Estrogen Matters in Metastasis
Publication date: Available online 20 July 2018Source: SteroidsAuthor(s): Shardool Nair, Geetanjali SachdevaAbstractMetastatic cancer cells meet several physical, biochemical and immunological barriers before colonizing a new territory. Cancerous cells turn invasive, mobile and eventually disengage from their native niche. This is followed by their intravasation, extravasation, survival, proliferation, and colonization into distant organs. Unlike well-confined tumors, which respond favorably to anti-cancer therapeutics, metastatic tumors are life-threatening and incurable. More than 90% of cancer-related mortality is cause...
Source: Steroids - July 20, 2018 Category: Drugs & Pharmacology Source Type: research

Crystal structures and Hirshfeld surface analyses of the hemi-hydrate and hemi-methanolate of 3α-hydroxy-16α-bromoandrostan-17-one, 3: differences in supramolecular arrangements
Publication date: Available online 20 July 2018Source: SteroidsAuthor(s): Ligia R. Gomes, John N Low, Alan B Turner, James L. WardellAbstractThe crystal structures and Hirshfeld surface analyses of two hemi-solvates of 3α-hydroxy-16α-bromoandrostan-17-one, 3, namely [(3)2.(H2O)] and [(3)2.(MeOH)], are reported. Both solvates crystallize in the monoclinic space group, P21, with Z = 4.. The asymmetric unit of the hemi-hydrate [(3)2.(H2O)] contains two independent but similar steroid molecules and a water molecule, while that of the hemi-methanoate [(3)2.(MeOH)] has four similar but independent steroid molecules a...
Source: Steroids - July 20, 2018 Category: Drugs & Pharmacology Source Type: research

3,20-Dihydroxy-13α-19-norpregna-1,3,5(10)-trienes. synthesis, structures, and cytotoxic, estrogenic, and antiestrogenic effects
Publication date: Available online 20 July 2018Source: SteroidsAuthor(s): Yury V. Kuznetsov, Inna S. Levina, Alexander M. Scherbakov, Olga E. Andreeva, Andrey S. Dmitrenok, Oleg R. Malyshev, Igor V. ZavarzinAbstractNew 3,20-dihydroxy-13α-19-norpregna-1,3,5(10)-trienes were synthesized. The effects of these compounds on breast cancer cells and ERα activation were investigated. The scaffold of compounds containing the six-membered ring D' annulated at 16α,17α-positions was constructed via the Lewis acid catalyzed Diels-Alder reaction of butadiene with 3-methoxy-13α-19-norpregna-1,3,5(10),16-tetr...
Source: Steroids - July 20, 2018 Category: Drugs & Pharmacology Source Type: research

Xenoestrogen interference with nongenomic signaling actions of physiological estrogens in endocrine cancer cells
Publication date: Available online 20 July 2018Source: SteroidsAuthor(s): Cheryl S. Watson, Luke Koong, Yow-Jiun Jeng, Rene VinasAbstractRapid nongenomic signaling by estrogens (Es), initiated near the cell membrane, provides new explanations for the potent actions of environmental chemicals that imperfectly mimic physiological Es. These pathways can affect tumor growth, stabilization, or shrinkage via a number of signaling streams such as activation/inactivation of mitogen-activated protein kinases and caspases, generation of second messengers, and phospho-triggering of cyclin instability. Though prostate cancers are bett...
Source: Steroids - July 20, 2018 Category: Drugs & Pharmacology Source Type: research

Design and semisynthesis of new herbicide as 1,2,3-triazole derivatives of the natural maslinic acid
Publication date: October 2018Source: Steroids, Volume 138Author(s): Aymen Ben Nejma, Mansour Znati, Adam Daich, Mohamed Othman, Ata Martin Lawson, Hichem Ben JannetAbstractInteresting biological activities (anti-inflammatory, anticancer, antiviral, antioxidant, antidiabetic…) have been reported for maslinic acid (MA) and MA-based compounds. In continuation of our previous work on MA, herbicide potential of Tunisian plant extracts and 1,4-triazolyl derivatives of MA, we now wish to report semisynthesis of new MA-based triazole hybrid compounds with herbicide potential. These compounds were synthesized through Cu-cat...
Source: Steroids - July 20, 2018 Category: Drugs & Pharmacology Source Type: research

Estrogen Receptors and Sex Hormone Binding Globulin in neuronal cells and tissue
Publication date: Available online 18 July 2018Source: SteroidsAuthor(s): Veronika M. Gebhart, Jack D. Caldwell, Andrea Rodewald, Konstantina Kalyvianaki, Marilena Kampa, Gustav F. JirikowskiAbstractEstrogens exert a critical influence on neuronal tissues and cells. As demonstrated in many clinical studies, estrogens are neuroprotective to the extent that they improve prognosis for women with neurodegenerative diseases. Unfortunately, we still do not know exactly how these effects are mediated. Fifty years ago the first estrogen receptor was found, but since then many other new pathways of estrogen action have been identif...
Source: Steroids - July 19, 2018 Category: Drugs & Pharmacology Source Type: research

Optimization of the synthesis of a key intermediate for the preparation of glucocorticoids
Publication date: Available online 12 July 2018Source: SteroidsAuthor(s): Romain Jouve, Vincent Thery, Sylvie Ducki, Julie Helfenbein, Jean-Christophe Thiery, Aurélie Job, Elodie Picard, Christophe Mallet, Isabelle Ripoche, Khalil BennisAbstractA short and efficient synthesis, based on a one-step double elimination, of a key intermediate in the synthesis of various glucocorticosteroids has been developed. This method can be carried out on large scale for further industrial applications. The synthesis allowed us to identify a novel prednisolone derivative 10 and its anti-inflammatory activity was determined in an in ...
Source: Steroids - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Purity and stability of the membrane-limited glucocorticoid receptor agonist dexamethasone-BSA
Publication date: Available online 20 September 2017Source: SteroidsAuthor(s): Grant L. Weiss, Jennifer R. Rainville, Qi Zhao, Jeffrey G. TaskerAbstractCellular 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 conjug...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Steroidal pheromones and their potential target sites in the vomeronasal organ
Publication date: Available online 28 September 2017Source: SteroidsAuthor(s): Andrea Rodewald, Daniel Mills, Veronika M. Gebhart, Gustav F. JirikowskiAbstractSteroids 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 wi...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

The expression of select genes necessary for membrane-associated estrogen receptor signaling differ by sex in adult rat hippocampus
Publication date: Available online 28 September 2017Source: SteroidsAuthor(s): John Meitzen, Kyla A. Britson, Krista Tuomela, Paul G. MermelsteinAbstract17β-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 acti...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Expression of membrane progesterone receptors (mPRs) in rat peripheral glial cell membranes and their potential role in the modulation of cell migration and protein expression
Publication date: Available online 28 September 2017Source: SteroidsAuthor(s): Luca F. Castelnovo, Valerio Magnaghi, Peter ThomasAbstractThe 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 n...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of 17β-estradiol on estrogen receptor negative breast cancer cells in an osteolytic mouse model
Publication date: Available online 10 November 2017Source: SteroidsAuthor(s): D. Joshua Cohen, Vaidehi Patel, Anjali Verma, Barbara D. Boyan, Zvi SchwartzAbstract17β-Estradiol (E2) promotes metastasis of triple negative breast cancer cells to bone. Recent studies show many triple negative breast cancer cell lines lacking the 66 kDa estrogen receptor (ER) alpha (ERα66) or its splice variant ERα46, express another splice variant, ERα36 associated with membrane-mediated rapid actions of the hormone. qPCR and western blot confirmed that MCF7 cells possessed ERα splice variants ERα66, ER&alp...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Regulation of extracellular matrix vesicles via rapid responses to steroid hormones during endochondral bone formation
Publication date: Available online 9 December 2017Source: SteroidsAuthor(s): Niels Asmussen, Zhao Lin, Michael J. McClure, Zvi Schwartz, Barbara D. BoyanAbstractEndochondral bone formation is a precise and highly ordered process whose exact regulatory framework is still being elucidated. Multiple regulatory pathways are known to be involved. In some cases, regulation impacts gene expression, resulting in changes in chondrocyte phenotypic expression and extracellular matrix synthesis. Rapid regulatory mechanisms are also involved, resulting in release of enzymes, factors and micro RNAs stored in extracellular matrisomes cal...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Membrane-initiated nuclear trafficking of the glucocorticoid receptor in hypothalamic neurons
Publication date: Available online 12 December 2017Source: SteroidsAuthor(s): Jennifer R. Rainville, Grant L. Weiss, Nathan Evanson, James P. Herman, Nandini Vasudevan, Jeffrey G. TaskerAbstractGlucocorticoid binding to the intracellular glucocorticoid receptor (GR) stimulates the translocation of the GR from the cytosol to the nucleus, which leads to the transactivation or transrepression of gene transcription. However, multiple lines of evidence suggest that glucocorticoid signaling can also be initiated from the plasma membrane. Here, we provide evidence for membrane-initiated glucocorticoid signaling by a membrane-impe...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Three steroid-binding globulins, their localization in the brain and nose, and what they might be doing there
Publication date: Available online 12 December 2017Source: SteroidsAuthor(s): J.D. Caldwell, K. Londe, S.D. Ochs, Z. Hajdu, A. Rodewald, V.M. Gebhart, G.F. JirikowskiAbstractSteroid-binding globulins (SBGs) such as sex hormone binding globulin, corticosteroid binding globulin, and vitamin-D binding protein are receiving increasing notice as being actively involved in steroid actions. This paper reviews data of all three of these SBGs, focusing on their presence and possible activity in the brain and nose. We have found all three proteins in the brain in limbic areas such as the paraventricular (PVN) and supraoptic nuclei (...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Estradiol receptor profile and estrogen responsiveness in laryngeal cancer and clinical outcomes
Publication date: Available online 20 December 2017Source: SteroidsAuthor(s): Nofrat Schwartz, Anjali Verma, Chandana Muktipaty, Caroline Bivens, Zvi Schwartz, Barbara D. BoyanAbstractThere is growing evidence that laryngeal cancers are responsive to sex hormones, specifically 17β-estradiol (E2), despite controversy regarding the presence and characterization of E2 receptors (ER). Determination of sex hormone responsiveness impacts the prognosis of laryngeal cancer patients and the treatment modalities implemented by their clinicians. Discovery of membrane-associated steroid hormone receptors and rapid membrane signal...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Membrane-initiated estrogen signaling via Gq-coupled GPCR in the central nervous system
Publication date: Available online 31 January 2018Source: SteroidsAuthor(s): Gwyndolin Vail, Troy A. RoepkeAbstractThe last few decades have revealed increasing complexity and depth to our knowledge of receptor-mediated estrogen signaling. Nuclear estrogen receptors (ERs) ERα and ERβ remain the fundamental dogma, but recent research targeting membrane-bound ERs urges for a more expanded view on ER signaling. ERα and ERβ are also involved in membrane-delineated signaling alongside membrane-specific G protein-coupled estrogen receptor 1 (GPER1), ER-X, and the Gq-coupled membrane ER (Gq-mER). Membrane ER...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

The response of C19- and some C21-steroids during Synacthen and insulin tolerance test
Publication date: Available online 2 February 2018Source: SteroidsAuthor(s): Kateřina Šimůnková, Michaela Dušková, Lucie Kolatorova, Mikuláš Kosák, Martin Hill, Hana Jandíková, Hana Pospíšilová, Monika Šrámková, Drahomíra Springer, Luboslav StárkaAbstractTesting of the adrenal function with ACTH 1–24 (Synacthen test) or insulin (insulin tolerance test-ITT) is commonly used. The question of ongoing debate is the dose of Synacthen. Moreover, it may be important from the physiological point of view be...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Estrogen receptor-alpha isoforms are the main estrogen receptors expressed in non-small cell lung carcinoma
In conclusion, our data show a wide extranuclear ERα-variant expression in normal lung and NSCLC that is not reported by routine pathology ER evaluation criteria, limited in the nuclear wild type receptor. (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

In memoriam: Mortimer Levitz): Levitz – Mortimer, PhD. (May 11, 1921 to February 7, 2018)
Publication date: Available online 9 May 2018Source: SteroidsAuthor(s): Seth Guller (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Complete androgen insensitivity syndrome caused by c.1769-1G > C mutation and activation of a cryptic splice acceptor site in the androgen receptor gene
Publication date: Available online 31 May 2018Source: SteroidsAuthor(s): Song Wang, Peng Xia, Nicholas A. Cacalano, Haikun Xu, Dejun LiAbstractAndrogen insensitivity syndrome (AIS) is the most common cause of 46,XY disorders of sex development (46,XY DSD). This syndrome is an X-linked recessive genetic disease characterized by resistance to the actions of androgens in an individual with a male karyotype and it is caused by mutations in the androgen receptor (AR) gene. We evaluated two siblings with primary amenorrhea, normal secondary sex characteristics, absence of uterus and ovaries, intra-abdominal testis, and elevated ...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Conjugates of 17-substituted testosterone and epitestosterone with pyropheophorbide a differing in the length of linkers
Publication date: Available online 7 July 2018Source: SteroidsAuthor(s): Vladimir A. Zolottsev, Gelii V. Ponomarev, Maria O. Taratynova, Galina E. Morozevich, Roman A. Novikov, Vladimir P. Timofeev, Pavel N. Solyev, Maria G. Zavialova, Olga V. Zazulina, Yaroslav V. Tkachev, Alexander Y. MisharinAbstractConjugates of 17α-substituted testosterone (1 and 2) and 17β-substituted epitestosterone (3 and 4) with pyropheophorbide a were synthesized. The scheme consisted of synthesis of 17α-hydroxy-3-oxopregn-4-en-21-oic and 17β-hydroxy-3-oxopregn-4-en-21-oic acids, and their coupling with pyropheophorbide a by...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Corticosterone Biosynthesis in Mouse Clonal Myoblastic C2C12 Cells
In conclusion, CORT synthesis occurs in C2C12 cells, and it is suggested that the initial steroidogenesis substrate is the pregnenolone-sulfate conjugate.Graphical abstract (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Cytotoxic steroids from the Vietnamese gorgonian Verrucella corona
Publication date: Available online 7 July 2018Source: SteroidsAuthor(s): Nguyen Hoai Nam, Ninh Thi Ngoc, Tran Thi Hong Hanh, Nguyen Xuan Cuong, Nguyen Van Thanh, Do Thi Thao, Do Cong Thung, Phan Van Kiem, Chau Van MinhAbstractUsing various chromatographic separations, seventeen steroids including seven new compounds, verrucorosteroids A−F (1−6) and verrucorosterone (7), were isolated from the Vietnamese gorgonian Verrucella corona. Their structures were elucidated by spectroscopic analysis, including HR QTOF MS, 1D and 2D NMR. Among isolates, verrucorosterone (7), 5,6α-epoxy-3β-hydroxy-(22E)-ergosta-...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Complete 1H NMR assignment of cholesteryl benzoate
Publication date: Available online 7 July 2018Source: SteroidsAuthor(s): Nury Pérez-Hernández, Elvia Becerra-Martínez, Pedro Joseph-NathanAbstractThe 750 MHz 1H NMR spectrum of cholesteryl benzoate (1b) could be assigned completely, which means all chemical shifts and all coupling constants, including some long-range values, were established. This task was possible by extracting many approximate coupling constant values in the overlapped spectrum region from an HSQC experiment, and using these values in the 1H iterative full spin analysis integrated in the PERCH NMR software. The task was facilitated u...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series
Publication date: Available online 8 July 2018Source: SteroidsAuthor(s): Alexander M. Scherbakov, Igor V. Zavarzin, Svetlana K. Vorontsova, Alakananda Hajra, Olga E. Andreeva, Anton V. Yadykov, Inna S. Levina, Yulia A. Volkova, Valerii Z. ShirinianAbstractNovel benzylidenes (chalcones) of the 16-dehydroprogesterone series were characterized and their antitumor activity against two breast cancer cell lines was evaluated. Benzylidenes exhibit significant antiproliferative effect on cells and inhibit cell growth in hormone-dependent MCF-7 and hormone-independent MDA-MB-231 breast cancer cell lines. Compound 3d exhibits the hi...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

In silico identification of new potentially active brassinosteroid analogues
Publication date: Available online 8 July 2018Source: SteroidsAuthor(s): Elena Moreno-Castillo, Daniel P. Ramírez-Echemendía, Giselle Hernández-Campoalegre, Dayana Mesa-Tejeda, Francisco Coll-Manchado, Yamilet Coll-GarcíaAbstractBrassinosteroids (BRs) are hormones found in a wide range of plant species, they are synthesized at low concentrations and are essential for normal growth and development. These phytohormones are recognized by the Leucine-rich-repeat ectodomain of the receptor-like-kinase BRI1 which leads to subsequent downstream signaling mediating plant growth/development. In spite of ...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

1H NMR determination of adulteration of anabolic steroids in seized drugs
Publication date: Available online 10 July 2018Source: SteroidsAuthor(s): Marcos Vinícius de Moura Ribeiro, Nivaldo Boralle, Lidiane Gaspareto Felippe, Helena Redigolo Pezza, Leonardo PezzaAbstractCounterfeiting and adulteration of pharmaceuticals is a prevalent problem worldwide and represents a major health risk to the population, with anabolic steroids being one of the main classes of drugs consumed and obtained from dubious sources. In this work, we propose the use of the 1H NMR technique to evaluate formulations containing anabolic steroids, with analysis of 40 samples of anabolic drugs that are used in injecta...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Testosterone enhances expression and functional activity of epithelial sodium channel (ENaC), Cystic Fibrosis transmembrane regulator (CFTR) and sodium hydrogen exchanger (NHE) in vas deferens of sex-steroid deficient male rats
Conclusions: Differential expression of ENaC, CFTR and NHE in vas deferens under testosterone influence indicated the important role of these transporters in creating optimal fluid microenvironment that is essential for preserving male fertility. (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Hybrid of dehydroergosterol and nitrogenous alternariol derivative from the fungus Pestalotiopsis uvicola
Publication date: Available online 10 July 2018Source: SteroidsAuthor(s): Guo-Mei Hou, Xiu-Mei Xu, Qian Wang, Dan-Yi Li, Zhan-Lin LiAbstractA new hybrid of dehydroergosterol and nitrogenous alternariol derivative, pestauvicomorpholine A (1), and three alternariol analogues (2−4) including a new aminated one, pestauvicolactone A (2), were isolated from the fermentation product of the fungus Pestalotiopsis uvicola on rice media. Compounds 1 and 2 represent the first example of aza-alternariol and aza-alternariol-steroid derived from transamination followed by intermolecular hetero-Diels-Alder reaction.Graphical abstract (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Synthesis, pharmacological evaluation and docking studies of progesterone and testosterone derivatives as anticancer agents
Publication date: August 2018Source: Steroids, Volume 136Author(s): Muafia Jabeen, Muhammad Iqbal Choudhry, Ghulam Abbas Miana, Khondaker Miraz Rahman, Umer Rashid, Hidayat-ullah Khan, Arshia, Abdul SadiqAbstractSteroidal hormones progesterone and testosterone play a vital role in breast and prostate cancers. In this research, we have synthesized and characterized a total of thirty-one (31) new nitrogenous derivatives of progesterone and testosterone. The synthesized derivatives (1–31) were screened for their anti-cancer potential against MCF-7 and PC-3 cell lines of breast using MTT assay. The compounds 1-31exhibite...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: August 2018Source: Steroids, Volume 136Author(s): (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Microbial biotransformation of bioactive and clinically useful steroids and some salient features of steroids and biotransformation
Publication date: August 2018Source: Steroids, Volume 136Author(s): Nighat SultanaAbstractSteroids are perhaps one of the most widely used group of drugs in present day. Beside the established utilization as immunosuppressive, anti-inflammatory, anti-rheumatic, progestational, diuretic, sedative, anabolic and contraceptive agents, recent applications of steroid compounds include the treatment of some forms of cancer, osteoporosis, HIV infections and treatment of declared AIDS. Steroids isolated are often available in minute amounts. So biotransformation of natural products provides a powerful means in solving supply proble...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Microbial synthesis of mammalian metabolites of spironolactone by thermophilic fungus Thermomyces lanuginosus
Publication date: August 2018Source: Steroids, Volume 136Author(s): Sreelatha B., ShyamPrasad G., Koteshwar Rao V., Girisham S.AbstractMesophilic fungi are well recognized as models of mammalian drug metabolism. Thermophilic fungi remained unexplored despite having a unique mechanism of growing at higher temperatures and performing wide diverse reactions. The present investigation is directed to isolate a promising thermophilic fungal strain capable of biotransformation using spironolactone as a model drug. Two-stage fermentation protocol was followed for the process. The transformation of spironolactone was identified by ...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Estradiol mediates relaxation of porcine lower esophageal sphincter
Publication date: August 2018Source: Steroids, Volume 136Author(s): Ching-Chung Tsai, Shu-Leei Tey, Li-Ching Chang, Yu-Tsun Su, Kai-Jen Lin, Shih-Che HuangAbstractMost pregnant women have symptoms of gastroesophageal reflux disease (GERD) during pregnancy. Postmenopausal hormone replacement therapy is associated with GERD. The effects of estradiol on lower esophageal sphincter (LES) motility and GERD are not clearly known. The purpose of this study is to investigate the effects of estradiol on the motility of the porcine LES. Relaxations of clasp and sling strips of porcine LES caused by estradiol were measured using isome...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Two new cytotoxic steroids from the Chinese soft coral Sinularia sp.
Publication date: August 2018Source: Steroids, Volume 136Author(s): Song-Wei Li, Wen-Ting Chen, Li-Gong Yao, Yue-Wei GuoAbstractTwo new steroids, ximaosteroid E (1) and ximaosteroid F (2), along with two known related compounds (3 and 4), were isolated from the Chinese soft coral Sinularia sp. Notably, 1 possesses an uncommon dihydrofuran group. Their structures were established from extensive spectroscopic analyses and comparisons of their spectral data with those reported in the literature. The absolute configuration of 2 was determined by applying the modified Mosher’s method. In bioassay, compounds 1, 2, and 4 sh...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “Comparison of [17(20)E]-21-Norpregnene oxazolinyl and benzoxazolyl derivatives as inhibitors of CYP17A1 activity and prostate carcinoma cells growth” [Steroids 129 (2018) 24-34]
Publication date: August 2018Source: Steroids, Volume 136Author(s): Vladimir A. Zolottsev, Yaroslav V. Tkachev, Alexandra S. Latysheva, Vladimir A. Kostin, Roman A. Novikov, Vladimir P. Timofeev, Galina E. Morozevich, Alexey V. Kuzikov, Victoria V. Shumyantseva, Alexander Y. Misharin (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Analysis of the impact of corticosteroids adjuvant treatment during experimental invasive meningococcal infection in mice
Publication date: August 2018Source: Steroids, Volume 136Author(s): Michaël Levy, Ala-Eddine Deghmane, Myriam Aouiti-Trabelsi, Stéphane Dauger, Albert Faye, Patricia Mariani-Kurkdjian, Muhamed-Kheir TahaAbstractInvasive meningococcal disease (IMD) is usually associated with intense inflammatory response that is correlated with severe infection. Corticosteroids may regulate this inflammatory response through an early but transient induction of IL-10 that is suggested to improve the outcome of IMD. We explored the mechanism of action of corticosteroids as an adjuvant treatment to antibiotics. Transgenic mice expr...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Eco-friendly microbial production of diosgenin from saponins in Dioscorea zingiberensis tubers in the presence of Aspergillus awamori
Publication date: August 2018Source: Steroids, Volume 136Author(s): Yu Chen, Yi Dong, Yuanlong Chi, Qiang He, Hui Wu, Yao RenAbstractA novel microbial procedure was proposed for diosgenin production from Dioscorea zingiberensis C.H. Wright (DZW) tubers via employing Aspergillus awamori for the first time. The optimal conditions of fermenter cultivation were established as inoculation dosage of 8%, fermentation temperature of 30 °C, cultivation time of 8 days, initial pH of 7.0 and a stirring rate of 180 rpm when the converted diosgenin content reached a peak value of 74.26 ± 3.23 mg/g substrate. The ...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Synthesis, molecular modeling and biological evaluation of potent analogs of 2-methoxyestradiol
Publication date: August 2018Source: Steroids, Volume 136Author(s): Nora al-Kazaale, Phuong T. Tran, Farhad Haidari, Eirik Johansson Solum, Sandra Liekens, Peter Vervaeke, Ingebrigt Sylte, Jing-Jy Cheng, Anders Vik, Trond Vidar HansenAbstractThe 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 a...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Ionotropin is the mammalian digoxin-like material (DLM). It is a phosphocholine ester of a steroid with 23 carbon atoms
We describe a novel steroid, which we have named “Ionotropin”. Its unique features are: [1] it has 23 carbon atoms and [2] it is a phosphocholine ester. There are no other known mammalian steroids with either structural feature. Ionotropin cross reacts with digoxin-specific antibodies and may be the long-sought, endogenous, mammalian digoxin-like material (DLM). Using LC–MS, we identified three other phosphocholine steroids in serum. Two of these steroids also cross-react with digoxin specific antibodies.In adrenal extracts, we found both phosphocholine esters and corresponding phospho-ethanolamine steroi...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

The sulfoconjugation of androstenone and dehydroepiandrosterone by human and porcine sulfotransferase enzymes
Publication date: August 2018Source: Steroids, Volume 136Author(s): Heidi Laderoute, Christine Bone, E. James SquiresAbstractPorcine sulfotransferase 2A1 (pSULT2A1) is a key enzyme involved in the testicular and hepatic sulfoconjugation of steroids such as dehydroepiandrosterone (DHEA) and potentially androstenone. This latter steroid is a major cause of boar taint, which is an unpleasant off-odour and off-flavour in pork from male pigs. Sulfotransferase 2B1 (pSULT2B1) may also be important, although no direct evidence exists for its involvement in sulfoconjugation of steroids. The purpose of this study was to investigate ...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Catalytic cyclometallation in steroid chemistry V: Synthesis of hybrid molecules based on steroid oximes and (5Z,9Z)-tetradeca-5,9-dienedioic acid as potential anticancer agents
Publication date: October 2018Source: Steroids, Volume 138Author(s): Vladimir A. D'yakonov, Regina A. Tuktarova, Lilya U. Dzhemileva, Svetlana R. Ishmukhametova, Milyausha M. Yunusbaeva, Usein M. DzhemilevAbstractSynthetic analogues of natural 5Z,9Z-dienoic acids - hybrid molecules based on the oximes of cholesterol, pregnenolone, and androsterone with 1,14-tetradeca-5Z,9Z-dienedicarboxylic acid - were synthesized for the first time and studied for antitumor activity in vitro. The acid was prepared using catalytic cyclomagnesiation of O-containing 1,2-dienes with Grignard reagent in the presence of Cp2TiCl2 as the key step...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

C11-oxy C19 and C11-oxy C21 steroids in neonates: UPC2-MS/MS quantification of plasma 11β-hydroxyandrostenedione, 11-ketotestosterone and 11-ketoprogesterone
Publication date: October 2018Source: Steroids, Volume 138Author(s): Therina du Toit, Martijn J.J. Finken, Henrike M. Hamer, Annemieke C. Heijboer, Amanda C SwartAbstractThe purpose of this study was to identify the C11-oxy C19 and C11-oxy C21 steroids in male and female neonate plasma. At birth, the most abundant C11-oxy steroids detected in neonatal plasma were 11β-hydroxyandrostenedione, ∼13 nM, and 11-ketoprogesterone, ∼23 nM. C11-oxy C19 steroids were higher than C19 steroids in neonatal plasma, 22.2 nM vs 5.4 nM. The inclusion of C11-oxy C19 and C21 steroid reference ranges in routine steroid ana...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Catalytic cyclometallation in steroid chemistry VI: Targeted synthesis of hybrid molecules based on steroids and tetradeca-5Z,9Z-diene-1,14-dicarboxylic acid and study of their antitumor activity
Publication date: October 2018Source: Steroids, Volume 138Author(s): Vladimir A. D'yakonov, Regina A. Tuktarova, Lilya U. Dzhemileva, Svetlana R. Ishmukhametova, Milyausha M. Yunusbaeva, Usein M. DzhemilevAbstractHybrid molecules based on a number of steroids (cholesterol, pregnenolone, androsterone) and 1,14-tetradeca-5Z,9Z-dienedicarboxylic acid linked via mono- and diethylene glycol spacers were synthesized for the first time and studied for antitumor activity in vitro. The acid was prepared using catalytic cyclomagnesiation of oxygenated 1,2-dienes with Grignard reagent in the presence of Cp2TiCl2 as the key synthetic ...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Penicisteroid C: New polyoxygenated steroid produced by co-culturing of Streptomyces piomogenus with Aspergillus niger
Publication date: October 2018Source: Steroids, Volume 138Author(s): Ahmed S. Abdel-Razek, Abdelaaty Hamed, Marcel Frese, Norbert Sewald, Mohamed ShaabanAbstractPenicisteroid C, a new polyoxygenated steroid was isolated from co-cultivation of Streptomyces piomogenus AS63D and Aspergillus niger using solid-state fermentation on rice medium. Additional diverse eleven known metabolites were identified: Fumigaclavine C, fumiquinazoline C, physcion, methylsulochrin, methyllinoleate, glycerol linoleate, cerebroside A, thymine, adenine, thymidine and adenosine. The structure of penicisteroid C was determined by HRESIMS, 1D and 2D...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Testosterone, androstenedione, cortisol and cortisone levels in human unstimulated, stimulated and parotid saliva
ConclusionThe way saliva is collected should be considered when analysing and interpreting salivary hormone concentrations. We advocate unstimulated saliva collection in simple polypropylene tubes for all steroid measurements. (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

1H NMR determination of adulteration of anabolic steroids in seized drugs
Publication date: Available online 10 July 2018Source: SteroidsAuthor(s): Marcos Vinícius de Moura Ribeiro, Nivaldo Boralle, Lidiane Gaspareto Felippe, Helena Redigolo Pezza, Leonardo PezzaAbstractCounterfeiting and adulteration of pharmaceuticals is a prevalent problem worldwide and represents a major health risk to the population, with anabolic steroids being one of the main classes of drugs consumed and obtained from dubious sources. In this work, we propose the use of the 1H NMR technique to evaluate formulations containing anabolic steroids, with analysis of 40 samples of anabolic drugs that are used in injecta...
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Testosterone enhances expression and functional activity of epithelial sodium channel (ENaC), Cystic Fibrosis transmembrane regulator (CFTR) and sodium hydrogen exchanger (NHE) in vas deferens of sex-steroid deficient male rats
Conclusions: Differential expression of ENaC, CFTR and NHE in vas deferens under testosterone influence indicated the important role of these transporters in creating optimal fluid microenvironment that is essential for preserving male fertility. (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Hybrid of dehydroergosterol and nitrogenous alternariol derivative from the fungus Pestalotiopsis uvicola
Publication date: Available online 10 July 2018Source: SteroidsAuthor(s): Guo-Mei Hou, Xiu-Mei Xu, Qian Wang, Dan-Yi Li, Zhan-Lin LiAbstractA new hybrid of dehydroergosterol and nitrogenous alternariol derivative, pestauvicomorpholine A (1), and three alternariol analogues (2−4) including a new aminated one, pestauvicolactone A (2), were isolated from the fermentation product of the fungus Pestalotiopsis uvicola on rice media. Compounds 1 and 2 represent the first example of aza-alternariol and aza-alternariol-steroid derived from transamination followed by intermolecular hetero-Diels-Alder reaction.Graphical abstract (Source: Steroids)
Source: Steroids - July 10, 2018 Category: Drugs & Pharmacology Source Type: research