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https://www.readbyqxmd.com/read/28617500/decamethyltitanocene-hydride-intermediates-in-the-hydrogenation-of-the-corresponding-titanocene-%C3%AE-2-ethene-or-%C3%AE-2-alkyne-complexes-and-the-effects-of-bulkier-auxiliary-ligands
#1
Jiří Pinkas, Róbert Gyepes, Ivana Císařová, Jiří Kubišta, Michal Horáček, Karel Mach
(1)H NMR studies of reactions of titanocene [Cp*2Ti] (Cp* = η(5)-C5Me5) and its derivatives [Cp*(η(5):η(1)-C5Me4CH2)TiMe] and [Cp*2Ti(η(2)-CH2[double bond, length as m-dash]CH2)] with excess dihydrogen at room temperature and pressures lower than 1 bar revealed the formation of dihydride [Cp*2TiH2] (1) and the concurrent liberation of either methane or ethane, depending on the organometallic reactant. The subsequent slow decay of 1 yielding [Cp*2TiH] (2) was mediated by titanocene formed in situ and controlled by hydrogen pressure...
June 15, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28536143/aurora-kinase-a-promotes-ar-degradation-via-the-e3-ligase-chip
#2
Sukumar Sarkar, David L Brautigan, James M Larner
Reducing the levels of the androgen receptor (AR) is one of the most viable approaches to combat castration-resistant prostate cancer (CRPC). Previously, we observed that proteasomal-dependent degradation of AR in response to 2-methoxyestradiol (2-ME) depends primarily on the E3 ligase C-terminus of HSP70-interacting protein (STUB1/CHIP). Here, 2-ME stimulation activates CHIP by phosphorylation via Aurora kinase A (AURKA). Aurora A kinase inhibitors and RNAi knockdown of Aurora A transcript selectively blocked CHIP phosphorylation and AR degradation...
May 23, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28511459/a-comparison-of-2-methoxyestradiol-value-in-women-with-severe-preeclampsia-versus-normotensive-pregnancy
#3
John Wantania, Ahsanuddin Attamimi, Rukmono Siswishanto
INTRODUCTION: Preeclampsia is a pregnancy complication characterized by high blood pressure and proteinuria. Endothelial dysfunction is a major theory suggested as its aetiology. It is caused by anti-angiogenic condition characterized by low Vascular Endothelial Growth Factor (VEGF). An estradiol metabolite, called 2-Methoxy Estradiol (2-ME), is produced with the help of Catechol-O-Methyltransferase (COMT). This substance has an important role in VEGF expression. A 2-ME is suppressed in women with preeclampsia...
March 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28468327/quasi-living-polymerization-of-propene-with-an-isotactic-specific-zirconocene-catalyst
#4
Kei Nishii, Miyuki Murase, Takeshi Shiono
Propene polymerization with isotactic (iso)-specific C₂-symmetric rac-Me₂Si(2-Me-Benz(e)-Ind)₂ZrCl₂ (1) and rac-Me₂Si(2-Me-4-Ph-1-Ind)₂ZrCl₂ (2) were conducted under various conditions for achieving iso-specific living polymerization of propene. When Complex 1 was activated with trialkylaluminum-free modified methylaluminoxane (dMMAO) at -40 °C, the number-average molecular weight (Mn) linearly increased against the polymerization time to reach Mn = 704,000 within 15 min of polymerization, although the molecular weight distributions was broad (Mw/Mn < 3)...
May 2, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28461606/catechol-o-methyltransferase-deficiency-leads-to-hypersensitivity-of-the-pressor-response-against-angiotensin-ii
#5
Norikazu Ueki, Keizo Kanasaki, Megumi Kanasaki, Satoru Takeda, Daisuke Koya
Catechol-O-methyltransferase (COMT) metabolizes 2-hydroxyestradiol into 2-methoxyestradiol (2-ME); COMT deficiency has shown to be associated with hypertension in men and preeclampsia, the disease associated with hypersensitivity of pressor response against angiotensin II (Ang II). Here, we found that COMT deficiency could explain the hypersensitivity of pressor response against Ang II in mice because of the lack of 2-ME-dependent suppression of angiotensin II receptor type 1 (AT1R). Male C57BL/6 mice were subjected to COMT inhibitor (COMTi: 25 mg/kg per day) or oil (control) for 4 weeks, with or without low-dose Ang II infusion (ANGII: 70 ng/kg per minute) for the last 3 weeks...
June 2017: Hypertension
https://www.readbyqxmd.com/read/28396280/high-oral-bioavailability-of-2-methoxyestradiol-in-peg-plga-micelles-microspheres-for-cancer-therapy
#6
XinHong Guo, CaiPing Chen, Xin Liu, PanPan Hou, XiaoNan Guo, Fang Ding, ZhiHao Wang, YuRong Hu, Zhi Li, ZhenZhong Zhang
The development of effective oral preparations of 2-methoxyestradiol (2-ME) has been a worldwide problem. In this study, breakthrough progress has been made in oral delivery of 2-ME by encapsulating 2-ME micelles in pH-responsive microspheres. 2-ME micelles with small particle size (58 nm) and high drug loading (7.94±0.23%) were successfully prepared and showed slower release characteristics and 12.8 times higher cytotoxicity on 4T1 cells than free 2-ME. The pH-sensitive microspheres could slowly release 82% of 2-ME micelles for 10 h in PBS (7...
April 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28376733/efficacy-of-intravitreal-injection-of-2-methoxyestradiol-in-regression-of-neovascularization-of-a-retinopathy-of-prematurity-rat-model
#7
Azza Mohamed Ahmed Said, Rania Gamal Eldin Zaki, Rania A Salah Eldin, Maha Nasr, Samar Saad Azab, Yaser Abdelmageuid Elzankalony
BACKGROUND: Retinopathy of prematurity (ROP) is one of the targets for early detection and treatment to prevent childhood blindness in world health organization programs. The purpose of study was to evaluate the efficacy of intravitreal injection of 2-Methoxyestradiol (2-ME) nanoemulsion in regressing neovascularization of a ROP rat model. METHODS: A prospective comparative case - control animal study conducted on 56 eyes of 28 healthy new born Sprague Dawley male albino rat...
April 4, 2017: BMC Ophthalmology
https://www.readbyqxmd.com/read/28342193/metabolism-of-the-tryptamine-derived-new-psychoactive-substances-5-meo-2-me-dalt-5-meo-2-me-alcht-and-5-meo-2-me-dipt-and-their-detectability-in-urine-studied-by-gc-ms-lc-ms-n-and-lc-hr-ms-ms
#8
Achim T Caspar, Jonas B Gaab, Julian A Michely, Simon D Brandt, Markus R Meyer, Hans H Maurer
Many N,N-dialkylated tryptamines show psychoactive properties and were encountered as new psychoactive substances. The aims of the presented work were to study the phase I and II metabolism and the detectability in standard urine screening approaches (SUSA) of 5-methoxy-2-methyl-N,N-diallyltryptamine (5-MeO-2-Me-DALT), 5-methoxy-2-methyl-N-allyl-N-cyclohexyltryptamine (5-MeO-2-Me-ALCHT), and 5-methoxy-2-methyl-N,N-diisopropyltryptamine (5-MeO-2-Me-DIPT) using GC-MS, LC-MS(n) , and LC-HR-MS/MS. For metabolism studies, urine was collected over a 24-h period after administration of the compounds to male Wistar rats at 20 mg/kg body weight (BW)...
March 24, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28319723/occurrence-of-and-exposure-to-benzothiazoles-and-benzotriazoles-from-textiles-and-infant-clothing
#9
Wenbin Liu, Jingchuan Xue, Kurunthachalam Kannan
Benzothiazoles (BTHs) and benzotriazoles (BTRs) are used in a wide range of applications, including rubber vulcanization and corrosion inhibition. Limited studies have reported the occurrence of BTHs and BTRs in textiles, including children's clothing. In this study, 79 textile samples (raw as well as tailored) collected in Albany, New York, USA, were analyzed to determine the occurrence of BTH, BTR and their seven common derivatives. BTH, 2-methylthio-benzothiazole (2-Me-S-BTH) and 2-hydroxy-benzothiazole (2-OH-BTH) were found in textiles at a detection rate (DR) of 86%, 54% and 19%, respectively...
March 15, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28214920/detection-of-brucella-sp-infection-through-serological-microbiological-and-molecular-methods-applied-to-buffaloes-in-maranh%C3%A3-o-state-brazil
#10
Larissa Sarmento Dos Santos, Joicy Cortez Sá, Diego Luiz Dos Santos Ribeiro, Nancyleni Pinto Chaves, Juliana Pinto da Silva Mol, Renato Lima Santos, Tatiane Alves da Paixão, Alcina Vieira de Carvalho Neta
The aim of the current study is to diagnose Brucella spp. infection using methods such as serology, bacterial isolation, and molecular analysis in buffaloes bred in Maranhão State. In order to do so, 390 samples of buffalo serum were subjected to serological tests, to Rose Bengal Plate Test (RBPT) and to 2-mercaptoethanol (2-ME) combined with slow agglutination test (SAT). Vaginal swabs were collected from seropositive animals and subjected to bacterial isolation and to generic PCR. According to the serological test, 16 animals had a positive reaction to the confirmatory test (2-ME/SAT)...
February 18, 2017: Tropical Animal Health and Production
https://www.readbyqxmd.com/read/28128569/potential-energy-curves-for-the-low-lying-electronic-states-of-k2-from-ab-initio-calculations-with-all-electrons-correlated
#11
Patrycja Skupin, Monika Musiał, Stanisław A Kucharski
The electron affinity (EA) calculations based on the equation-of-motion coupled cluster method proved to be an efficient scheme in the treatment of potential energy curves (PECs) for alkali molecular ions, Me2(+). The EA approach provides description of states obtained by an attachment of one electron to the reference, which for the Me2(+) is a doubly ionized Me2(+2) system. The latter has a very concrete advantage in the calculations of the PECs, since it dissociates into the closed-shell fragments (Me2(+2) → Me(+) + Me(+)); hence, the restricted Hartree-Fock reference can be used in the whole range of interatomic distances...
February 8, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28036168/development-of-an-azoreductase-based-reporter-system-with-synthetic-fluorogenic-substrates
#12
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 fluorogenic substrates. These derivatives were nonfluorescent, probably due to ultrafast conformational change around the N═N bond after photoexcitation...
January 13, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28027603/survival-implications-of-opioid-use-before-and-after-liver-transplantation
#13
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
Implications of prescription opioid use for outcomes after liver transplantation (LT) have not been described. We integrated national transplant registry data with records from a large pharmaceutical claims clearinghouse (2008-2014; n = 29,673). Opioid fills on the waiting list were normalized to morphine equivalents (MEs), and exposure was categorized as follows: > 0-2 ME/day (level 1), > 2-10 ME/day (level 2), > 10-70 ME/day (level 3), and >70 ME/day (level 4). Associations (adjusted hazard ratio [aHR], 95% LCL aHR 95% UCL ) of pretransplant ME level with patient and graft survival over 5 years after transplant were quantified by multivariate Cox regression including adjustment for recipient, donor, and transplant factors, as well as propensity adjustment for opioid use...
March 2017: 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
#14
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...
March 1, 2017: Life Sciences
https://www.readbyqxmd.com/read/27928078/polymerase-chain-reaction-based-assays-for-the-diagnosis-of-active-and-relapsed-cases-of-human-brucellosis
#15
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
#16
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...
April 2017: Journal of Palliative Medicine
https://www.readbyqxmd.com/read/27911395/preparation-of-primary-mixed-glial-cultures-from-adult-mouse-spinal-cord-tissue
#17
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
#18
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...
June 2017: 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
#19
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...
February 2017: Epidemiology and Infection
https://www.readbyqxmd.com/read/27780722/gsno-promotes-functional-recovery-in-experimental-tbi-by-stabilizing-hif-1%C3%AE
#20
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
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