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https://www.readbyqxmd.com/read/28036168/development-of-an-azoreductase-based-reporter-system-with-synthetic-fluorogenic-substrates
#1
Narae Shin, Kenjiro Hanaoka, Wen Piao, Takuya Miyakawa, Tomotsumi Fujisawa, Satoshi Takeuchi, Shodai Takahashi, Toru Komatsu, Tasuku Ueno, Takuya Terai, Tahei Tahara, Masaru Tanokura, Tetsuo Nagano, Yasuteru Urano
Enzyme/substrate pairs, such as β-galactosidase with chromogenic x-gal substrate, are widely used as reporters to monitor biological events, but there is still a requirement for new reporter systems, which may be orthogonal to existing systems. Here, we focused on azoreductase (AzoR). We designed and synthesized a library of azo rhodamine derivatives as candidate fluo-rogenic substrates. These derivatives were non-fluorescent, probably due to ultrafast conformational change around the N=N bond after photoexcitation...
December 30, 2016: ACS Chemical Biology
https://www.readbyqxmd.com/read/28027603/survival-implications-of-opioid-use-before-and-after-liver-transplantation
#2
Henry B Randall, Tarek Alhamad, Mark A Schnitzler, Zidong Zhang, Sophia Ford-Glanton, David A Axelrod, Dorry L Segev, Bertram L Kasiske, Gregory P Hess, Hui Yuan, Rosemary Ouseph, Krista L Lentine
BACKGROUND: Implications of prescription opioid use for outcomes after liver transplant have not been described. METHODS: We integrated national transplant registry data with records from a large pharmaceutical claims clearinghouse (2008-2014; n=26,925). Opioid fills on the waiting list were normalized to morphine equivalents (ME), and exposure was categorized as: >0 to 2 ME/day (level 1), >2 to 10 ME/day (level 2), >10 to 70 ME/day (level 3), and >70 ME/day (level 4)...
December 27, 2016: Liver Transplantation
https://www.readbyqxmd.com/read/28007499/3-hydroxy-4-methoxy-%C3%AE-methyl-%C3%AE-nitrostyrene-inhibits-tumor-growth-through-ros-generation-and-gsh-depletion-in-lung-cancer-cells
#3
Chun-Hao Tsai, Pei-Wen Hsieh, Yi-Chen Lee, Chie-Hong Wang, Wen-Chin Chiu, Chun-Wun Lu, Yen-Yun Wang, Stephen Chu-Sung Hu, Tain-Lu Cheng, Shyng-Shiou F Yuan
AIMS: Members of the β-nitrostyrene family are known to suppress tumor growth, with the underlying mechanisms of β-nitrostyrene remain mostly unclear. Herein, we synthesized a β-nitrostyrene derivative, 3'-hydroxy-4'-methoxy-β-methyl-β-nitrostyrene (CYT-Rx20), and explored its anticancer activities in human lung cancer cells in vitro and in vivo. MAIN METHODS: Cell viability was measured by XTT assay. Apoptosis was detected by Annexin V/PI staining. Caspase activation was determined by western blotting...
December 19, 2016: Life Sciences
https://www.readbyqxmd.com/read/27928078/polymerase-chain-reaction-based-assays-for-the-diagnosis-of-active-and-relapsed-cases-of-human-brucellosis
#4
Mohammad Reza Hasanjani Roushan, Seyed Mahmoud Amin Marashi, Zahra Moulana
This study aimed to compare polymerase chain reaction (PCR) with serum agglutination test (SAT) in the diagnosis of patients before and 6 months after treatment. Peripheral blood specimens from 50 patients with brucellosis (case group) and 30 subjects without brucellosis (control group) were selected and entered into the study. The diagnosis of brucellosis was established using SAT ≥ 1:160 and 2-mercaptoethanol (2-ME) ≥ 1:80 with clinical signs and symptoms compatible with brucellosis. For each case, both before treatment and 6 months after completion of therapy, SAT, 2-ME, and PCR were performed...
December 7, 2016: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/27923102/pain-treatment-continues-to-be-inaccessible-for-many-patients-around-the-globe-second-phase-of-opioid-price-watch-a-cross-sectional-study-to-monitor-the-prices-of-opioids
#5
Tania Pastrana, Roberto Wenk, Lukas Radbruch, Ebtesam Ahmed, Liliana De Lima
BACKGROUND: Strong opioids are a cornerstone of pain treatment, of which morphine is considered an essential analgesic by the World Health Organization. Access to opioids is limited, due to restrictive laws, limited education, and high prices. This is the second phase of a global project to monitor and report the dispensing price of opioids with the specific aim to expand and increase the information and allow further analysis of the challenges in their availability and affordability...
December 6, 2016: Journal of Palliative Medicine
https://www.readbyqxmd.com/read/27911395/preparation-of-primary-mixed-glial-cultures-from-adult-mouse-spinal-cord-tissue
#6
Jennifer T Malon, Ling Cao
It has been well-accepted that spinal cord glial responses contribute significantly to the development of neuropathic pain. Tremendous information regarding glial activities at the cellular and molecular levels has been obtained through in vitro cell culture systems. The in vitro systems utilized, mainly include primary glia derived from neonatal brain cortical tissue and immortalized cell lines. However, these systems may not reflect the characteristics of spinal cord glial cells in vivo. In order to further investigate the roles of spinal cord glial cells in the development of peripheral nerve injury-induced neuropathic pain using a culture system that better reflects the in vivo condition, our laboratory has developed a method to establish primary spinal cord mixed glial cultures from adult mice...
November 19, 2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27883247/2-methoxyestradiol-mediated-induction-of-frzb-contributes-to-cell-death-and-autophagy-in-mg63-osteosarcoma-cells
#7
Dalibel Bravo, Kristen L Shogren, Dongqing Zuo, Eric R Wagner, Gobinda Sarkar, Michael J Yaszemski, Avudaiappan Maran
Osteosarcoma is a bone tumor that mainly affects children and adolescents. Although its pathogenesis is still not fully understood, activation of Wnt signaling has been implicated in the development and metastasis of osteosarcoma. In this report, we have investigated the effect of the anti-tumor compound, 2-methoxyestradiol (2-ME) on Wnt antagonist frizzled-related protein b (Frzb), also known as secreted frizzled-related protein (sFRP)3 in human osteosarcoma (MG63) cells. Our results show that 2-ME treatment induces Frzb gene promoter activity, and increases Frzb mRNA and protein levels in osteosarcoma cells...
November 24, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27866494/brucellosis-as-a-neglected-disease-in-a-neglected-population-a-seroepidemiological-study-of-migratory-nomads-in-the-fars-province-of-iran
#8
B Honarvar, M Moghadami, K B Lankarani, M A Davarpanah, M Ataolahi, A Farbod, E Eskandari, M Panahi, A Ghorbani, Z Zahiri, R Tabrizi, M Pourjafar, S M M Heidari
This study assessed the seroprevalence of brucellosis and its risk factors in migratory nomads in the Fars province of Iran. Active brucellosis was defined as the combination of clinical symptoms, including fever, chills, night sweats, headache, low back pain, arthralgia, or myalgia, and positive laboratory testing, including either a serum agglutination test (SAT) ⩾1:80 with a 2-mercaptoethanol (2-ME) test ⩾1:40, or a SAT <1:80 combined with a positive Coombs Wright test (CWT) at a titre of at least threefold higher than SAT titre results...
November 21, 2016: Epidemiology and Infection
https://www.readbyqxmd.com/read/27780722/gsno-promotes-functional-recovery-in-experimental-tbi-by-stabilizing-hif-1%C3%AE
#9
Mushfiquddin Khan, Tajinder S Dhammu, Mauhamad Baarine, Jinsu Kim, Manjeet K Paintlia, Inderjit Singh, Avtar K Singh
Traumatic brain injury (TBI) causes sustained disability due to compromised neurorepair mechanisms. Crucial to neurorepair and functional recovery following both TBI and stroke is hypoxia-inducible factor-1 alpha (HIF-1α). Based on reports that HIF-1α could be stabilized via S-nitrosylation, we tested the hypothesis that the S-nitrosylating agent S-nitrosoglutathione (GSNO) would stabilize HIF-1α, thereby stimulating neurorepair mechanisms and aiding in functional recovery. TBI was induced by controlled cortical impact (CCI) in adult rats...
October 22, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27756753/benefits-of-multifaceted-chemopreventives-in-the-suppression-of-the-oral-squamous-cell-carcinoma-oscc-tumorigenic-phenotype
#10
Susan R Mallery, Daren Wang, Brian Santiago, Ping Pei, Steven P Schwendeman, Kari Nieto, Richard Spinney, Meng Tong, George Koutras, Brian Han, Andrew Holpuch, James Lang
Over one third of patients who have undergone oral squamous cell carcinoma (OSCC) surgical resections develop life-threatening and often untreatable recurrences. A variety of drugs, intended for management of recurrent or disseminated cancers, were designed to exploit cancer cells' reliance upon overexpressed receptors and gratuitous signaling. Despite their conceptual promise, clinical trials showed these agents lacked efficacy and were often toxic. These findings are consistent with evasion of pathway-targeted treatments via extensive signaling redundancies and compensatory mechanisms common to cancers...
January 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/27741574/dna-polymerase-%C3%AE-rapidly-bypasses-o-6-methyl-dg-but-not-o-6-4-3-pyridyl-4-oxobutyl-dg-and-o-2-alkyl-dts
#11
A S Prakasha Gowda, Thomas E Spratt
4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) is a potent tobacco carcinogen that forms mutagenic DNA adducts including O(6)-methyl-2'-deoxyguanosine (O(6)-Me-dG), O(6)-[4-(3-pyridyl)-4-oxobut-1-yl]-dG (O(6)-POB-dG), O(2)-methylthymidine (O(2)-Me-dT), and O(2)-POB-dT. We evaluated the ability of human DNA polymerase ν to bypass this damage to evaluate the structural constraints on substrates for pol ν and to evaluate if there is kinetic evidence suggesting the in vivo activity of pol ν on tobacco-induced DNA damage...
November 21, 2016: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/27718769/podophyllum-hexandrum-ameliorates-endosulfan-induced-genotoxicity-and-mutagenicity-in-freshwater-cyprinid-fish-crucian-carp
#12
Sabzar Ahmad Dar, Abdul Rehman Yousuf, Masood-Ul-Hassan Balkhi, Bashir Ahmad Ganai, Mudasir Tantry, Farooz Ahmad Bhat
CONTEXT: Medicinal plants continue to act as a repository for novel drug leads with novel mechanisms of action. Podophyllum hexandrum Royale (Berberideceae) treats diverse conditions in folk medicine. OBJECTIVE: The antimutagenic potential of P. hexandrum was evaluated against endosulfan-induced clastogenicity in a piscine model by cytogenetic endpoints. MATERIALS AND METHODS: Podophyllum hexandrum rhizomes were subjected to successive solvent extraction...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27643820/a-luminescent-zirconium-iv-complex-as-a-molecular-photosensitizer-for-visible-light-photoredox-catalysis
#13
Yu Zhang, Jeffrey L Petersen, Carsten Milsmann
Titanium and zirconium complexes carrying two 2,6-bis(pyrrolyl)pyridine ligands have been synthesized and characterized. The neutral complexes Ti((Me)PDP)2 and Zr((Me)PDP)2 ((Me)PDP = 2,6-bis(5-methyl-3-phenyl-1H-pyrrol-2-yl)pyridine) show intense ligand-to-metal charge-transfer bands in the visible region and undergo multiple reversible redox events under highly reducing conditions. Zr((Me)PDP)2 exhibits photoluminescent behavior and its excited state can be quenched by mild reductants to generate a powerful electron transfer reagent with a ground state potential of -2...
October 12, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27581631/different-spectrophotometric-and-tlc-densitometric-methods-for-determination-of-mesalazine-in-presence-of-its-two-toxic-impurities
#14
Martha Moheb Morcoss, Nada Sayed Abdelwahab, Nouruddin Wagieh Ali, Mohammed Taha Elsaady
Two selective spectrophotometric and TLC-densitometric methods were developed for determination of mesalazine (ME) and its two toxic impurities, 4-amino phenol (4AP) and salicylic acid (SA) without preliminary separation. The proposed methods are: ratio difference in the subtracted spectra (RDSS) {Method 1}, area under the curve (AUC) {Method 2} and TLC-densitometric {Method 3}. In method {1} combination of measuring the amplitude of the constant at 350 nm (using standard spectrum of 10 µg/mL ME as a divisor) and ratio difference in the subtracted ratio spectrum for determination of 4AP and SA using the ratio difference at 221...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27573587/discovery-of-alkenones-with-variable-methylene-interrupted-double-bonds-implications-for-the-biosynthetic-pathway
#15
Yinsui Zheng, James T Dillon, Yifan Zhang, Yongsong Huang
Alkenones (C37 -C40 ) are highly specific biomarkers produced by certain haptophyte algae in ocean and lacustrine environments and have been widely used for paleoclimate studies. Unusual shorter-chain alkenones (SCA; e.g., C35 and C36 ) have been found in environmental and culture samples, but the origin and structure of these compounds are much less understood. The marine alkenone producer, Emiliania huxleyi CCMP2758 strain, was reported with abundant C35:2 Me (∆(12, 19) ) alkenones when cultured at 15°C (Prahl et al...
December 2016: Journal of Phycology
https://www.readbyqxmd.com/read/27571142/aluminum-monohydride-catalyzed-selective-hydroboration-of-carbonyl-compounds
#16
Vineet Kumar Jakhar, Milan Kr Barman, Sharanappa Nembenna
The well-defined aluminum monohydride compound [{(2,4,6-Me3-C6H2)NC(Me)}2(Me)(H)]AlH·(NMe2Et) (1) catalyzes hydroboration of a wide range of aldehydes and ketones under mild reaction conditions. Moreover, compound 1 displayed chemoselective hydroboration of aldehydes over ketones at rt.
September 16, 2016: Organic Letters
https://www.readbyqxmd.com/read/27438708/influence-of-ancillary-ligands-and-isomerism-on-the-luminescence-of-bis-cyclometalated-platinum-iv-complexes
#17
Fabio Juliá, María-Dulce García-Legaz, Delia Bautista, Pablo González-Herrero
The synthesis, characterization, and photophysical properties of a wide variety of bis-cyclometalated Pt(IV) complexes featuring a C2-symmetrical or unsymmetrical {Pt(ppy)2} unit (sym or unsym complexes, respectively; ppy = C-deprotonated 2-phenylpyridine) and different ancillary ligands are reported. Complexes sym-[Pt(ppy)2X2] (X = OTf(-), OAc(-)) were obtained by chloride abstraction from sym-[Pt(ppy)2Cl2] using the corresponding AgX salts, and the triflate derivative was employed to obtain homologous complexes with X = F(-), Br(-), I(-), trifluoroacetate (TFA(-))...
August 1, 2016: Inorganic Chemistry
https://www.readbyqxmd.com/read/27438559/exploring-steric-effects-in-diastereoselective-synthesis-of-chiral-aminophenolate-zinc-complexes-and-stereoselective-ring-opening-polymerization-of-rac-lactide
#18
Haobing Wang, Yang Yang, Haiyan Ma
A series of tridentate chiral aminophenol proligands and corresponding zinc complexes, LZnX (L = (S)-2-{[(1-R(4)-2-pyrrolidinyl)CH2N(R(3))-]CH2}-6-R(1)-4-R(2)-C6H2O, X = N(SiMe3)2, R(3) = (n)Bu, R(4) = Bn: R(1) = R(2) = Cl (1), R(1) = R(2) = Me (2), R(1) = R(2) = (t)Bu (3); X = N(SiMe3)2, R(1) = trityl, R(2) = Me: R(3) = n-octyl, R(4) = Bn (4), R(3) = Bn, R(4) = Bn (5), R(3) = (n)Bu, R(4) = naphthalen-1-ylmethyl (6), R(3) = (n)Bu, R(4) = (i)Pr (7); R(1) = R(2) = cumyl, R(3) = Et, R(4) = Bn: X = N(SiMe3)2 (8), X = O(t)Bu (9), X = Et (10), X = Cl (11)), have been synthesized...
August 1, 2016: Inorganic Chemistry
https://www.readbyqxmd.com/read/27390871/mgi2-chemoselective-cleavage-for-removal-of-amino-acid-protecting-groups-a-fresh-vision-for-peptide-synthesis
#19
Mathéo Berthet, Jean Martinez, Isabelle Parrot
In the field of peptide synthesis, the key to a successful access to synthetic targets lies on a pertinent combination of protecting groups. Their choice is directed by their selective removal conditions. We present here the behaviour of some of the most used protecting groups in peptide chemistry under experimental cleavage conditions, combining MgI2 with MW irradiation, using 2-Me-THF as a green solvent. In these experimental conditions, the benzyloxycarbonyl protecting group as well as the Merrifield resin can be re-considered in peptide chemistry...
July 8, 2016: Biopolymers
https://www.readbyqxmd.com/read/27363580/inhibition-of-hypoxia-inducible-factor-1%C3%AE-attenuates-abdominal-aortic-aneurysm-progression-through-the-down-regulation-of-matrix-metalloproteinases
#20
Shih-Hung Tsai, Po-Hsun Huang, Yu-Juei Hsu, Yi-Jen Peng, Chien-Hsing Lee, Jen-Chun Wang, Jaw-Wen Chen, Shing-Jong Lin
Hypoxia inducible factor-1α (HIF-1α) pathway is associated with many vascular diseases, including atherosclerosis, arterial aneurysms, pulmonary hypertension and chronic venous diseases. Significant HIF-1α expression could be found at the rupture edge at human abdominal aortic aneurysm (AAA) tissues. While our initial in vitro experiments had shown that deferoxamine (DFO) could attenuate angiotensin II (AngII) induced endothelial activations; we unexpectedly found that DFO augmented the severity of AngII-induced AAA, at least partly through increased accumulation of HIF-1α...
2016: Scientific Reports
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