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steroid synthesis

Dejun Xu, Huanshan He, Xiaohan Jiang, Lulu Yang, Dinbang Liu, Li Yang, Guoxia Geng, Jianyong Cheng, Huali Chen, Rongmao Hua, Jiaxin Duan, Xiaoya Li, Lin Wu, Yuan Li, Qingwang Li
Steroid hormones are required for normal reproductive function of female. The aim of this study was to investigate the role of Raf-ERK1/2 on steroid hormone synthesis in bovine ovarian granulosa cells. Immunohistochemistry assay showed that both B-Raf and C-Raf were expressed in granulosa cells, theca cells and sertoli cells. The protein expression of Raf or ERK1/2 was clearly decreased by Raf inhibitor GSK2118436 or ERK1/2 inhibitor SCH772984, respectively (P<0.05). In addition, western blotting was performed for investigating the cross-talk between Raf and ERK1/2, the data showed that Raf positively regulated ERK1/2, whereas, ERK1/2 played a negative feedback effect on Raf...
February 20, 2019: Reproduction in Domestic Animals, Zuchthygiene
Manikanta Murahari, Vivek Mahajan, Sreenivasulu Neeladri, Maushmi S Kumar, Y C Mayur
The design and synthesis of novel pyrazole based derivatives has been carried out using the ligand based approach like pharmacophore and QSAR modelling of reported pyrazoles from the available literature to investigate the chemical features that are essential for the design of selective and potent COX-2 inhibitors. Both pharmacophore and QSAR models with good statistical parameters were selected for the design of the lead molecule. Also by exploiting the chemical structures of selective and marketed COX-2 inhibitors, celecoxib and SC-558 were used in designing the molecules which are used in the treatment of inflammation and related disorders...
February 14, 2019: Bioorganic Chemistry
Sarah Akbib, Jordy Stichelmans, Geert Stangé, Zhidong Ling, Zerihun Assefa, Karine H Hellemans
Cell therapy for diabetes could benefit from the identification of small-molecule compounds that increase the number of functional pancreatic beta cells. Using a newly developed screening assay, we previously identified glucocorticoids as potent stimulators of human and rat beta cell proliferation. We now compare the stimulatory action of these steroid hormones to a selection of checkpoint tyrosine kinase inhibitors that were also found to activate the cell cycle-in beta cells and analyzed their respective effects on DNA-synthesis, beta cell numbers and expression of cell cycle regulators...
2019: PloS One
Wolfgang Dohle, Andrea E Prota, Grégory Menchon, Ernest Hamel, Michel O Steinmetz, Barry V L Potter
Tetrahydroisoquinoline (THIQ) 6- O -sulfamate-based anticancer agents, inspired by the endogenous steroid 2-methoxyestradiol and its sulfamate derivatives, are further explored for antiproliferative and microtubule disruptor activity. Based on recently designed C3-methyl C7-methoxy-substituted THIQ derivatives, compounds with mono- and dichloro-substitutions on the pendant N -benzyl ring were synthesized and evaluated. Although improved antiproliferative activity was observed, for example, 4a versus 4b and 4b versus 8c , it was relatively modest...
January 31, 2019: ACS Omega
Nikolaos Nikolaou, Laura L Gathercole, Lucy Kirkwood, James E Dunford, Beverly A Hughes, Lorna C Gilligan, Udo Oppermann, Trevor M Penning, Wiebke Arlt, Leanne Hodson, Jeremy W Tomlinson
Steroid hormones, including glucocorticoids and androgens, have potent actions to regulate many cellular processes within the liver. The steroid A-ring reductase, 5β-reductase (AKR1D1), is predominantly expressed in the liver, where it inactivates steroid hormones and, in addition, plays a crucial role in bile acid synthesis. However, the precise functional role of AKR1D1 to regulate steroid hormone action in vitro has not been demonstrated. We have therefore hypothesised that genetic manipulation of AKR1D1 has the potential to regulate glucocorticoid availability and action in human hepatocytes...
February 12, 2019: Journal of Steroid Biochemistry and Molecular Biology
Noor Atatreh, Amal M Youssef, Mohammad A Ghattas, Mohammad Al Sorkhy, Sara Alrawashdeh, Khaled B Al-Harbi, Ibrahim M El-Ashmawy, Tariq I Almundarij, Amani A Abdelghani, Alaa S Abd-El-Aziz
In this study, the acid chlorides of pyrazolo[3,4-d]pyrimidine compounds were prepared and reacted with a number of nucleophiles. The novel compounds were experimentally tested via enzyme assay and they showed cyclooxygenase-2 inhibition activity in the middle micro molar range (4b had a COX-1 IC50 of 26 µM and a COX-2 IC50 of 34 µM, 3b had a COX-1 IC50 of 19 µM and a COX-2 IC50 of 31 µM, 3a had a COX-2 IC50 of 42 µM). These compounds were analyzed via docking and were predicted to interact with some of the COX-2 key residues...
February 5, 2019: Bioorganic Chemistry
Peter J O'Shaughnessy, Jean Philippe Antignac, Bruno Le Bizec, Marie-Line Morvan, Konstantin Svechnikov, Olle Söder, Iuliia Savchuk, Ana Monteiro, Ugo Soffientini, Zoe C Johnston, Michelle Bellingham, Denise Hough, Natasha Walker, Panagiotis Filis, Paul A Fowler
Masculinization of the external genitalia in humans is dependent on formation of 5α-dihydrotestosterone (DHT) through both the canonical androgenic pathway and an alternative (backdoor) pathway. The fetal testes are essential for canonical androgen production, but little is known about the synthesis of backdoor androgens, despite their known critical role in masculinization. In this study, we have measured plasma and tissue levels of endogenous steroids in second trimester human fetuses using multidimensional and high-resolution mass spectrometry...
February 2019: PLoS Biology
Alan Conley, Erin Lea Legacki, Cynthia Jo Corbin, Scott D Stanley, Carl Dahlen, Lawrence P Reynolds
Dexamethasone (DEX) initiates parturition by inducing progesterone withdrawal and affecting placental steroidogenesis, but the effects of DEX in fetal and maternal tissue steroid synthetic capacity remains poorly investigated. Blood was collected from cows at 270 days of gestation before DEX or saline (SAL) treatment, and blood and tissues were collected at slaughter 38 hours later. Steroid concentrations were determined by liquid chromatography tandem mass spectrometry to detect multiple steroids including 5α-reduced pregnane metabolites of progesterone...
February 1, 2019: Reproduction: the Official Journal of the Society for the Study of Fertility
Rajenahally Jagadeesh, Kathiravan Murugesan, Matthias Beller
The preparation of nickel nanoparticles as efficient reductive amination catalysts by pyrolysis of in situ generated Ni-tartaric acid complex on silica is presented. The resulting stable and reusable Ni-nanocatalyst enables the synthesis of functionalized and structurally diverse primary benzylic, heterocyclic and aliphatic amines starting from inexpensive and readily available carbonyl compounds and ammonia in presence of molecular hydrogen. Applying this Ni-based amination protocol, -NH2 moiety can be introduced in structurally complex compounds, e...
February 14, 2019: Angewandte Chemie
Xiaoping Xin, Zhonghui Li, Yuyi Zhong, Qingqing Li, Jiaying Wang, Hao Zhang, Xiaolong Yuan, Jiaqi Li, Zhe Zhang
Previous studies have strongly recommended that KISS-1 metastasis suppressor ( KISS1 ) plays an essential gatekeeper of the initiation of reproductive maturation in mammals. However, KISS1 has been recently reported to highly express in ovarian granulosa cells (GCs). But the biological functionalities of KISS1 on cell apoptosis, cell cycle, and synthesis of estradiol-17β (E2) have not been explored in GCs. In this study, using porcine GCs as a cellular model, the overexpression plasmid of KISS1 was built to explore the biological effects of KISS1 on the PI3K signaling pathway, estrogen signaling pathway, cell apoptosis, cell cycle, and E2 secretion...
February 12, 2019: Animals: An Open Access Journal From MDPI
Aliakbar Fazaeli, Abolfazl Golestani, Mostafa Lakzaei, Samaneh Sadat Rasi Varaei, Mahdi Aminian
Cholesterol oxidase is a bifunctional bacterial flavoenzyme which catalyzes oxidation and isomerization of cholesterol. This valuable enzyme has attracted a great deal of attention because of its wide application in the clinical laboratory, synthesis of steroid derived drugs, food industries, and its potentially insecticidal activity. Therefore, development of an efficient protocol for overproduction of cholesterol oxidase could be valuable and beneficial in this regard. The present study examined the role of various parameters (host strain, culture media, induction time, isopropyl ß-D-1-thiogalactopyranoside concentration, as well as post-induction incubation time and temperature) on over-expression of cholesterol oxidase from Chromobacterium sp...
2019: PloS One
Tokutaro Yamaguchi, Joo-Ho Lee, A-Rang Lim, Eun-Ji Yu, Tae-Jin Oh
Recently, 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 UDP-glucosyltransferase, glucoside synthesis was successful in linking β-D -glucopyranose and β-D -laminaribiose to 11α oxygen of 1 at a high conversion ratio, and full assignment structure was analyzed for the two glucosides by high-resolution quadrupole-time flight electrospray ionization-mass spectrometry, 1D (1 H and 13 C) NMR and 2D (COSY, ROESY, HSQC-DEPT and HMQC) NMR...
February 9, 2019: Steroids
Osman Ahmad, Janaina Nogueira, James E Heubi, Kenneth D R Setchell, Ambika P Ashraf
Vitamin D-deficiency rickets, not responding to large treatment doses of oral vitamin D, suggest rare receptor mutations, malabsorption, or hepatobiliary dysfunction. We present a set of twins of Hispanic origin who presented with refractory vitamin D-deficiency rickets and failure to thrive (FTT) at 6 months of age. On follow-up, mild elevations in serum alanine transaminases and normal aspartate aminotransferase were noted. Subsequently, patients manifested fat-soluble vitamin deficiencies. More targeted evaluations revealed a diagnosis of 3 β -hydroxy- Δ 5 -C27 -steroid oxidoreductase deficiency...
February 1, 2019: Journal of the Endocrine Society
Graham W Anderson, Christopher J Kenyon, Emad A S Al-Dujaili
Mechanisms to explain post-prandial increases in circulating glucocorticoids are not well understood and may involve increased adrenal secretion and/or altered steroid metabolism. We have compared salivary levels of cortisol and cortisone levels in healthy male and female volunteers fed either a low or cholesterol-rich midday meal. Urinary levels of steroids, bile acids and markers of lipid peroxidation were also measured. Males and females showed expected circadian changes in salivary steroids and postprandial peaks within 1h of feeding...
February 9, 2019: Nutrients
Nicola Pluchino, Yveline Ansaldi, Andrea R Genazzani
Allopregnanolone (ALLO) has a crucial role in brain development and remodeling. Reproductive transitions associated with endocrine changes affect synthesis and activity of ALLO with behavioral/affective consequences. Pregnancy is characterized by an increased synthesis of progesterone/ALLO by the placenta, maternal and fetal brains. This suggests the critical role of these steroids in maternal brain adaptation during pregnancy and the development of the fetal brain. ALLO is brain protective during complications of pregnancy, such as preterm delivery or intrauterine growth restriction (IUGR), reducing the impact of hypoxia, and excitotoxic brain damage...
February 11, 2019: Hormone Molecular Biology and Clinical Investigation
Nisal Gajadeera, Robert N Hanson
The 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 retain high ER affinity...
February 6, 2019: Steroids
Barbara Seroka, Zenon Łotowski, Agnieszka Wojtkielewicz, Przemysław Bazydło, Ewelina Dudź, Agnieszka Hryniewicka, Jacek W Morzycki
Two 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 acrylonitrile (in the case of 1,3-diamines), followed by the reduction of intermediate aminonitriles. Furthermore, the other two amines were synthesized from 16-dehydropregnenolone acetate using aza-Michael addition as a key step...
February 6, 2019: Steroids
Ivana Beara, Tatjana Majkić, Stefania Fioravanti, Laura Trulli, Neda Mimica-Dukić, Lucio Pellacani, Luciano Saso
BACKGROUND: Convenient approach to modulation of the inflammation is influence on production of inflammatory mediators - eicosanoids, generated in arachidonic acid (AA) metabolism. Common therapeutic activity of non-steroidal anti-inflammatory drugs (NSAID), such as aspirin, includes inhibition of two crucial enzymes of AA metabolism - cyclooxygenase-1 and -2 (COX-1/2), with certain risk for gastrointestinal and renal intolerance. Ever since enrolment of COX-2, particularly overabundance of its main products prostaglandin E2 (PGE2) and thromboxane A2 (TXA2) in numerous pathological processes was recognized, it became significant therapeutic target...
February 8, 2019: Medicinal Chemistry
Pradipta Jana, Md Mobidullah Khan, Subrata Kumar De, Asru K Sinha, Santanu Guha, Gausal A Khan, Smarajit Maiti
BACKGROUND: An increase in the level of cytokines like TNF-α and IL-6 causes the inflammatory surge in acute ischemic heart disease (AIHD). OBJECTIVE: A high-level dermcidin isoform-2 (DCN-2) occurrence in AIHD was subjected to determine a possible regulation on cytokines expression.Effect of estrogen to counteract the inflammatory response was determined. METHODS: Blood was collected from AIHD patients and normal volunteers with consent nitric oxide (NO) was done with methemoglobin method...
February 7, 2019: Current Molecular Medicine
Laurna Bullock, John Bedson, Joanne L Jordan, Bernadette Bartlam, Carolyn A Chew-Graham, Paul Campbell
OBJECTIVES: To describe the current literature on pain assessment and pain treatment for community-dwelling people with dementia. METHOD: A comprehensive systematic search of the literature with narrative synthesis was conducted. Eight major bibliographic databases were searched in October 2018. Titles, abstracts, and full-text articles were sequentially screened. Standardised data extraction and quality appraisal exercises were conducted. RESULTS: 32 studies were included in the review, 11 reporting findings on pain assessment tools or methods, and 27 reporting findings on treatments for pain...
February 6, 2019: International Journal of Geriatric Psychiatry
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