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steroid synthesis

G Saito, D Velluto, M Resmini
In this work, we report the synthesis of novel fluorescent molecules, based on 1,8-naphthalimide thio- and amino-derivatives, designed to display an OFF-ON and ON-OFF photoelectron transfer fluorescence switch upon interaction with a proton-donor drug. We have functionalized the new probes to allow easy formation of a covalent link to polymer matrices, for future applications as drug delivery sensors. We have investigated the fluorescent switch of the new probes using flufenamic acid (FA, pKa 3.65), a water insoluble, non-steroidal anti-inflammatory drug, as a model drug and proton source...
June 2018: Royal Society Open Science
Mina Kim, Young Sil Min, Uy Dong Sohn
Indomethacin is a non-steroidal anti-inflammatory drug with clearly known side effects on the gastrointestinal tract. The purpose of the present study was to investigate whether eupatilin inhibit cell injury induced by indomethacin in cultured feline esophageal epithelial cells (EECs). EECs were used to investigate the ability of eupatilin to induce the expression of heat shock proteins (HSP27 and HSP70) and analyze its cytoprotective effect against indomethacin-induced damage. The treatment of EECs with indomethacin for 8 h decreased cell viability...
August 14, 2018: Archives of Pharmacal Research
Maxim D Seferovic, Christine A Beamish, Rockann E Mosser, Shannon E Townsend, Kirk Pappan, Vincent Poitout, Kjersti Aagaard, Maureen Gannon
Pancreatic β-cell expansion is a highly regulated metabolic adaptation to increased somatic demands, including obesity and pregnancy; adult β-cells otherwise rarely proliferate. We previously showed that high fat diet (HFD) feeding induces mouse β-cell proliferation in less than one week in the absence of insulin resistance. Here we metabolically profiled tissues from a short-term HFD β-cell expansion mouse model to identify pathways and metabolite changes associated with β-cell proliferation. Mice fed HFD vs CD showed a 14...
August 14, 2018: American Journal of Physiology. Endocrinology and Metabolism
Kathryn Wilsterman, Neta Gotlieb, Lance J Kriegsfeld, George E Bentley
Stress-induced glucocorticoid release is thought to be a primary driver by which maternal stress negatively impacts pregnancy outcomes, but the neuroendocrine targets mediating these adverse outcomes are less well understood. We hypothesized that stress-induced glucocorticoid secretion influences pituitary hormone secretion, resulting in altered ovarian progesterone synthesis. Using a chronic restraint model of stress in mice, we quantified pituitary hormones, steroid hormone production, and expression of ovarian genes that support progesterone production at both early- (day 5) and mid-pregnancy (day 10)...
August 14, 2018: American Journal of Physiology. Endocrinology and Metabolism
Olga V Fedorova, Valentina V Ishkaraeva, Yulia N Grigorova, Vitaly A Reznik, Nikolai I Kolodkin, Irina E Zazerskaya, Valentina Zernetkina, Natalia I Agalakova, Natalia I Tapilskaya, C David Adair, Edward G Lakatta, Alexei Y Bagrov
BACKGROUND: Previous studies implicated cardiotonic steroids, including Na/K-ATPase inhibitor marinobufagenin (MBG), in the pathogenesis of preeclampsia (PE). Immunoneutralization of heightened MBG by Digibind, a digoxin antibody, reduces blood pressure (BP) in patients with PE, and anti-MBG monoclonal antibody lessens BP in a rat model of PE. Recently, we demonstrated that MBG induces fibrosis in cardiovascular tissues via a mechanism involving inhibition of Fli-1, a nuclear transcription factor and a negative regulator of collagen-1 synthesis...
August 13, 2018: International Journal of Molecular Sciences
Sampada Kallol, Xiao Huang, Stefan Müller, Corneille Edgar Ontsouka, Christiane Albrecht
Cholesterol is indispensable for cellular membrane composition and function. It is also a precursor for the synthesis of steroid hormones, which promote, among others, the maturation of fetal organs. A role of the ATP-binding-cassette-transporter-A1 (ABCA1) in the transport of maternal cholesterol to the fetus was suggested by transferring cholesterol to apolipoprotein-A-1 (apo-A1), but the directionality of the apoA-1/ABCA1-dependent cholesterol transport remains unclear. We isolated primary trophoblasts from term placentae to test the hypotheses that (1) apoA-1/ABCA1 dispatches cholesterol mainly towards the fetus to support fetal developmental maturation at term, and (2) differentiated syncytiotrophoblasts (STB) exert higher cholesterol transport activity than undifferentiated cytotrophoblasts (CTB)...
August 9, 2018: International Journal of Molecular Sciences
Cedric Shackleton, Oscar J Pozo, Josep Marcos
Gas chromatography/mass spectrometry (GC/MS) has been used for steroid analysis since the 1960s. The advent of protective derivatization, capillary columns, and inexpensive electron ionization bench-top single quadrupole soon made it the method of choice for studying disorders of steroid synthesis and metabolism. However, the lengthy sample workup prevented GC/MS from becoming routine for steroid hormone measurement, which was dominated by radioimmunoassay. It was the emergence of liquid chromatography/tandem MS (LC/MS/MS) that sparked a renewed interest in GC/MS for the multicomponent analysis of steroids...
August 1, 2018: Journal of the Endocrine Society
Majorie B M van Duursen
Phytoestrogens are increasingly used as dietary supplements due to their suggested health promoting properties, but also by women for breast enhancement and relief of menopausal symptoms. Generally, phytoestrogens are considered to exert estrogenic activity via estrogen receptors (ERs), but they may also affect estrogen synthesis and metabolism locally in breast, endometrial and ovarian tissues. Considering that accurate regulation of local hormone levels is crucial for normal physiology, it is not surprising that interference with hormonal synthesis and metabolism is associated with a wide variety of women's health problems, varying from altered menstrual cycle to hormone-dependent cancers...
November 1, 2017: Toxicology Research
Lianne Pope, Cristina Arrigoni, Hubing Lou, Clifford Bryant, Alejandra Gallardo-Godoy, Adam R Renslo, Daniel L Minor
K2P potassium channels generate leak currents that stabilize the resting membrane potential of excitable cells. Various K2Ps are implicated in pain, ischemia, depression, migraine, and anesthetic responses, making this family an attractive target for small molecule modulator development efforts. BL-1249, a compound from the fenamate class of non steroidal anti inflammatory drugs is known to activate K2P2.1 (TREK-1), the founding member of the thermo- and mechanosensitive TREK subfamily; however, its mechanism of action and effects on other K2Ps are not well-defined...
August 8, 2018: ACS Chemical Neuroscience
Vivaswath S Ayyar, Siddharth Sukumaran, Debra C DuBois, Richard R Almon, William J Jusko
Corticosteroids (CS) regulate the expression of numerous genes at the mRNA and protein levels. The time-course of CS pharmacogenomics and proteomics were examined in livers obtained from adrenalectomized rats given a 50 mg/kg bolus dose of methylprednisolone. Microarrays and mass-spectrometry based proteomics were employed to quantify hepatic transcript and protein dynamics. A total of 163 differentially expressed mRNA and their corresponding proteins (163 genes) were clustered into two dominant groups. The temporal profiles of most proteins were delayed compared to its mRNA, attributable to synthesis delays and slower degradation kinetics...
August 7, 2018: Journal of Pharmacology and Experimental Therapeutics
Maria Elvira Brocca, Luis Miguel Garcia-Segura
The modulation of brain function and behavior by steroid hormones was classically associated with their secretion by peripheral endocrine glands. The discovery that the brain expresses the enzyme aromatase, which produces estradiol from testosterone, expanded this traditional concept. One of the best-studied roles of brain estradiol synthesis is the control of reproductive behavior. In addition, there is increasing evidence that estradiol from neural origin is also involved in a variety of non-reproductive functions...
August 6, 2018: Cellular and Molecular Neurobiology
Arshia, Almas Jabeen, Aisha Faheem, Khalid Mohammed Khan, Shazia Shah, Shahnaz Perveen
BACKGROUND: Inflammation is a biological rejoinder of vascular tissues against destructive agents e.g. irritants, damaged cell or pathogens. During inflammation respiratory burst occur by activated phagocytes helps to destroy invading pathogens. Phagocytic cells such as neutrophils and macrophages are one of the major sources of reactive oxygen species (ROS) and nitric oxide (NO). Normally the redox environment is maintained by various antioxidant defense systems, however, these reactive oxygen species may be destructive and can lead to various pathological conditions...
August 5, 2018: Medicinal Chemistry
Christine E Peek, Rachel E Cohen
Steroid hormones, such as testosterone and estradiol, are necessary for reproductive behavior. Seasonally breeding animals have increased sex steroid hormone levels during the breeding compared to non-breeding season, with increased reproductive behaviors and altered brain morphology in breeding individuals. Similar to other seasonally breeding animals, green anole lizards (Anolis carolinensis) have high sex steroid hormone levels and increased reproductive behaviors in the breeding season. Relatively less is known regarding the regulation of steroidogenesis in reptiles and this experiment examined whether enzymes involved in sex steroid hormone synthesis vary seasonally within the brain and gonads in wild-caught anole lizards...
August 2, 2018: General and Comparative Endocrinology
Giuseppe Dilauro, Sergio Mata García, Donato Tagarelli, Paola Vitale, Filippo M Perna, Vito Capriati
Pd-catalysed Suzuki-Miyaura cross-couplings between (hetero)aryl halides (Cl, Br, I) and versatile, moisture-stable mono- and bifunctional potassium aryltrifluoroborates proceed efficiently and chemoselectively in air and under generally mild conditions, with a catalyst loading as low as 1 mol%, in the absence of additional ligands, and employing Na2CO3 as base, and the deep eutectic solvent (DES) choline chloride/glycerol (1:2) as a sustainable and environmentally responsible medium. Catalyst, base and DES have been easily and successfully recycled up to six times with an E-factor as low as 8...
August 3, 2018: ChemSusChem
Li Cheng, Lin Li, Liling Wang, Xiaofang Li, Hui Xing, Jinting Zhou
Ovarian cancer (OC) is associated with a poor prognosis due to difficulties in early detection. The aims of the present study were to construct a recurrence risk prediction model and to reveal important OC genes or pathways. RNA sequencing data was obtained for 307 OC samples, and the corresponding clinical data were downloaded from The Cancer Genome Atlas database. Additionally, two validation datasets, GSE44104 (20 recurrent and 40 non‑recurrent OC samples) and GSE49997 (204 OC samples), were obtained from the Gene Expression Omnibus database...
July 19, 2018: Molecular Medicine Reports
Anant Kapdi, Yogesh G Shelke, Afsana Yashmeen, Aniket V A Gholap, Santosh J Gharpure
Homogeneous catalysis has played an important and a ubiquitous role in the synthesis of simple to complex molecules ranging from drugs, natural products to agrochemicals. The wide-reaching importance of homogeneous catalysis in recent years has also made it an indispensable tool for the modification of bio molecules such as carbohydrates (sugars), amino acids, peptides, nucleosides, nucleotides and steroids. Such a synthetic strategy provides researchers with several advantages leading to the development of molecules of biological relevance at a rapid rate compared to the available synthetic protocols...
July 31, 2018: Chemistry, An Asian Journal
Ivan S Golovanov, Galina S Mazeina, Yulia V Nelyubina, Roman A Novikov, Anton S Mazur, Sergey N Britvin, Vladimir A Tartakovsky, Sema L Ioffe, Alexey Yu Sukhorukov
Click-like condensation of boronic acids with specifically designed triols (boronate-triol coupling) produces stable diamantane adducts in aqueous medium, which can be controllably cleaved to initial components under acidic conditions or by using boric acid as a chemical trigger. This novel "click-declick" strategy allows to create temporary covalent connections between two or more modular units that was demonstrated by the synthesis of new fluorophore-labeled natural molecules (peptides, steroids), supramolecular assemblies, modified polymers, boronic acid scavengers, solid-supported organocatalysts, biodegradable COF-like materials and dynamic combinatorial libraries...
July 31, 2018: Journal of Organic Chemistry
Davide M Dominoni, Maaike de Jong, Michelle Bellingham, Peter O'Shaughnessy, Kees van Oers, Jane Robinson, Bethany Smith, Marcel E Visser, Barbara Helm
Artificial light at night (ALAN) is increasingly recognized as a potential threat to wildlife and ecosystem health. Among the ecological effects of ALAN, changes in reproductive timing are frequently reported, but the mechanisms underlying this relationship are still poorly understood. Here, we experimentally investigated these mechanisms by assessing dose-dependent photoperiodic responses to ALAN in the great tit (Parus major). We individually exposed photosensitive male birds to one of three nocturnal light levels (0...
July 29, 2018: Journal of Experimental Zoology. Part A, Ecological and Integrative Physiology
Yan Zhang, Yu Wang, Can Huang, Yi Wang, Hongyu Qi, Yingying Han, Zhengrong Yuan, Qiang Weng, Haolin Zhang
The prostate gland is a male accessory reproductive gland that requires androgenic steroids for maintaining its vitality and function. The aim of the study was to investigate the localization and expressions of the androgen receptor (AR), SRD5A1 and SRD5A2 in the prostate glands of wild male ground squirrels during different reproductive periods by immunohistochemistry and real-time PCR. Gross mass of the prostate gland was higher in the breeding season than that of the non-breeding season. Histological observation showed that exocrine lumens in the prostate gland were enlarged in the breeding season and shrank in the non-breeding season...
July 2, 2018: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
Maria Ginalska-Malinowska
Congenital adrenal hyperplasia (CAH) is a group of autosomal recessive disorders characterized by impaired cortisol synthesis. The most common form of CAH is caused by mutations in CYP21A, the gene encoding the adrenal steroid 21-hydroxylase enzyme. Deficiency of the enzyme leads to life-threatening adrenocortical insufficiency, which is not demonstrable during the first days of life. Additionally, some of the affected neonates have varying degrees of pathology of the external genitalia, classified as disorders of sex development (DSD)...
2018: Developmental Period Medicine
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