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Steroids

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https://www.readbyqxmd.com/read/27916502/renaissance-of-isoprenoids-research
#1
EDITORIAL
Vladimir A Khripach, Pavel B Drašar
No abstract text is available yet for this article.
December 1, 2016: Steroids
https://www.readbyqxmd.com/read/27913097/effect-of-24-epibrassinolide-on-brassica-napus-alternative-respiratory-pathway-guard-cells-movements-and-phospholipid-signaling-under-salt-stress
#2
Michael Derevyanchuk, Sergii Kretynin, Oksana Iakovenko, Raisa Litvinovskaya, Vladimir Zhabinskii, Jan Martinec, Yaroslav Blume, Vladimir Khripach, Volodymyr Kravets
Using Brassica napus roots we observed statistically significant increase in alternative respiratory pathway in response to exogenous 24-epibrassinolide (EBL) under optimal conditions and salinity. Also we observed activation of phospholipid signaling under the same conditions in response to EBL by measuring levels of lipid second messengers - diacylglycerol (DAG) and phosphatidic acid (PA). We found that brassinosteroids cause closure of stomata in isolated leaf disks while inhibitors of alternative oxidase cancelled these effects...
November 29, 2016: Steroids
https://www.readbyqxmd.com/read/27913096/a-sensitive-and-accurate-lc-ms-ms-assay-with-the-derivatization-of-1amino4methylpiperazine-applied-to-serum-allopregnanolone-pregnenolone-and-androsterone-in-pre-and-postmenopausal-women
#3
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
https://www.readbyqxmd.com/read/27876568/design-synthesis-and-biological-evaluation-of-steroidal-analogs-as-estrogenic-anti-estrogenic-agents
#4
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 5.49 μM, while LA-10 did not show any binding affinity towards neither ER-α nor ER-β; suggesting another mechanism for inhibition...
November 19, 2016: Steroids
https://www.readbyqxmd.com/read/27871861/the-role-of-steroids-in-the-prediction-of-affective-disorders-in-adult-men
#5
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
https://www.readbyqxmd.com/read/27864020/regio-and-stereoselective-reduction-of-17-oxosteroids-to-17%C3%AE-hydroxysteroids-by-a-yeast-strain-zygowilliopsis-sp-wy7905
#6
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
https://www.readbyqxmd.com/read/27864019/bioconversion-of-6-n-methyl-n-phenyl-aminomethyl-androstane-steroids-by-nocardioides-simplex
#7
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
https://www.readbyqxmd.com/read/27864018/synthesis-and-biological-evaluation-of-novel-3-o-tethered-triazoles-of-diosgenin-as-potent-antiproliferative-agents
#8
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
https://www.readbyqxmd.com/read/27815034/continuous-corticosterone-delivery-via-the-drinking-water-or-pellet-implantation-a-comparative-study-in-mice
#9
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
https://www.readbyqxmd.com/read/27815033/brassinosteroid-induced-changes-of-lipid-composition-in-leaves-of-pisum-sativum-l-during-senescence
#10
Evgenia Fedina, Andrey Yarin, Faimya Mukhitova, Alexander Blufard, Ivan Chechetkin
The effect of steroid phytohormone 24-epibrassinolide (EBR) on the composition of some lipid classes (free fatty acids, triacylglycerols and galactolipids) in detached pea leaves was studied for the first time. EBR (0.1μM) promoted senescence and increased the content of 14:0, 16:0 and 18:1 free fatty acids as well as 18:2 and 18:3 bound to triacylglycerols in the detached leaves in contrast to mock-treated leaves. The content of all identified fatty acids bound to galactolipids decreased in the detached leaves treated with EBR compared to that in mock-treated leaves...
November 2, 2016: Steroids
https://www.readbyqxmd.com/read/27789379/a-new-label-free-screen-for-steroid-5%C3%AE-reductase-inhibitors-using-lc-ms
#11
Jukkarin Srivilai, Karma Rabgay, Nantaka Khorana, Neti Waranuch, Nitra Nuengchamnong, Kornkanok Ingkaninan
Steroid 5α-reductase (S5αR) plays an important role in metabolizing testosterone into active androgen dihydrotestosterone (DHT) which is involved in many androgen dependent disorders, such as androgenic alopecia, benign prostatic hyperplasia and acne. The method for screening for S5αR inhibition is key in finding new antagonists. In this study, the label-free S5αR inhibitory assay using LC-MS was developed. S5αR type 1 enzyme was obtained from LNCaP prostate cancer cells. The enzymatic assay was optimised for enzyme-substrate (testosterone) concentration, NADPH-cofactor concentration, solvent tolerance, enzyme activity stability and incubation time...
October 24, 2016: Steroids
https://www.readbyqxmd.com/read/27770617/design-synthesis-of-methotrexate-diosgenin-conjugates-and-biological-evaluation-of-their-effect-on-methotrexate-transport-resistant-cells
#12
Bangrong Cai, Aimei Liao, Kyung-Ku Lee, Jae-Sam Ban, Hyun-Sam Yang, Young Jun Im, ChangJu Chun
A series of methotrexate-diosgenin conjugates was designed and synthesized to enhance the passive internalization of methotrexate (MTX) into transport-resistant cells. The inhibitory effects of these conjugates on dihydrofolate reductase (DHFR), and their anti-proliferation behaviors against a transport-resistant breast cancer cell line, MDA-MB-231, were investigated. All of the synthesized conjugates retained an ability to inhibit DHFR after the diosgenin substitution. The MTX conjugates were much more potent against methotrexate-resistant MDA-MB-231 cells than MTX...
October 19, 2016: Steroids
https://www.readbyqxmd.com/read/27770616/antiproliferative-and-anti-inflammatory-furostanol-saponins-from-the-rhizomes-of-tupistra-chinensis
#13
Limin Xiang, Yihai Wang, Xiaomin Yi, Xiangjiu He
Phytochemical investigations of the rhizome of Tupistra chinensis led to the isolation of ten new furostanol saponins along with fourteen known spirostanols. Their chemical structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, MS, and GC analyses. The antiproliferative effects against FaDu and Detroit 562 cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds...
October 19, 2016: Steroids
https://www.readbyqxmd.com/read/27756542/cholesterol-photo-oxidation-a-chemical-reaction-network-for-kinetic-modeling
#14
Carlo Barnaba, Maria Teresa Rodríguez-Estrada, Giovanni Lercker, Hugo Sergio García, Ilce Gabriela Medina-Meza
In this work we studied the effect of polyunsaturated fatty acids (PUFAs) methyl esters on cholesterol photo-induced oxidation. The oxidative routes were modeled with a chemical reaction network (CRN), which represents the first application of CRN to the oxidative degradation of a food-related lipid matrix. Docosahexaenoic acid (DHA, T-I), eicosapentaenoic acid (EPA, T-II) and a mixture of both (T-III) were added to cholesterol using hematoporphyrin as sensitizer, and were exposed to a fluorescent lamp for 48h...
October 15, 2016: Steroids
https://www.readbyqxmd.com/read/27725099/modulation-of-the-circadian-clock-by-glucocorticoid-receptor-isoforms-in-the-h295r-cell-line
#15
Zsolt Nagy, Alexa Marta, Henriett Butz, Istvan Liko, Karoly Racz, Attila Patocs
Peripheral clocks are set by different nervous, hormonal and metabolic stimuli, and regulate the circadian expression of several genes. We investigated whether a peripheral clock could be induced in the human adrenocortical cell line H295R and whether glucocorticoid receptor isoforms (GRα and GRß) are involved in this clock system. After synchronization of cells with serum shock, the rhythmic oscillation of clock genes PER1, PER2, REV-ERBα, and ARNTL was confirmed. In addition, H295R cells even without serum shock showed rhythmic expression of PER1, PER2, CRY1 and ARNTL...
October 8, 2016: Steroids
https://www.readbyqxmd.com/read/27692994/synthesis-of-monomeric-and-dimeric-steroids-containing-1-2-4-triazolo-1-5-a-pyrimidines
#16
Ailed Arenas-González, Luis Antonio Mendez-Delgado, Penélope Merino-Montiel, José M Padrón, Sara Montiel-Smith, José Luis Vega-Báez, Socorro Meza-Reyes
The synthesis of several monomeric and dimeric steroidal [1,2,4]triazolo[1,5-a]pyrimidines (TPs) derived from steroids are described. These derivatives were prepared from α,β-unsaturated carbonyl compounds through a Claisen Schmidt condensation and rearrangement of the spiro moiety followed by a cycloaddition with 3-amino-1,2,4-triazole. The antiproliferative activity of compounds 7, 13-15 was tested against human cancer cells; several IG50 values were below 10μM.
October 6, 2016: Steroids
https://www.readbyqxmd.com/read/27718364/uptake-and-metabolism-of-fluorescent-steroids-by-mycobacterial-cells
#17
Yaroslav Faletrov, Anna Brzostek, Renata Plocinska, Jarosław Dziadek, Elena Rudaya, Irina Edimecheva, Vladimir Shkumatov
Fluorescent steroids BODIPY-cholesterol (BPCh) and 7-nitrobenzoxadiazole-4-amino-(NBD)-labeled 22-NBD-chelesterol (22NC) as well as synthesized 20-(NBD)-pregn-5-en-3β-ol (20NP) were found to undergo bioconversions by Mycobacterium tuberculosis H37Rv and M. smegmatis mc(2) 155. The major fluorescent products were determined to be 4-en-3-one derivatives of the compounds. Degradation of NBD fluorophore was also detected in the cases of 22NC and 20NP, but neither NBD degradation nor steroidal part modification were observed for the synthesized 3-(NBD)-cholestane...
October 5, 2016: Steroids
https://www.readbyqxmd.com/read/27697501/deoxycholic-acid-derivatives-as-inhibitors-of-p-glycoprotein-mediated-multidrug-efflux
#18
Luc Rocheblave, Marc Rolland de Ravel, Elodie Monniot, Jeremy Tavenard, Claude-Yves Cuilleron, Catherine Grenot, Sylvie Radix, Eva-Laure Matera, Charles Dumontet, Nadia Walchshofer
Deoxycholic acid derivatives were designed as P-glycoprotein (Pgp, ABCB1) inhibitors. Thus the synthesis and the biological activity of methyl deoxycholate derivatives 5-10 and their ether analogs 15-20 have been reported. The potency of these compounds to modulate Pgp-mediated MDR was evaluated through daunorubicin accumulation and potentiation of doxorubicin cytotoxicity in K562/R7 multidrug resistant cells overexpressing Pgp. In parallel, their intrinsic toxicity was appreciated on K562 sensitive cells. Methyl 12α-[(2R or 2S) tetrahydro-2H-pyran-2-yloxy]-3-oxo-5β-cholan-24-oate 9b has shown a good efficiency as a Pgp inhibitor and a low intrinsic toxicity...
September 30, 2016: Steroids
https://www.readbyqxmd.com/read/27693094/stereoselectivity-of-formation-of-monoterpene-amino-acids-hybrid-molecules-in-the-reaction-of-monoterpene-nitroso-chlorides-with-%C3%AE-amino-acid-derivatives
#19
K S Marenin, Yu V Gatilov, A M Agafontsev, A V Tkachev
Reaction of nitrosochlorides of natural monoterpene hydrocarbons (+)-3-carene and (-)-α-pinene with L-amino acids and their methyl esters results in stereoselective formation of terpene-amino acids hybrids, which belong to the series of α-substituted amino oximes. The reaction with an excess of racemic DL-amino acids and their derivatives induces partial resolution of the amino acid components and formation of the diastereomeric mixtures of the terpene-amino acids hybrids, with diastereomeric excess varying from 0 to 100%...
September 28, 2016: Steroids
https://www.readbyqxmd.com/read/27665527/development-of-a-high-yielding-bioprocess-for-11-%C3%AE-hydroxylation-of-canrenone-under-conditions-of-oxygen-enriched-air-supply
#20
Martina Letizia Contente, Benedetta Guidi, Immacolata Serra, Valerio De Vitis, Diego Romano, Andrea Pinto, Roberto Lenna, Ricardo Pinheiro de Souza Oliveira, Francesco Molinari
A high yielding bioprocess for 11-α hydroxylation of canrenone (1a) using Aspergillus ochraceus ATCC 18500 was developed. The optimization of the biotransformation involved both fermentation (for achieving highly active mycelium of A. ochraceus) and biotransformation with the aim to obtain 11-α hydroxylation with high selectivity and yield. A medium based on sucrose as C-source resulted particularly suitable for conversion of canrenone into the corresponding 11-hydroxy derivative, whereas the use of O2-enriched air and dimethyl sulfoxide (DMSO) as a co-solvent for increasing substrate solubility played a crucial role for obtaining high yields (>95%) of the desired product in high chemical purity starting from 30mM (10...
September 22, 2016: Steroids
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