Furostanol saponins from Chinese onion induce G2/M cell-cycle arrest and apoptosis through mitochondria-mediate pathway in HepG2 cells
Publication date: Available online 24 April 2019Source: SteroidsAuthor(s): Yihai Wang, Xiaomin Yi, Limin Xiang, Yuying Huang, Zhe Wang, Xiangjiu HeAbstractPhytochemical investigations on the bulbs of Chinese onion led to the isolation of three new furostanol saponins (1, 2, 5) together with seven known furostanol saponins (3, 4, 6-10). Their chemical structures were elucidated on the basis of spectroscopic and chemical methods, including IR, MS, NMR, and GC analyses. The anti-proliferative and anti-inflammatory activities of the isolates were evaluated. Compounds 7–10 showed potential anti-proliferative activities ag...
Source: Steroids - April 24, 2019 Category: Drugs & Pharmacology Source Type: research

Enhancing effect of cystamine in its amides with betulinic acid as antimicrobial and antitumor agent in vitro
Publication date: Available online 22 April 2019Source: SteroidsAuthor(s): Uladzimir Bildziukevich, Lucie Rárová, Lucie Janovská, David Šaman, Zdeněk WimmerAbstractAmides of betulinic acid with cystamine were synthesized to investigate their antimicrobial and antitumor activity, and their influence on the cell cycle and cell apoptosis. The former target amide (6) displayed cytotoxicity in CEM cell line after 72 h of treatment (IC50 = 3.0 ± 0.7 μM; TI = 20), and induced apoptosis by caspase-3/7 activation in CEM cells. The latter target amide (9) displayed antimicrobial activity agains...
Source: Steroids - April 23, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: June 2019Source: Steroids, Volume 146Author(s): (Source: Steroids)
Source: Steroids - April 23, 2019 Category: Drugs & Pharmacology Source Type: research

Seed germination, respiratory processes and phosphatidic acid accumulation in Arabidopsis diacylglycerol kinase knockouts - the effect of brassinosteroid, brassinazole and salinity
This study demonstrates that dgk mutants possess lower germination rates, lower total respiration rates, an alternative respiratory pathway and PA content under optimal and high salinity conditions in response to EBL treatment comparing to WT plants. (Source: Steroids)
Source: Steroids - April 12, 2019 Category: Drugs & Pharmacology Source Type: research

Regio- and stereoselective C–H functionalization of brassinosteroids
Publication date: June 2019Source: Steroids, Volume 146Author(s): Alaksiej L. Hurski, Aliaksandr G. Kukel, Aliaksandra I. Liubina, Aliona G. Baradzenka, Darya Straltsova, Vadim Demidchik, Pavel Drašar, Vladimir N. Zhabinskii, Vladimir A. KhripachAbstractLate stage CH functionalization is a powerful tool for modification of natural compounds. Herein we report that the rhodium-catalyzed reaction of brassinosteroids with aryloxysulfonamides proceeds regio- and stereoselectively at C15 position. The derivative obtained from 24-epibrassinolide was easily transformed to the conjugate with a BODIPY dye bearing unaffected f...
Source: Steroids - April 9, 2019 Category: Drugs & Pharmacology Source Type: research

Synthesis and Evaluation of Novel D-ring Substituted Steroidal Pyrazolines as Potential Anti-inflammatory Agents
Publication date: Available online 2 April 2019Source: SteroidsAuthor(s): Xiaorui Cai, Shulin Zhao, De Cai, Jinhong Zheng, Zhiwei Zhu, Duncan Wei, Zhiwei Zheng, Huide Zhu, Yicun ChenAbstractTo identify new potential anti-inflammatory agents, a number of novel steroidal derivatives with nitrogen heterocyclic side chains 4a-4l were synthesized and evaluated for their anti-inflammatory effects in activated RAW 264.7 macrophage cells. The synthesis scheme involves two steps, Claisen-Schmidt condensation with the corresponding pregnenolone and aromatic aldehydes as the first step followed by nucleophilic addition of thiosemicar...
Source: Steroids - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Clinical Utility of an Ultrasensitive Urinary Free Cortisol Assay by Tandem Mass Spectrometry
ConclusionsThe improved LC-MS/MS method is both sensitive and specific with enhanced analytical performance and clinical diagnostic utility to screen for CS. The clinical diagnostic sensitivity and specificity were superior based on retrospective patient chart review. (Source: Steroids)
Source: Steroids - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Regio- and stereoselective C-H functionalization of brassinosteroids
Publication date: Available online 2 April 2019Source: SteroidsAuthor(s): Alaksiej L. Hurski, Aliaksandr G. Kukel, Aliaksandra I. Liubina, Aliona G. Baradzenka, Darya Straltsova, Vadim Demidchik, Pavel Drašar, Vladimir N. Zhabinskii, Vladimir A. KhripachAbstractLate stage C-H functionalization is a powerful tool for modification of natural compounds. Herein we report that the rhodium-catalyzed reaction of brassinosteroids with aryloxysulfonamides proceeds regio- and stereoselectively at C15 position. The derivative obtained from 24-epibrassinolide was easily transformed to the conjugate with a BODIPY dye bearing una...
Source: Steroids - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Timosaponin AIII, a steroidal saponin, exhibits anti-tumor effect on taxol-resistant cells in vitro and in vivo
In this study, MTT assay showed that TAIII exhibited significant cytotoxicity against A549/Taxol and A2780/Taxol cells in vitro. Annexin V-FITC/PI staining revealed that TAIII induced apoptosis in A549/T and A2780/T cells. Furthermore, Western blot analysis demonstrated that TAIII inhibited the expressions of phosphatidylinositol 3-kinase (PI3K), protein kinase B (AKT), mammalian target of rapamycin (mTOR) as well as Ras, Raf, mitogen-activated protein kinase (MEPK), extracellular regulated protein kinases (ERK) in two taxol-resistant cancer cell lines. Besides, in vivo studies demonstrated that TAIII inhibited tumor growt...
Source: Steroids - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Concise Synthesis of 2-Methoxyestradiol from 17β-Estradiol through the C(sp2)-H Hydroxylation
Publication date: Available online 2 April 2019Source: SteroidsAuthor(s): Meng-Yu Ba, Li-Wen Xia, Hong-Liang Li, Ying-Ge Wang, Ya-Nan Chu, Qing Zhao, Chao-Ping Hu, Xiao-Tong He, Tian-Xiao Li, Kai-Yue Liang, Ya-Han Zhang, Liu Yang, Wen-Hao Xie, Hua Yang, Mo-Ran SunAbstractA four-step route for the synthesis of 2-methoxyestradiol (5) starting from 17β-estradiol (1) has been achieved with a 51% overall yield. The key step was the ruthenium-catalyzed ortho-C(sp2)-H bond hydroxylation of aryl carbamates. Using dimethyl carbamate as the directing group, [RuCl2(p-cymene)]2 as the catalyst, PhI(OAc)2 as the oxidant and triflu...
Source: Steroids - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Elucidation of the Biosynthetic Pathways of Boldenone in the Equine Testis
In conclusion, boldenone and boldienone are naturally present in the equine testis, with the biosynthesis of these steroids arising from the conversion of testosterone and androstenedione. However, additional work employing larger numbers of animals, further enzyme kinetic experiments and pure reference standards for 2-OH androstenedione isomers would be required to better characterize the pathways involved in these transformations. (Source: Steroids)
Source: Steroids - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Acute estradiol treatment reduces skeletal muscle protein breakdown markers in early- but not late-postmenopausal women
Publication date: Available online 27 March 2019Source: SteroidsAuthor(s): Young-Min Park, Amy C. Keller, Shauna S. Runchey, Benjamin F. Miller, Wendy M. Kohrt, Rachael E. Van Pelt, Chounghun Kang, Catherine M. Jankowski, Kerrie L. MoreauAbstractObjectivesMenopause and decline in estradiol (E2) may contribute to sarcopenia (i.e., age-related decline in muscle mass and strength) in women. E2 may directly impact skeletal muscle protein breakdown via estrogen receptor (ER) signaling, primarily ERα. It is not yet known whether: 1) E2 regulates pathways of skeletal muscle protein breakdown; 2) E2-mediated changes in prote...
Source: Steroids - March 28, 2019 Category: Drugs & Pharmacology Source Type: research

The Synthesis of 16-androstene Sulfoconjugates from Primary Porcine Leydig Cell Culture
Publication date: Available online 20 March 2019Source: SteroidsAuthor(s): Heidi Laderoute, Christine Bone, Dyanne Brewer, E. James SquiresAbstractIncreased public interest in the welfare of pigs reared for pork production has led to an enhanced effort in finding alternatives to castration for controlling the unpleasant odour and flavour from heated pork products known as boar taint. The purpose of this study was to investigate the testicular metabolism of androstenone, one of the major components of boar taint. Leydig cells were isolated from mature boars and incubated with radiolabeled androstenone for 10 min, 1h, 4h, 8h...
Source: Steroids - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “Membrane-initiated nuclear trafficking of the glucocorticoid receptor in hypothalamic neurons” [Steroids 142 (2019) 55–64]
Publication date: Available online 20 March 2019Source: SteroidsAuthor(s): Jennifer R. Rainville, Grant L. Weiss, Nathan Evanson, James P. Herman, Nandini Vasudevan, Jeffrey G. Tasker (Source: Steroids)
Source: Steroids - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

BPA disrupts the cardioprotection by 17β-oestradiol against ischemia/reperfusion injury in isolated guinea pig hearts
Publication date: Available online 20 March 2019Source: SteroidsAuthor(s): Nan Mao, Qinghua Gao, Tong zhu, Liying HaoAbstractBisphenol A (BPA) is an environmental oestrogen or xenoestrogen (XEs). XEs represent a health risk due to their potential for endocrine disruption and ability to mimic estrogenic activity. The effects of BPA on isolated hearts under normal and ischemia/reperfusion (I/R) conditions were investigated for the first time, with a focus on the effects of BPA and 17β-oestradiol (E2) co-administration on I/R injury. Our results indicated that BPA at 10-7 M and 10-5 M did not significantly affect Heart r...
Source: Steroids - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Metabolism of formestane in humans: identification of urinary biomarkers for antidoping analysis
Publication date: Available online 20 March 2019Source: SteroidsAuthor(s): X. de la Torre, D. Martinez Brito, C. Colamonici, M.K. Parr, F. BotrèAbstractFormestane (4-hydroxyandrost-4-ene-3,17-dione, 4OH-AED) is an aromatase inhibitor prohibited in sports. In recent years, it has been demonstrated that it can also originate endogenously by the hydroxylation in C4 position of androstenedione. Thus, the use of isotope ratio mass spectrometry (IRMS) is mandatory according to the World Antidoping Agency (WADA) to discriminate endogenous from synthetic origin.In a previous work and after oral administrations of formestane...
Source: Steroids - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Design and synthesis of novel steroidal imidazoles as dual inhibitors of AR/CYP17 for the treatment of prostate cancer
Publication date: Available online 15 March 2019Source: SteroidsAuthor(s): Qiangqiang Hou, Conghui He, Kejing Lao, Guoshun Luo, Qidong You, Hua XiangAbstractBoth AR and CYP17 are important targets for blocking androgen signaling, and it has been accepted that multifunctional drugs have a low risk of drug resistance in the treatment of cancer. Thus, herein a series of steroidal imidazoles were designed, synthesized and evaluated as dual AR/CYP17 ligands. Several compounds displayed good biological profiles in both enzymatic and cellular assays. SAR studies showed that introducing oximino at the C-3 position of steriodal sca...
Source: Steroids - March 17, 2019 Category: Drugs & Pharmacology Source Type: research

Expression of estrogen receptor alpha in developing brain, ovary and shell gland of Gallus gallus domesticus: Impact of stress and estrogen
Publication date: Available online 15 March 2019Source: SteroidsAuthor(s): Mukesh Kumar Niranjan, Rashmi SrivastavaAbstractEstrogen plays a central role in the control of reproductive behaviour and in the regulation of neuroendocrine system. To elucidate the mechanism by which it controls the stress-modulated functions, it is important to understand how estrogenic effects are mediated. The distribution of estrogen receptor alpha (ERα) protein in brain, ovary and shell gland of chickens has been investigated. Immature chickens were taken and randomly divided into four groups. First group served as control (C), second ...
Source: Steroids - March 17, 2019 Category: Drugs & Pharmacology Source Type: research

Synthesis, characterization and antiproliferative activity of seco analogues of brassinosteroids
Publication date: Available online 16 March 2019Source: SteroidsAuthor(s): Miroslav Kvasnica, Katerina Buchtova, Milos Budesinsky, Tibor Beres, Lucie Rarova, Miroslav StrnadAbstractSynthesis and structure-activity relationship analysis of a two groups of 2,3-seco analogues of brassinosteroids (BRs) were performed to examine their antiproliferative activities. Two steroid skeletons were chosen for the preparation of seco analogues – cholestane and stigmastane. The synthetic strategy consists of multistep reactions and detailed analysis of compounds prepared. We have discovered unpublished behaviour of 2,3-seco-2,3-dih...
Source: Steroids - March 17, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: May 2019Source: Steroids, Volume 145Author(s): (Source: Steroids)
Source: Steroids - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

Design and Synthesis of Fluorescently Labeled Steroidal Antiestrogens
Publication date: Available online 21 February 2019Source: SteroidsAuthor(s): Robert N. Hanson, Nisal GajadeeraAbstractA set of derivatives of 11β-(4-oxyphenyl)estradiol were prepared as potential fluorescent imaging agents for the evaluation of the estrogen receptor. The compounds were designed based on the established affinity and selectivity of 11β-[4-(dimethylethoxy)phenyl]estradiol (RU39411) as an estrogen receptor (ER) antagonist. The 5-(dimethylamino) naphathalene-1-sulfonyl (dansyl) and 7-nitrobenzo[c][1,2,5] oxadiaol-4-yl (NBD) moieties were selected based on their fluorescent and physicochemical propert...
Source: Steroids - February 23, 2019 Category: Drugs & Pharmacology Source Type: research

Upregulated Cyclin B1/CDK1 Mediates Apoptosis Following 2-Methoxyestradiol-Induced Mitotic Catastrophe: Role of Bcl-XL Phosphorylation
Publication date: Available online 22 February 2019Source: SteroidsAuthor(s): Hye Joung Choi, Bao Ting ZhuAbstract2-Methoxyestradiol is an endogenous nonpolar metabolite of 17β-estradiol with a strong antitubulin activity. Earlier we showed that 2-methoxyestradiol increases the level and activity of cyclin B1/CDK1, which subsequently induces mitotic prometaphase arrest. In the present study, we demonstrate that upregulation of cyclin B1/CDK1 is responsible for the increased phosphorylation of the anti-apoptotic proteins Bcl-2 and Bcl-XL in 2-methoxyestradiol-induced, mitotically-arrested cancer cells. Additional analy...
Source: Steroids - February 23, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: April 2019Source: Steroids, Volume 144Author(s): (Source: Steroids)
Source: Steroids - February 23, 2019 Category: Drugs & Pharmacology Source Type: research

Novel antimicrobial agents’ discovery among the steroid derivatives
Publication date: Available online 15 February 2019Source: SteroidsAuthor(s): Nanuli Sh. Nadaraia, Lela Sh. Amiranashvili, Maia Merlani, Meri L. Kakhabrishvili, Nana N. Barbakadze, Athina Geronikaki, Anthi Petrou, Vladimir Poroikov, Ana Ciric, Jarmila Glamoclija, Marina SokovicAbstractFourteen steroid compounds were in silico evaluated using computer program PASS as antimicrobial agents. The experimental studies evaluation revealed that all compounds have good antibacterial activity with MIC at range of 0.003-0.96 mg/mL and MBC 0.06-1.92 mg/mL. Almost all compounds except of compound 4 (3β-acetoxy-1/-p-chlorophenyl-3/...
Source: Steroids - February 16, 2019 Category: Drugs & Pharmacology Source Type: research

Trace Analysis of Estrogens in Milk Samples by Molecularly Imprinted Solid Phase Extraction with Genistein as a Dummy Template Molecule and High-performance Liquid Chromatography–tandem Mass Spectrometry
Publication date: Available online 15 February 2019Source: SteroidsAuthor(s): Jiwang Tang, Jianxiu Wang, Liejiang Yuan, Yong Xiao, Xiu wang, Zong yangAbstractDummy molecularly imprinted polymer microspheres (DMIPMS) towards estrogens were synthesized by Pickering emulsion polymerization employing genistein (GEN) as a dummy template molecule. The FTIR analysis indicated the successful preparation of the imprinted polymers, and the characterization results of scanning electron microscopy and nitrogen adsorption desorption measurement indicated that the obtained DMIPMS are in possess of regular spherical shapes, porous struct...
Source: Steroids - February 16, 2019 Category: Drugs & Pharmacology Source Type: research

Effect of testosterone cypionate and stanozolol on the heart of young trained mice: a morphometric study
In conclusion, the use of AAS in supraphysiological doses can change the heart morphology and can lead to serious health consequences.Graphical abstract (Source: Steroids)
Source: Steroids - February 15, 2019 Category: Drugs & Pharmacology Source Type: research

Review of fluorescent steroidal ligands for the estrogen receptor 1995–2018
Publication date: April 2019Source: Steroids, Volume 144Author(s): Nisal Gajadeera, Robert N. HansonAbstractThe development of fluorescent ligands for the estrogen receptor (ER) continues to be of interest. Over the past 20 years, most efforts have focused on appending an expanding variety of fluorophores to the B-, C- and D-rings of the steroidal scaffold. This review highlights the synthesis and evaluation of derivatives substituted primarily at the 6-, 7α- and 17α-positions, culminating with our recent work on 11β-substituted estradiols, and proposes an approach to new fluorescent imaging agents that ...
Source: Steroids - February 15, 2019 Category: Drugs & Pharmacology Source Type: research

Biotransformation into 11α-hydroxyprogesterone glucosides by glucosyltransferase
Publication date: Available online 10 February 2019Source: SteroidsAuthor(s): Tokutaro Yamaguchi, Joo-Ho Lee, A-Rang Lim, Eun-Ji Yu, Tae-Jin OhAbstractRecently, studies on the steroidal hormone activity in the brain have attracted attention, and the influences of the varied glucosides and their artificial derivatives have been discussed; additionally, it has been suggested that glucosides are the synthetic precursors of glucuronide as a label molecule. However, glucosides are formed with 11α-hydroxyprogesterone (1), which is important as a blood pressure regulator, but anti-androgen activity remains unknown. Using UD...
Source: Steroids - February 12, 2019 Category: Drugs & Pharmacology Source Type: research

Immunomodulatory effects of progesterone and selective ligands of membrane progesterone receptors
The objective of this study was to examine the effects of P4 and new selective mPRs ligands on the expression of pro- and anti-inflammatory cytokines in activated human peripheral blood mononuclear cells (PBMCs), THP-1 monocyte cells, and Jurkat T cells. It was demonstrated that the action of P4 and selective ligands was unidirectional, but in different types of the immune cells, their effects were different, and sometimes even opposite. In PBMCs, exposure to these steroids resulted in the increase of mRNA and secreted protein levels of IL-1β, TNFα, and IL-6 cytokines, as well as in the increase of INFγ mR...
Source: Steroids - February 12, 2019 Category: Drugs & Pharmacology Source Type: research

Severe forms of complete androgen insensitivity syndrome caused by a p.Q65X novel mutation in androgen receptor: clinical manifestations, imaging findings and molecular genetics
This study indicates that US and MRI are two useful and noninvasive imaging methods for the diagnosis and evaluation of CAIS, and identification of this novel mutation expands the database of AR gene mutations. Furthermore, with the availability of the identification technology for this mutation, prenatal diagnosis could be offered for future pregnancies. (Source: Steroids)
Source: Steroids - February 9, 2019 Category: Drugs & Pharmacology Source Type: research

Synthesis of steroidal 1,2- and 1,3-diamines as ligands for transition metal ion complexation
Publication date: Available online 6 February 2019Source: SteroidsAuthor(s): Barbara Seroka, Zenon Łotowski, Agnieszka Wojtkielewicz, Przemysław Bazydło, Ewelina Dudź, Agnieszka Hryniewicka, Jacek W. MorzyckiAbstractTwo series of cholestane-based diamines (1,2 and 1,3) were synthesized using simple and efficient procedures. The convenient substrates for these syntheses were cholesteryl mesylate and tosylate, which were converted to appropriate amines via easily obtained azides. The final diamines were prepared using a substitution reaction with bromoacetonitrile (in the case of 1,2-diamines) or condensation with acrylo...
Source: Steroids - February 7, 2019 Category: Drugs & Pharmacology Source Type: research

Induced Production of Steroids by Co-Cultivation of Two Endophytes from Mahonia fortunei
Publication date: Available online 6 February 2019Source: SteroidsAuthor(s): Zi-Ru Wang, Gang Li, Li-Xia Ji, Hang-Hang Wang, Han Gao, Xiao-Ping Peng, Hong-Xiang LouAbstractA new ergosterol derivative, 23R-hydroxy-(20Z,24R)-ergosta-4,6,8(14),20(22)-tetraen-3-one (1), and a biosynthetically related known compound, (22E,24R)-ergosta-4,6,8(14),22-tetraen-3-one (2), were isolated from the co-culture between endophytic fungus Pleosporales sp. F46 and endophytic bacterium Bacillus wiedmannii Com1 both inhibiting in the medicinal plant Mahonia fortunei. The structure of the new compound 1 was determined by extensive spectroscopic ...
Source: Steroids - February 7, 2019 Category: Drugs & Pharmacology Source Type: research

Synthesis of Benzoylbenzamide Derivatives of 17α-E-Vinyl Estradiol and Evaluation as Ligands for the Estrogen Receptor-α Ligand Binding Domain
Publication date: Available online 6 February 2019Source: SteroidsAuthor(s): Robert N. Hanson, Emmett McCaskill, Edward Hua, Pakamas Tongcharoensirikul, Robert Dilis, Jessa L. Silver, Timothy A. Coulther, Mary Jo Ondrechen, David Labaree, Richard B. HochbergAbstractA series consisting of substituted benzoylbenzamide derivatives of 17α-E-vinyl estradiol 6a-i and 7a-d was prepared in good overall yields from the corresponding novel iodinated benzoylbenzamide precursors using Pd(0)-catalyzed Stille coupling. Biological evaluation using competitive binding assays indicated that all compounds were effective ligands for th...
Source: Steroids - February 7, 2019 Category: Drugs & Pharmacology Source Type: research

Sex differences in glucocorticoids-induced anabolic effects on energy balance
The objective of the current study was to evaluate the effects of prolonged (28 days) treatment with dexamethasone or corticosterone in intact rats, both male and female, on food intake, body weight gain, Lee index, weights and area of adipocytes of retroperitoneal and perigonadal+perirenal adipose tissues, glucose tolerance test (GTT) and plasma concentrations of free fatty acids, cholesterol and triglycerides. Treatment with dexamethasone was able to increase body weight gain, food intake, area of adipocytes and weight of retroperitoneal adipose tissue in males. Prolonged treatment with corticosterone also stimulated bod...
Source: Steroids - February 7, 2019 Category: Drugs & Pharmacology Source Type: research

Review of Fluorescent Steroidal Ligands for the Estrogen Receptor 1995-2018
Publication date: Available online 6 February 2019Source: SteroidsAuthor(s): Nisal Gajadeera, Robert N. HansonAbstractThe development of fluorescent ligands for the estrogen receptor (ER) continues to be of interest. Over the past 20 years, most efforts have focused on appending an expanding variety of fluorophores to the B-, C- and D-rings of the steroidal scaffold. This review highlights the synthesis and evaluation of derivatives substituted primarily at the 6-, 7α- and 17α-positions, culminating with our recent work on 11β-substituted estradiols, and proposes an approach to new fluorescent imaging agen...
Source: Steroids - February 6, 2019 Category: Drugs & Pharmacology Source Type: research

Molecular modelling predicts that 2-methoxyestradiol disrupts HIF function by binding to the PAS-B domain
Publication date: Available online 6 February 2019Source: SteroidsAuthor(s): Andrea Poch, Felipe Villanelo, Soledad Henriquez, Paulina Kohen, Alex Muñoz, Jerome F. Strauss, Luigi DevotoAbstractAn estradiol metabolite, 2-methoxyestradiol (2ME), has emerged as an important regulator of ovarian physiology. 2ME is recognized as a potent anti-angiogenic agent in clinical trials and laboratory studies. However, little is known about its molecular actions and its endogenous targets. 2ME is produced by human ovarian cells during the normal menstrual cycle, being higher during regression of the corpus luteum, and is postulat...
Source: Steroids - February 6, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: March 2019Source: Steroids, Volume 143Author(s): (Source: Steroids)
Source: Steroids - February 6, 2019 Category: Drugs & Pharmacology Source Type: research

Alpha lipoic acid protects against dexamethasone-induced metabolic abnormalities via APPL1 and PGC-1 α up regulation
Conclusion: ALA can prevent metabolic abnormalities induced by dexamethasone via PGC1α and APPL1 upregulation. (Source: Steroids)
Source: Steroids - February 1, 2019 Category: Drugs & Pharmacology Source Type: research

Membrane androgen receptors (OXER1, GPRC6A AND ZIP9) in prostate and breast cancer: A comparative study of their expression
Publication date: Available online 29 January 2019Source: SteroidsAuthor(s): Konstantina Kalyvianaki, Athanasios A. Panagiotopoulos, Panagiotis Malamos, Eleni Moustou, Maria Tzardi, Efstathios N. Stathopoulos, Georgios S. Ioannidis, Kostas Marias, George Notas, Panayiotis A. Theodoropoulos, Elias Castanas, Marilena KampaAbstractAccumulating evidence during the last decades revealed that androgens exert membrane-initiated actions leading to the modulation of significant cellular processes, important for cancer cell growth and metastasis (including prostate and breast), that involve signaling via specific kinases. Collective...
Source: Steroids - January 30, 2019 Category: Drugs & Pharmacology Source Type: research

Estrogen Metabolism Pathways in Preeclampsia and Normal Pregnancy
Conclusion(s)Our findings show that estradiol concentrations were elevated in preeclampsia versus controls in early pregnancy. In mid-pregnancy, all three estrogen metabolism (2-, 4-, and 16-) pathways showed some reduction in preeclampsia that appeared to continue for the 2- and 4-pathways in late pregnancy. We hypothesize that this may indicate that there is a generalized reduction in estrogen metabolism in preeclampsia rather than a deficit of specific enzymes, such as those involved in the 2-hydroxylation pathway. (Source: Steroids)
Source: Steroids - January 25, 2019 Category: Drugs & Pharmacology Source Type: research

Alpha lipoic acid protects against dexamethasone- induced metabolic abnormalities via APPL1 and PGC-1 α up regulation
Conclusion: ALA can prevent metabolic abnormalities induced by dexamethasone via PGC1α and APPL1 upregulation. (Source: Steroids)
Source: Steroids - January 24, 2019 Category: Drugs & Pharmacology Source Type: research

Expression of Aromatase and Synthesis of Sex Steroid Hormones in Skeletal Muscle Following Exercise Training in Ovariectomized Rats
Publication date: Available online 18 January 2019Source: SteroidsAuthor(s): Rengfei Shi, Xiangyang Tian, Yu Feng, Zepeng Cheng, Jianqiang Lu, Darrell W. Brann, Quanguang ZhangAbstractAge-related muscle wasting (sarcopenia) is accompanied by a decrease in estrogen levels which can compromise the health of aging women. Recent studies have shown that the key enzyme of estrogen synthesis (aromatase) is detected in the skeletal muscle. The purpose of this study was to investigate the effects of exercise on the expression of aromatase and the synthesis of sex steroid hormones in skeletal muscle following exercise training. Ovar...
Source: Steroids - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Characterization of a highly specific monoclonal antibody against human aldo-keto reductase AKR1C3
In this report, a highly specific monoclonal antibody for AKR1C3, 10B10, was developed and characterized. Compared to other AKR1C3 antibodies, 10B10 is highly specific and sensitive to AKR1C3 in multiple assay formats. Thus, 10B10 will be a valuable tool for the clinical development of AKR1C3 targeting therapeutics and the study of AKR1C3 biology. (Source: Steroids)
Source: Steroids - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Ile351, Leu355 and Ile461 residues are essential for catalytic activity of bovine cytochrome P450scc (CYP11A1)
This study was aimed to find out the amino acid residues substitution of which could modify the conformation of the active site providing possible higher enzyme activity towards β-sitosterol. After structural and bioinformatics analysis three amino acid residues I351, L355, I461 were chosen. Molecular dynamics simulations of P450scc evidenced the stability of the wild type, double (I351A/L355A) and triple (I351A/L355A/I461A) mutants. Mutant variants of cDNA encoding P450scc with the single, double and triple mutations were obtained by site-directed mutagenesis. However, the experimental data indicate that the introduc...
Source: Steroids - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Establishment of reference intervals for serum concentrations of androstanediol glucuronide by a newly developed LC-MS/MS method
ConclusionAn easy, fast and straightforward LC-MS/MS method for the determination of androstanediol glucuronide has been developed and fully validated. Besides, reference interval for normal European populations, including prepubertal and pubertal children has been established for the first time. (Source: Steroids)
Source: Steroids - January 7, 2019 Category: Drugs & Pharmacology Source Type: research

Biotransformation of progestonic hormone dydrogesterone with Macrophomina phaseolina, and study of the effect of biotransformed products on phagocytes oxidative burst
Publication date: Available online 6 January 2019Source: SteroidsAuthor(s): Abdul Wajid, Malik Shoaib Ahmad, Sammer Yousuf, Atia-tul-Wahab, Almas Jabeen, Atta-ur-Rahman, M. Iqbal ChoudharyAbstractBiotransformation of a synthetic progestonic hormone dydrogesterone (1), C21H28O2, with a plant pathogenic fungus Macrophomina phaseolina yielded two new 2 and 3, and a known 4 metabolites. These analogues were identified as, 3β,11α-dihydroxy-5β,9β,10α-pregna-7-ene-6,20-dione (2), 15β-hydroxy-9β,10α-pregna-4,6-diene-3,20-dione (3), and 8α-hydroxy-9β,10α-pregna-4,6-diene-3...
Source: Steroids - January 6, 2019 Category: Drugs & Pharmacology Source Type: research

Research on isoprenoids is of great relevance to human life
Publication date: Available online 4 January 2019Source: SteroidsAuthor(s): Jerzy Wicha, Pavel Drašar, Jacek W. Morzycki (Source: Steroids)
Source: Steroids - January 4, 2019 Category: Drugs & Pharmacology Source Type: research

Design, Synthesis and Antitumor Activity of Steroidal Pyridine Derivatives Based on Molecular Docking
Publication date: Available online 25 December 2018Source: SteroidsAuthor(s): Ya-Ling Song, Cheng-Piao Tian, Wu Yan, Li-he Jiang, Li-Qun ShenAbstractWith steroid as a carrier nucleus and introducing a pyridine heterocycle as a pharmacophore on the D ring, a series of steroidal pyridine derivatives were designed and studied for their antitumor activity by molecular docking software. The compounds were synthesized as small molecule inhibitors and studied as anticancer agents. The synthesis of the analogs was performed in a one-pot multi-component reaction and the corresponding compounds were screened in vitro for their antit...
Source: Steroids - December 25, 2018 Category: Drugs & Pharmacology Source Type: research

Structural analysis of 25-hydroxycholesterol stereoisomers differing in configuration in position 17 and 20, by three-dimensional NMR spectra
Publication date: Available online 22 December 2018Source: SteroidsAuthor(s): Maria Misiak, Wiktor Koźmiński, Jacek Wójcik, Rafał R. Siciński, Jerzy WichaAbstractThe application of 3D NMR experiments and DFT calculations enabled the structure investigation of C-17 epimer of 3-(25-hydroxycholest-5-enyl) acetate is presented. The H-17 and H-20 protons features the same values of 1H chemical shift, what causes that the structure elucidation require additional resolution enabled by 3D NMR experiments. The NMR experiments and theoretical calculations allowed for: the resonance assignment (3D COSY-HMBC and 3D TOCSY-HS...
Source: Steroids - December 22, 2018 Category: Drugs & Pharmacology Source Type: research

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Publication date: January 2019Source: Steroids, Volume 141Author(s): (Source: Steroids)
Source: Steroids - December 22, 2018 Category: Drugs & Pharmacology Source Type: research