Singh, Sanjay Kumar, Manjula Vinayak
INTRODUCTION: Pain is an unpleasant sensation triggered by noxious stimulation. It is one of the most prevalent conditions, limiting productivity and diminishing quality of life. Non steroidal anti inflammatory drugs (NSAIDs) are widely used as pain relievers in present day practice as pain is mostly initiated due to inflammation. However, due to potentially serious side effects, long term use of these antihyperalgesic drugs raises concern. Therefore there is a demand to search novel medicines with least side effects...
May 16, 2018: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
Paul A Foster, Jonathan Wolf Mueller
Sulfation and desulfation pathways represent highly dynamic ways of shuttling, repressing and re-activating steroid hormones, thus controlling their immense biological potency at the very heart of endocrinology. This theme currently experiences growing research interest from various sides, including, but not limited to, novel insights about PAPS synthase and sulfotransferase function and regulation, novel analytics for steroid conjugate detection and quantification. Within this review, we will also define how sulfation pathways are ripe for drug development strategies, which have translational potential to treat a number of conditions, including chronic inflammatory diseases and steroid-dependent cancers...
May 15, 2018: Journal of Molecular Endocrinology
Chanatda Worawit, David J Cocovi-Solberg, Pakorn Varanusupakul, Manuel Miró
A novel concept for automation of nanostructured hollow-fiber supported microextraction, combining the principles of liquid-phase microextraction (LPME) and sorbent microextraction synergically, using mesofluidic platforms is proposed herein for the first time, and demonstrated with the determination of acidic drugs (namely, ketoprofen, ibuprofen, diclofenac and naproxen) in urine as a proof-of-concept applicability. Dispersed carbon nanofibers (CNF) are immobilized in the pores of a single-stranded polypropylene hollow fiber (CNF@HF) membrane, which is thereafter accommodated in a stereolithographic 3D-printed extraction chamber without glued components for ease of assembly...
August 1, 2018: Talanta
Yang Ouyang, Hongbin Tong, Ping Luo, Hongwei Kong, Zhiliang Xu, Peiyuan Yin, Guowang Xu
Periodical changes of steroid hormones have a great impact on the homeostasis of the female. However, there are few studies concerning the metabolome changes during the cycle. To study the periodic metabolic changes, a female cohort was enrolled with time-series serum samples collected during a menstrual cycle. To meet the requirement of the large-scale sample analysis, a high throughput metabolomics method was established by using an efficient sample preparation on a 96 well filter plate and a rapid LC condition in 12 min, which reduces about 70% of the samples preprocessing time and 60% analysis time...
August 1, 2018: Talanta
Ratchanok Pingaew, Veda Prachayasittikul, Nuttapat Anuwongcharoen, Supaluk Prachayasittikul, Somsak Ruchirawat, Virapong Prachayasittikul
A three series of thioureas, monothiourea type I (4a-g), 1,4-bisthiourea type II (5a-h) and 1,3-bisthiourea type III (6a-h) were synthesized. Their aromatase inhibitory activities have been evaluated. Interestingly, eight thiourea derivatives (4e, 5f-h, 6d, 6f-h) exhibited the aromatase inhibitory activities with IC50 range of 0.6-10.2 μM. The meta-bisthiourea bearing 4-NO2 group (6f) and 3,5-diCF3 groups (6h) were shown to be the most potent compounds with sub-micromolar IC50 values of 0.8 and 0.6 μM, respectively...
May 4, 2018: Bioorganic Chemistry
Satheesh Kumar Palanisamy, Velusamy Arumugam, Magesh D Peter, Umamaheswari Sundaresan
The complex nature of marine biodiversity is partially responsible for the lack of studies in Indian ascidian species, which often target a small number of novel biomolecules. We performed untargeted metabolomics using gas chromatography-mass spectrometry (GC-MS) in two invasive ascidian species to investigate the inter-specific chemical diversity of Phallusia nigra and P. arabica in search of drug-like properties and metabolic pathways. The chemical profiling of individual ascidian species was obtained using GC-MS, and the metabolites were determined by searching in NIST library and literature data...
May 2018: 3 Biotech
Yufang Liu, Jibin Zhang, Qiao Xu, Xiaolong Kang, Kejun Wang, Keliang Wu, Meiying Fang
BACKGROUND: Tan sheep is an indigenous Chinese breed well known for its beautiful curly fleece. One prominent breed characteristic of this sheep breed is that the degree of curliness differs markedly between lambs and adults, but the molecular mechanisms regulating the shift are still not well understood. In this study, we identified 49 differentially expressed (DE) microRNAs (miRNAs) between Tan sheep at the two stages through miRNA-seq, and combined the data with that in our earlier Suppression Subtractive Hybridization cDNA (SSH) library study to elucidate the mechanisms underlying curly fleece formation...
May 11, 2018: BMC Genomics
Maria G Belvisi, Katie Baker, Nicole Malloy, Kristof Raemdonck, Bilel Dekkak, Michael Pieper, Anthony T Nials, Mark A Birrell
BACKGROUND: Asthmatics that are exposed to inhaled pollutants such as cigarette smoke (CS) have increased symptom severity. Approximately 25% of adult asthmatics are thought to be active smokers and many sufferers, especially in the third world, are exposed to high levels of inhaled pollutants. The mechanism by which CS or other airborne pollutants alter the disease phenotype and the effectiveness of treatment in asthma is not known. The aim of this study was to determine the impact of CS exposure on the phenotype and treatment sensitivity of rodent models of allergic asthma...
May 10, 2018: Respiratory Research
Cinthia Gallegos, Farrell Tobowlosky, Masayuki Nigo, Rodrigo Hasbun
OBJECTIVES: To report the prevalence of delayed cerebral injury in adults with bacterial meningitis and explore its association with adjunctive steroids. DESIGN: Retrospective analysis of adults with bacterial meningitis between 2005 and 2016. SETTING: Ten hospitals in the Greater Houston area. PATIENTS: Consecutive subjects with culture proven community-acquired bacterial meningitis. INTERVENTION: Subjects were categorized as receiving or not adjunctive steroids within 4 hours...
May 9, 2018: Critical Care Medicine
Rui Liu, Pengfei Zhao, Wenfeng Tan, Miaojia Zhang
Rheumatoid arthritis (RA), an autoimmune disease, is characterised by a persistent synovitis in the joints and systemic inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs), corticosteroids and disease-modifying antirheumatic drugs (DMARDs) are widely used to treat RA patients. However, a portion of patients still have inadequate response to traditional medications. Recently, cell-based therapies have become the focus, attracting more attention due to their potential for remission induction. Several immune-regulatory cell types, such as haematopoietic stem cells, mesenchymal stem cells and regulatory T cells have been defined as novel targets...
May 8, 2018: Clinical and Experimental Rheumatology
Sara De Iudicibus, Marianna Lucafò, Nicola Vitulo, Stefano Martelossi, Rosanna Zimbello, Fabio De Pascale, Claudio Forcato, Samuele Naviglio, Alessia Di Silvestre, Marco Gerdol, Gabriele Stocco, Giorgio Valle, Alessandro Ventura, Matteo Bramuzzo, Giuliana Decorti
The aim of this research was the identification of novel pharmacogenomic biomarkers for better understanding the complex gene regulation mechanisms underpinning glucocorticoid (GC) action in paediatric inflammatory bowel disease (IBD). This goal was achieved by evaluating high-throughput microRNA (miRNA) profiles during GC treatment, integrated with the assessment of expression changes in GC receptor (GR) heterocomplex genes. Furthermore, we tested the hypothesis that differentially expressed miRNAs could be directly regulated by GCs through investigating the presence of GC responsive elements (GREs) in their gene promoters...
May 8, 2018: International Journal of Molecular Sciences
Ayami Matsushima
Huge numbers of chemicals are released uncontrolled into the environment and some of these chemicals induce unwanted biological effects, both on wildlife and humans. One class of these chemicals are endocrine-disrupting chemicals (EDCs), which are released even though EDCs can affect not only the functions of steroid hormones but also of various signaling molecules, including any ligand-mediated signal transduction pathways. Dichlorodiphenyltrichloroethane (DDT), a pesticide that is already banned, is one of the best-publicized EDCs and its metabolites have been considered to cause adverse effects on wildlife, even though the exact molecular mechanisms of the abnormalities it causes still remain obscure...
May 5, 2018: International Journal of Molecular Sciences
Adriana Carol Eleonora Graziano, Giovanna Pannuzzo, Ettore Salemi, Andrea Santagati, Rosanna Avola, Emanuele Longo, Venera Cardile
The present study reports the synthesis, molecular docking and biological evaluation of eight (5-8 and 5a-8a) newly synthesized thieno-pyrimidinone methanesulphonamide thio-derivatives. The synthetic route used to prepare the new isomers thioaryl and thio-cycloesyl derivatives of the heterocyclic system 6-phenylthieno[3,2]pyrimidinone was economically and environmentally very advantageous and characterized by the simplicity of procedure, reduction of isolation steps, purification phases, time, costs, and waste production...
May 7, 2018: Clinical and Experimental Pharmacology & Physiology
Kate Laycock, Abhijit Chaudhuri, Charlotte Fuller, Zahra Khatami, Frederick Nkonge, Nemanja Stojanovic
Hashimoto's encephalopathy (HE) is rarely reported with only a few hundred cases published. Diagnosis is made in patients with an appropriate clinical picture and high antithyroperoxidase (anti-TPO) antibodies after infectious, toxic and metabolic causes of encephalopathy have been excluded. There is little objective data on the neurocognitive impairment in patients with HE and their improvement with treatment. We present the case of a 28-year-old woman with HE. Approach to management was novel as objective neuropsychological assessment was used to assess her clinical condition and response to treatment...
2018: Endocrinology, Diabetes & Metabolism Case Reports
Yudan Wang, Yang Zhang, Jianan Cui, Shuo Li, Ming Yuan, Ting Wang, Qi Hu, Xiaohong Hou
A series of novel MOFs/PVA composite cryogel (MIL-101(Cr)/PVA, MIL-100(Fe)/PVA, ZIF-8(Zn)/PVA, MOF-199(Cu)/PVA and MIL-53(Al)/PVA) were fabricated by using a facile and green freeze-thaw approach for the first time. MIL-101(Cr)/PVA cryogel was selected as a VA-SPE sorbent for extraction of four NSAIDs in environmental water samples. The procedures of condition investigation (synthesis and extraction optimization) and characterization were also performed. And a satisfactory result of methodology validation was obtained by making use of HPLC-MS/MS...
August 31, 2018: Analytica Chimica Acta
Wei Lu, Xi Chen, Jinhui Feng, Yun-Juan Bao, Yu Wang, Qiaqing Wu, Dunming Zhu
In this study, we identified a P450 enzyme (STH10) and an oxidoreductase (POR) from Thanatephorus cucumeris NBRC 6298 by a combination of transcriptome sequencing and heterologous expression in Pichia pastoris The biotransformation of 11-deoxycortisol was performed by using the Pichia pastoris whole cells co-expressing sth10 and por , and the product analysis indicated that the STH10 enzyme possessed steroidal 19- and 11β-hydroxylase activities. This is a novel fungal P450 enzyme with 19-hydroxylase activity, which is different from the known steroidal aromatase CYP19 and CYP11B families of enzymes...
May 4, 2018: Applied and Environmental Microbiology
Manabu Kawata, Yusuke Sasabuchi, Shuji Taketomi, Hiroshi Inui, Hiroki Matsui, Kiyohide Fushimi, Hideo Yasunaga, Sakae Tanaka
PURPOSE: Although various risk factors for surgical site infection after anterior cruciate ligament reconstruction (ACLR) have been reported, the number of studies with large sample sizes on this topic is limited. The aim of the present study was to clarify the risk factors for early surgical site infection after ACLR in a large cohort using a national database in Japan. METHODS: The data of patients who underwent ACLR from 2010 to 2015 were obtained from the Diagnosis Procedure Combination database, which covers approximately half of all hospital admissions in Japan...
May 3, 2018: Knee Surgery, Sports Traumatology, Arthroscopy: Official Journal of the ESSKA
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