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https://www.readbyqxmd.com/read/28803210/investigation-of-ph-and-substituent-effects-on-the-distribution-ratio-of-novel-steroidal-ring-d-and-a-fused-arylpyrazole-regioisomers-and-evaluation-of-their-cell-growth-inhibitory-effects-in-vitro
#1
Ádám Baji, Ferenc Kovács, Gergő Mótyán, Gyula Schneider, János Wölfling, Izabella Sinka, István Zupkó, Imre Ocsovszki, Éva Frank
Novel androstanopyrazoles have been efficiently synthesized from steroidal β-ketoaldehydes with different arylhydrazine hydrochlorides both under acidic and basic conditions. Knorr-type transformations of 16-hydroxymethylene-dehydroepiandrosterone containing its 1,3-dicarbonyl moiety on ring D, proved to be regioselective in pyridine at room temperature, while mixtures of regioisomers were obtained in acidic EtOH under reflux. Contrarily, the cyclocondensation reactions of 2-hydroxymethylene-dihydrotestosterone bearing its reactive functionalities on ring A, led to a mixture of pyrazole regioisomers in varying ratio depending on the applied medium...
August 9, 2017: Steroids
https://www.readbyqxmd.com/read/28800142/alcohol-mediated-missplicing-of-mcl-1-pre-mrna-is-involved-in-neurotoxicity
#2
Rahsan Sariyer, Francesca I De Simone, Martina Donadoni, Jan B Hoek, Sulie L Chang, Ilker Kudret Sariyer
BACKGROUND: Heavy and chronic ethanol (EtOH) exposure can cause significant structural and functional damage to the adult brain. The most devastating consequence of EtOH exposure is the neurotoxicity associated with the depletion of neurons. Regulation of splice variants in the brain can modulate protein functions, which may ultimately affect behaviors associated with alcohol dependence and EtOH-mediated neurotoxicity. Since alcohol consumption is associated with neurotoxicity, it is possible that altered splicing of survival and pro-survival factors during the development of alcoholism may contribute to the neurotoxicity...
August 11, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/28790377/the-analgesic-activities-of-stauntonia-brachyanthera-and-ym11-through-regulating-inflammatory-mediators-and-directly-controlling-the-sodium-channel-prompt
#3
Dali Meng, Lei Wang, Jingnan Du, Jianchao Chen, Chao Chen, Wei Xu, Chunli Li
The analgesic studies on Stauntonia brachyanthera, a traditional Chinese folk medicine used to treat headache, pains and inflammatory diseases in local areas, showed that the EtOH extracts (EESB) and the characteristic ingredient YM11 could significantly inhibit the acetic acid-induced writhing responses by 43.1% and 78.95%, and decrease the xylene-induced ear edemas by 48.9% and 21.4%, respectively. EESB could significantly increase pain threshold of mice in hot-plate test, but the effect of YM11 was not obviously...
August 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28783086/bioactive-constituents-from-the-whole-plants-of-gentianella-acuta-michx-hulten
#4
Zhijuan Ding, Yanxia Liu, Jingya Ruan, Shengcai Yang, Haiyang Yu, Meiling Chen, Yi Zhang, Tao Wang
As a Mongolian native medicine and Ewenki folk medicinal plant, Gentianella acuta has been widely used for the treatment of diarrhea, hepatitis, arrhythmia, and coronary heart disease. In the course of investigating efficacy compounds to treat diarrhea using a mouse isolated intestine tissue model, we found 70% EtOH extract of G. acuta whole plants had an inhibitory effect on intestine contraction tension. Here, nineteen constituents, including five new compounds, named as gentiiridosides A (1), B (2), gentilignanoside A (3), (1R)-2,2,3-trimethyl-4-hydroxymethylcyclopent-3-ene-1-methyl-O-β-d-glucopyranoside (4), and (3Z)-3-hexene-1,5-diol 1-O-α-l-arabinopyranosyl(1→6)-β-d-glucopyranoside (5) were obtained from it...
August 6, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28782661/clinical-impact-of-small-advanced-gastric-cancer-%C3%A2-40%C3%A2-mm-in-elderly-patients-a-retrospective-cohort-study
#5
Yoshitake Ueda, Hajime Fujishima, Teijiro Hirashita, Hidefumi Shiroshita, Tsuyoshi Etoh, Masafumi Inomata, Norio Shiraishi
OBJECTIVES: Recently, the incidence of small advanced gastric cancer has been increasing in elderly patients. To clarify the clinical impact of small advanced gastric cancer (≤40 mm) in elderly patients, short- and long-term outcomes after gastrectomy for this disease were examined and compared with those for large gastric cancer. PATIENTS AND METHOD: Forty-seven patients aged 80 years or older with advanced gastric cancer (deeper than pT2) who underwent curative gastrectomy from 1998 to 2015 were enrolled in this study...
August 3, 2017: International Journal of Surgery
https://www.readbyqxmd.com/read/28774818/the-protective-effect-of-platelet-released-growth-factors-and-bone-augmentation-bio-oss-%C3%A2-on-ethanol-impaired-osteoblasts
#6
Tolga Taha Sönmez, Andreas Bayer, Tillman Cremer, Jennifer Vanessa Phi Hock, Bernd Lethaus, Nisreen Kweider, Christoph Jan Wruck, Wolf Drescher, Holger Jahr, Sebastian Lippross, Thomas Pufe, Mersedeh Tohidnezhad
BACKGROUND: Chronic alcohol consumption is a known limiting factor for bone healing. One promising strategy to improve bone augmentation techniques with Bio-Oss(®) in oral and maxillofacial surgery might be the supportive application of platelet-concentrated biomaterials as platelet-released growth factor (PRGF). To address this matter, we performed an in vitro study investigating the protective effects of PRGF and Bio-Oss(®) in ethanol (EtOH) treated osteoblasts. METHODS: The SAOS-2 osteosarcoma cell line, with and without EtOH pretreatment was used...
July 31, 2017: Annals of Anatomy, Anatomischer Anzeiger: Official Organ of the Anatomische Gesellschaft
https://www.readbyqxmd.com/read/28768933/7-hydroxy-3-methyleneisoindolin-1-one-as-a-new-esipt-fluorescent-probe-to-monitor-aqueous-environments
#7
Yusuke Kimuro, Kazuteru Usui, Satoru Karasawa, Go Hirai, Mariko Aso
A 7-hydroxy derivative of 3-methyleneisoindolin-1-one 1 was synthesized and its properties as a new fluorophore undergoing excited-state intramolecular proton transfer (ESIPT) were investigated. In alcohols and dimethylsulfoxide, 1 exhibited dual emission at ca. 380 and 525-540 nm when excited at ca. 336 nm, which agreed well with the density functional theory (DFT) and time-dependent (TD)-DFT-calculated emission predictions of 1 and its ESIPT tautomer. In aqueous solutions at near neutral pH, 1 exhibited a broad emission band at ca...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28766388/surgical-training-with-live-animal-models-for-laparoscopic-gastrectomy
#8
Yoshitake Ueda, Norio Shiraishi, Teijiro Hirashita, Tsuyoshi Etoh, Masafumi Inomata, Seigo Kitano
No abstract text is available yet for this article.
August 1, 2017: Surgical Innovation
https://www.readbyqxmd.com/read/28765564/acceleration-of-batch-type-heterogeneous-ligand-free-suzuki-miyaura-reactions-with-polymer-composite-supported-pd-catalyst
#9
Mian Wang, Han Xue, Fei Ju, Haijie Yang
An efficient and recyclable palladium (II) catalyst supported on a double-structured amphiphilic polymer composite was reported previously containing a polymer hydrogel within macroporous polystyrene (PS) microspheres. However, some critical questions have been unaddressed. First, the catalyst accelerated the heterogeneous ligand-free batch Suzuki-Miyaura reaction in a H2O/EtOH mixture solution at room temperature in the presence of air, which could be ascribed to the "on-water" effect taking place at the interface of the aqueous-organic and basic-aqueous phases created by sodium carbonate in H2O/EtOH...
August 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28765086/spectrum-of-atrial-arrhythmias-using-the-ligament-of-marshall-in-patients-with-atrial-fibrillation
#10
Aman Chugh, Hitinder S Gurm, Kavita Krishnasamy, Mohammed Saeed, Watchara Lohawijarn, Kyle Hornsby, Ryan Cunnane, Hamid Ghanbari, Rakesh Latchamsetty, Thomas Crawford, Krit Jongnarangsin, Frank Bogun, Hakan Oral, Fred Morady
BACKGROUND: The role of the ligament of Marshall (LOM) in patients with atrial fibrillation (AF) has not been well defined. OBJECTIVE: The purpose of this study was to describe the role of the LOM in patients with AF and related arrhythmias. METHODS: Fifty-six patients (mean age 63 ± 11 years; persistent AF in 48 [86%]; ejection fraction 0.49 ± 0.13; left atrial diameter 4.7 ± 0.6 cm) with LOM-mediated arrhythmias were included. RESULTS: A LOM-pulmonary vein (PV) connection was present in 18 patients (32%) and was eliminated with radiofrequency (RF) ablation at the left lateral ridge or crux (n = 12), at the mitral annulus (n = 3), or with alcohol/ethanol (EtOH) ablation of the vein of Marshall (VOM; n = 3)...
July 29, 2017: Heart Rhythm: the Official Journal of the Heart Rhythm Society
https://www.readbyqxmd.com/read/28762981/crystal-structure-and-luminescent-properties-of-novel-coordination-polymers-constructed-with-bifurandicarboxylic-acid
#11
Xianyu Huang, Daoliang Chen, Mingrui He, Jianfeng Li, Jiawei Huang, Baolin Li
Four novel coordination polymers (CPs) assembled with [2,2'-bifuran]-5,5'-dicarboxylic acid (H2L) and metal ions Zn(II), Cd(II) or Co(II) have been successfully synthesized. Their molecular structures have been determined to be Zn(L)(H2O)2 (1), [Zn(L)(DMF)]2 (2), [Cd(L)(EtOH)(DMF)2]2 (3) and Co(L)(H2O)4·(H2O)2 (4) by crystallographic analysis. It is found that (2) exhibits a two-dimensional infinite framework, whereas the others exhibit a one-dimensional framework. Both (2) and (3) exhibit ligand-based emission which is blue-shifted compared with the emission from the H2L ligand...
August 1, 2017: Acta Crystallographica Section B, Structural Science, Crystal Engineering and Materials
https://www.readbyqxmd.com/read/28760662/acute-ethanol-modulation-of-neurocircuit-function-in-the-nucleus-of-the-tractus-solitarius
#12
Michael A Aimino, Caitlin Coker, Yuval Silberman
The nucleus of the tractus solitarius (NTS) is a brain stem region critical to many physiologic processes and has been implicated in addiction to multiple classes of abused drugs, including alcohol (EtOH). That said, the mechanism by which EtOH modulates NTS neurocircuit activity is not well characterized and has yet to be examined utilizing electrophysiologic methods in mouse models of alcohol use disorders. To begin to address this gap in knowledge, we sought to use whole-cell and cell-attached recordings to determine the mechanism of acute EtOH action on GABAergic and glutamatergic neurotransmission, as well as on action potential firing in the NTS of adult male, EtOH naïve mice...
July 28, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28759992/a-tandem-synthesis-of-%C3%AE-diazoketones-from-1-3-diketones
#13
Jianlan Zhang, Wenwen Chen, Dayun Huang, Xiaobao Zeng, Xinyan Wang, Yuefei Hu
A highly efficient synthesis of α-diazoketone was achieved by simply stirring the mixture of 1,3-diketone, TsN3 and MeNH2 in EtOH. It was a tandem reaction including a novel primary amine-catalyzed Regitz diazo-transfer of 1,3-diketone and a novel primary amine-mediated C-C bond cleavage of 2-diazo-1,3-diketone.
August 1, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28753742/stress-facilitates-the-development-of-cognitive-dysfunction-after-chronic-ethanol-exposure
#14
Ellen M Rodberg, Carolina R den Hartog, Rachel I Anderson, Howard C Becker, David E Moorman, Elena M Vazey
BACKGROUND: Chronic exposure to stress or alcohol can drive neuroadaptations that alter cognition. Alterations in cognition may contribute to alcohol use disorders by reducing cognitive control over drinking and maintenance of abstinence. Here we examined effects of combined ethanol (EtOH) and stress exposure on prefrontal cortex (PFC)-dependent cognition. METHODS: Adult male C57BL/6J mice were trained to drink EtOH (15%, v/v) on a 1 h/d 1-bottle schedule. Once stable, mice were exposed to cycles of chronic intermittent EtOH (CIE) or air-control vapor exposure (Air), followed by test cycles of 1 h/d EtOH drinking...
July 28, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/28749689/superacidic-cyclization-of-activated-anthranilonitriles-into-2-unsubstituted-4-aminoquinolines
#15
Hubert Lavrard, Paolo Larini, Florence Popowycz
4-Aminoquinolines were prepared in a three-step synthesis starting from substituted anthranilonitriles. The condensation on 1,1,1-trichloro-4-ethoxybut-3-enone proceeded efficiently either neat or in refluxing EtOH. Cyclization in superacidic trifluoromethanesulfonic acid provided unstable intermediate, which upon treatment with NaOEt in ethanol, afforded the expected esters. Theoretical investigations pointed out a monoprotonated nitrilium as the reactive species during the cyclization process.
July 27, 2017: Organic Letters
https://www.readbyqxmd.com/read/28744261/antifungal-potential-of-copper-ii-manganese-ii-and-silver-i-1-10-phenanthroline-chelates-against-multidrug-resistant-fungal-species-forming-the-candida-haemulonii-complex-impact-on-the-planktonic-and-biofilm-lifestyles
#16
Rafael M Gandra, Pauraic Mc Carron, Mariana F Fernandes, Lívia S Ramos, Thaís P Mello, Ana Carolina Aor, Marta H Branquinha, Malachy McCann, Michael Devereux, André L S Santos
Candida haemulonii, Candida haemulonii var. vulnera and Candida duobushaemulonii, which form the C. haemulonii complex, are emerging etiologic agents of fungal infections known to be resistant to the most commonly used antifungals. The well-established anti-Candida potential of metal complexes containing 1,10-phenanthroline (phen) ligands encouraged us to evaluate different copper(II), manganese(II), and silver(I) phen chelates for their ability to inhibit planktonic growth and biofilm of C. haemulonii species complex...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28741978/effects-of-co-exposure-to-atrazine-and-ethanol-on-the-oxidative-damage-of-kidney-and-liver-in-wistar-rats
#17
Sunny O Abarikwu, Queen C Duru, Rex-Clovis C Njoku, Benjamin A Amadi, Aseme Tamunoibuomie, Enebimoere Keboh
Both ethanol (EtoH) and atrazine (ATZ) have hepatic and nephro-toxic effects in rats. In the present study, the toxicity of EtoH (5 g kg(-1)) on the kidney and liver in the absence or in the presence of different doses of ATZ (50, 100, 300 mg kg(-1)) was evaluated after 21 days in rats. Results showed that the mixture effects on catalase and superoxide dismutase activities were more severe in both tissues compared to EtoH alone, especially as the dose of ATZ was increased. Hepatic malondialdehyde level (an index of lipid peroxidation) was increased from 20...
November 2017: Renal Failure
https://www.readbyqxmd.com/read/28739177/triterpenoids-from-the-bark-of-dysoxylum-hainanense-and-their-anti-inflammatory-and-radical-scavenging-activity
#18
Yu-Hai Zou, Wen-Ting Liu, Jin-Xia Zhang, Ding-Cheng Xiang
A phytochemical investigation on the 70% EtOH extract of the bark of Dysoxylum hainanense resulted in the isolation of four new triterpenoids, dysoxyhaines A-D (1-4). Structural elucidation of all the compounds were performed by spectral methods such as 1D and 2D ((1)H(1)H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated components were evaluated in vitro for anti-inflammatory activities for Cox-1 and Cox-2, and radical scavenging potential using ABTS(·+) and DPPH test...
July 21, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28732851/nanoparticle-assisted-solvent-selective-transdermal-combination-therapy-of-curcumin-and-5-flurouracil-for-efficient-cancer-treatment
#19
T S Anirudhan, Anoop S Nair, Sabari J Bino
Skin cancer is one among the many prominent diseases of the modern world and millions of people are suffering due to the lack of proper medication. Even though transdermal drug delivery systems (TDDS) provide an efficient route of drug administration, the advantages of combination chemotherapy have rarely been extended into TDDS. In the present work, a polymer capable of simultaneously encapsulating two anti-cancer drugs: 5-flurouracil (5-FU) and curcumin (CUR), and releasing them with varying kinetics as a function of the leaching solvent was developed...
October 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28730708/evaluation-of-the-hypocholesterolemic-effect-and-prebiotic-activity-of-a-lentil-lens-culinaris-medik-extract
#20
Maria Vittoria Micioni Di Bonaventura, Cinzia Cecchini, Pilar Vila Donat, Giovanni Caprioli, Carlo Cifani, Maria Magdalena Coman, Alberto Cresci, Dennis Fiorini, Massimo Ricciutelli, Stefania Silvi, Sauro Vittori, Gianni Sagratini
SCOPE: the aim of our work was to produce a hydroalcoholic extract of lentils and to examine: a) the hypocholesterolemic action in an animal model, by studying the plasma cholesterol level and the concentration of bile acids in the faeces; b) the potential prebiotic effect, by conducting an in vitro culture fermentation experiment and assessing the level of short chain fatty acids (SCFAs) in the faeces of rats. METHODS AND RESULTS: Lentil extract (LE) was obtained by extracting lentils with a solution of H2 0/EtOH (70/30 v/v) for 3 h, and the content of main nutrients was determined...
July 21, 2017: Molecular Nutrition & Food Research
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