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Caroline Ceailles Flarakos, Andrew Weiskopf, Matthew Robinson, Guoshun Wang, Paul Vouros, Gino J Sasso, Milan R Uskokovic, G Satyanarayana Reddy
Analogs of 1α,25-dihydroxyvitamin D3 (S1) with 20-epi modification (20-epi analogs) possess unique biological properties. We previously reported that 1α,25-dihydroxy-20-epi-vitamin D3 (S2), the basic 20-epi analog is metabolized into less polar metabolites (LPMs) in rat osteosarcoma cells (UMR-106) but not in a perfused rat kidney. Furthermore, we also noted that only selective 20-epi analogs are metabolized into LPMs. For example, 1α,25-dihydroxy-16-ene-20-epi-vitamin D3 (S4), but not 1α,25-dihydroxy-16-ene-23-yne-20-epi-vitamin D3 (S5) is metabolized into LPMs...
January 12, 2017: Steroids
Janae Strickland, Stephen McIlmoil, Brice J Williams, Dennis C Seager, James P Porter, Allan M Judd
Mechanisms of interleukin-6 (IL-6)-induced cortisol release (CR) were investigated by exposing H295R cells to IL-6 and determining mRNA/protein expression (PCR/western blots) for steroidogenic enzymes (SE), steroidogenic acute regulatory protein (StAR), steroidogenic factor-1 (SF-1)(enhances SE/StAR expression), activator protein 1 (AP-1)(regulates SE/StAR expression) and adrenal hypoplasia congenita-like protein (DAX-1)(inhibits SE/StAR expression). Promoter activity of StAR (SPA) was measured by a luciferase-coupled promoter...
January 4, 2017: Steroids
Marek Kłobucki, Aleksandra Grudniewska, Damian A Smuga, Małgorzata Smuga, Joanna Jarosz, Joanna Wietrzyk, Gabriela Maciejewska, Czesław Wawrzeńczyk
Dehydroepiandrosterone (DHEA) is a natural hormone with many beneficial properties including an anticancer activity. Unfortunately, DHEA is unstable in the body and exhibits cytotoxicity against healthy cells. In this study, a series of new phosphocholines containing DHEA at sn-1 and/or sn-2 positions were prepared. Succinic acid was used as a linker between the active drug and sn-glycero-3-phosphocholine. All the compounds were evaluated in vitro for their antiproliferative activities against four cell lines: Balb/3T3, HL-60, B16, and LNCaP...
January 4, 2017: Steroids
Fayaz Ali Larik, Aamer Saeed, Danish Shahzad, Muhammad Faisal, Hesham El-Seedi, Haroon Mehfooz, Pervaiz Ali Channar
Spironolactone is a well-known multi-target drug and is specifically used for the treatment of high blood pressure and heart failure. It is also used for the treatment of edema, cirrhosis of the liver, malignant, pediatric, nephrosis and primary hyperaldosteronism. Spironolactone in association with thiazide diuretics treats hypertension and in association with furosemide treats bronchopulmonary dyspepsia. The therapeutic mechanism of action of spironolactone involves binding to intracellular mineralocorticoids receptors (MRs) in kidney epithelial cells, thereby inhibiting the binding of aldosterone...
December 29, 2016: Steroids
Rayala Naveen Kumar, Seongmin Lee
An efficient synthesis of the 23-deoxy-25-epi north unit of cephalostatin 1 has been achieved in 17 steps via reductive and oxidative functionalizations of hecogenin acetate with an overall yield of 3.8%. This synthesis features transetherification-mediated E-ring opening, D-ring oxidation, hemiketalization-mediated E-ring closure, and stereoselective 5/5-spiroketalization.
December 29, 2016: Steroids
Elvar Örn Viktorsson, Mari Gabrielsen, Nugalya Kumarachandran, Ingebrigt Sylte, Pål Rongved, Ove Alexander Høgmoen Åstrand, Eili Tranheim Kase
The endogenous oxysterol 22(R)-hydroxycholesterol (22RHC, 1) is an LXR agonist which upregulates genes of critical involvement in human cholesterol- and lipid metabolism. In contrast, its synthetic epimer 22(S)-hydroxycholesterol (22SHC, 8) has shown specific antagonistic effects in recent studies, avoiding unwanted side effects provided by potent LXR agonists. In terms of LXR modulation, the aim of this study was to compare 22SHC (8), 22RHC (1) and synthesized ligands with keto- and amide functionality in the 22nd position of the cholesterol scaffold...
December 21, 2016: Steroids
Izabella Jastrzebska, Katarzyna Niemirowicz, Wioleta I Brzozowska, Robert Bucki
An efficient procedure for the synthesis of (20S)-3β-acetoxy-5α-pregnane-20,16β-carbolactone is described. Bactericidal and fungicidal activity of the lactone against different bacteria such as MSSA, MRSA, E. coli ESBL, P. aeruginosa and clinical isolates of Candida spp., in planktonic and biofilm growth stage were assessed. Additionally, the affinity of this new compound to microbial plasma membrane and hemoglobin release from human red blood cells were determined using fluorometric and colorimetric assay, respectively...
December 18, 2016: Steroids
Quan Zhang, Zheng Chen, Shenghuo Chen, Youyun Xu, Huihua Deng
BACKGROUND: Cortisol, cortisone and the ratio of cortisol to cortisone in saliva, urine and hair are acute, short-term and long-term biomarkers to reliably assess the activity of hypothalamic-pituitary-adrenal (HPA) axis and 11β-hydroxysteroid dehydrogenase (11β-HSD). One key issue is whether these biomarkers have intraindividual relative stability. Salivary, urinary and hair cortisol was proven to show considerable long-term intraindividual relative stability. However, currently unknown is whether cortisone and the ratio in saliva, urine and hair show intraindividual relative stability...
December 18, 2016: Steroids
Marina V Efimova, Radomira Vankova, Victor V Kusnetsov, Raisa P Litvinovskaya, Ilya E Zlobin, Petre Dobrev, Nina P Vedenicheva, Alina L Savchuk, Raisa A Karnachuk, Natalia V Kudryakova, Vladimir V Kuznetsov
In order to evaluate whether brassinosteroids (BS) and green light regulate the transcription of plastid genes in a cross-talk with cytokinins (CKs), transcription rates of 12 plastid genes (ndhF, rrn23, rpoB, psaA, psaB, rrn16, psbA, psbD, psbK, rbcL, atpB, and trnE/trnY) as well as the accumulation of transcripts of some photoreceptors (PHYA, CRY2, CRY1A, and CRY1B) and signaling (SERK and CAS) genes were followed in detached etiolated barley leaves exposed to darkness, green or white light ±1μm 24-epibrassinolide (EBL)...
December 18, 2016: Steroids
Wentao Li, Xiaona Lin, Rui Wang, Feng Wang, Shaohua Xie, Lap Ah Tse
The mortality of lung cancer presents a significant difference between the sexes. A role of hormone therapy (HT) in lung cancer mortality has been suggested, but the evidence is inconclusive. We sought to elucidate this issue with a meta-analysis. We conducted a systematic literature search in both Pubmed and Embase. Studies that reported the association of HT and mortality of lung cancer cases were included. Pooled hazard ratio (HR) was computed as the effect size to reflect the association between HT and lung cancer mortality...
December 11, 2016: Steroids
Yun Sik Kim, Won Se Suh, Kyoung Jin Park, Sang Un Choi, Kang Ro Lee
A new pregnane-type steroidal glycoside (1), two new spirostane-type steroidal glycosides (2, 3), and two new furostane-type steroidal glycosides (4, 5), named allimacrosides A-E, together with four known compounds (6-9) were isolated from a 80% MeOH extract of Allium macrostemon Bunge. The identification and structural elucidation of these compounds were based on their 1D- and 2D-NMR spectra, and HR-FAB-MS data analysis. The isolated compounds were tested for cytotoxicity against four human tumor cell lines in vitro using the sulforhodamine B bioassay...
December 11, 2016: Steroids
Yuyong Ke, Renaud Gonthier, Fernand Labrie
The concentrations of allopregnanolone (Allopreg), pregnenolone (Preg) and androsterone (ADT) are very low in the circulation, especially in postmenopausal women, resulting in a considerable challenge for their accurate measurements in serum or plasma. In this report, a sensitive and reliable LC-MS/MS assay method has been developed using a simple sample preparation and the 1-Amino-4-methylpiperazine (AMP) derivatization procedure. A 5pg/ml (0.1pg on column) of low limit of quantitation has been achieved for Allopreg, Preg and ADT, with a sensitivity comparable to data obtained with the commercial reagent...
November 29, 2016: Steroids
Abdulrhman Alsayari, Lucas Kopel, Mahmoud Salama Ahmed, Adam Pay, Taylor Carlson, Fathi T Halaweish
Series of estrone based analogs were synthetically investigated at positions C-9, C-11, C-16, and C-17 positions, to be biologically evaluated via assessment of cell proliferation, cytotoxicity, and estrogenic/anti-estrogenic activity. LA-7 and LA-10 revealed their potential to exhibit inhibitory estrogenic profile. This was further validated by Estrogen Receptor-α (ER-α) and Estrogen Receptor-β (ER-β) competitive binding assays to reveal the high selective affinity of LA-7 towards ER-α at 5.49μM, while LA-10 did not show any binding affinity towards neither ER-α nor ER-β; suggesting another mechanism for inhibition...
November 20, 2016: Steroids
Monika Šrámková, Michaela Dušková, Martin Hill, Marie Bičíková, Daniela Řípová, Pavel Mohr, Luboslav Stárka
OBJECTIVE: Anxiety and mood disorders (AMD) are the most frequent mental disorders in the human population. They have recently shown increasing prevalence, and commonly disrupt personal and working lives. The aim of our study was to analyze the spectrum of circulating steroids in order to discover differences that could potentially be markers of affective depression or anxiety, and identify which steroids could be a predictive component for these diseases. METHODS: We studied the steroid metabolome including 47 analytes in 20 men with depression (group D), 20 men with anxiety (group AN) and 30 healthy controls...
November 18, 2016: Steroids
Yuanyuan Liu, Yu Wang, Xi Chen, Qiaqing Wu, Min Wang, Dunming Zhu, Yanhe Ma
The reduction of 17-oxosteroids to 17β-hydroxysteroids is one of the important transformations for the preparation of many steroidal drugs and intermediates. The strain Zygowilliopsis sp. WY7905 was found to catalyze the reduction of C-17 carbonyl group of androst-4-ene-3,17-dione (AD) to give testosterone (TS) as the sole product by the constitutive 17β-hydroxysteroid dehydrogenase (17β-HSD). The optimal conditions for the reduction were pH 8.0 and 30°C with supplementing 10g/l glucose and 1% Tween 80 (w/v)...
November 15, 2016: Steroids
Galina Sukhodolskaya, Victoria Fokina, Andrei Shutov, Vera Nikolayeva, Tatiana Savinova, Yuri Grishin, Alexey Kazantsev, Nikolay Lukashev, Marina Donova
The newly synthesized (α/β)-diastereomers of 6-(N-methyl-N-phenyl)aminomethylandrost-4-ene-3,17-dione (5) and 6-(N-methyl-N-phenyl)aminomethylandrost-4-en-17β-ol-3-one (6) were firstly investigated as substrates for the whole cells of Nocardioides simplex VKM Ac-2033D in comparison with their unsubstituted analogs, - androst-4-ene-3,17-dione (1) and androst-4-en-17β-ol-3-one (2). 1(2)-Dehydroderivatives were identified as the major bioconversion products from all the substrates tested. When using the mixtures of (α/β)-stereoisomers of 5 and 6 as the substrates, only β-stereoisomers of the corresponding 1,4-diene-steroids were formed...
November 15, 2016: Steroids
Masood-Ur-Rahman, Younis Mohammad, Khalid Majid Fazili, Khursheed Ahmad Bhat, Tabassum Ara
Diosgenin, a promising anticancer steroidal sapogenin, was isolated from Dioscorea deltoidea. Keeping its stereochemistry rich architecture intact, a scheme for the synthesis of novel diosgenin analogues was designed using Cu (I)-catalysed alkyne-azide cycloaddition in order to study their structure-activity relationship. Both diosgenin and its analogues exhibited interesting anti-proliferative effect against four human cancer cell lines viz. HBL-100 (breast), A549 (lung), HT-29 (colon) and HCT-116 (colon) using [3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazoliumbromide] (MTT) assay...
November 15, 2016: Steroids
Sylvia J Gasparini, Marie-Christin Weber, Holger Henneicke, Sarah Kim, Hong Zhou, Markus J Seibel
In order to investigate the effects of glucocorticoid excess in rodent models, reliable methods of continuous glucocorticoid delivery are essential. The current study compares two methods of corticosterone (CS) delivery in regards to their ability to induce typical adverse outcomes such as fat accrual, insulin resistance, sarcopenia and bone loss. Eight-week-old mice received CS for 4weeks either via the drinking water (25-100μgCS/mL) or through weekly surgical implantation of slow release pellets containing 1...
November 2, 2016: Steroids
Luiz Gustavo de Almeida Chuffa, Luiz Antonio Lupi-Júnior, Aline Balandis Costa, João Paulo de Arruda Amorim, Fábio Rodrigues Ferreira Seiva
Sex steroids have been widely described to be associated with a number of human diseases, including hormone-dependent tumors. Several studies have been concerned about the factors regulating the availability of sex steroids and its importance in the pathophysiological aspects of the reproductive cancers in women. In premenopausal women, large fluctuations in the concentration of circulating estradiol (E2) and progesterone (P4) orchestrate many events across the menstrual cycle. After menopause, the levels of circulating E2 and P4 decline but remain at high concentration in the peripheral tissues...
February 2017: Steroids
Gyula Schneider, Anita Kiss, Erzsébet Mernyák, Zsanett Benke, János Wölfling, Éva Frank, Noémi Bózsity, András Gyovai, Renáta Minorics, István Zupkó
No abstract text is available yet for this article.
January 2017: Steroids
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